Sharing the latest findings and technologies within the scientific community is crucial to driving science forward. Explore our list of publications from NUVISAN's team of scientists and get to know the fascinating research stories they have unraveled, often in collaboration with our partners from academia and industry. These include topics covering a wide range of areas along the value chain, from early drug discovery to clinical studies. For further information, please send an email to hello@nuvisan.com.
Günther, J. et al. BAY-069, a Novel (Trifluoromethyl)pyrimidinedione-Based BCAT1/2 Inhibitor and Chemical Probe. J. Med. Chem. 65, 14366–14390 (2022).
Orsi, D. L. et al. Discovery and Structure-Based Design of Potent Covalent PPARγ Inverse-Agonists BAY-4931 and BAY-0069. Journal of Medicinal Chemistry 65, 14843–14863 (2022).
Diamanti, E. et al. Frontiers in Medicinal Chemistry 2022 Goes Virtual. ChemMedChem e202200419 (2022) doi:10.1002/cmdc.202200419.
Billié, S. et al. Completion of the impurity profile of lymecycline: Formal identification of impurities E and F. Journal of Pharmaceutical and Biomedical Analysis 220, 114993 (2022).
Boiteau, J.-G. et al. Complete 1 H, 13 C, and 15 N assignments of the minor isomer of codeine N-oxide. Magnetic resonance in chemistry: MRC (2022) doi:10.1002/mrc.5302.
Regan, J. L. et al. Identification of a neural development gene expression signature in colon cancer stem cells reveals a role for EGR2 in tumorigenesis. iScience 25, 104498 (2022).
J Cowan, K. et al. Biomarker context-of-use: how organizational design can impact the implementation of the appropriate biomarker assay strategy. Bioanalysis 14, 911–917 (2022).
Karwelat, D. et al. A rodent thyroid-liver chip to capture thyroid toxicity on organ functional level. ALTEX (2022) doi:10.14573/altex.2108262.
Henß, T. et al. Optogenetic tools for manipulation of cyclic nucleotides functionally coupled to cyclic nucleotide-gated channels. British Journal of Pharmacology 179, 2519–2537 (2022).
Chume, F. C., Freitas, P. A. C., Schiavenin, L. G., Pimentel, A. L. & Camargo, J. L. Glycated albumin in diabetes mellitus: a meta-analysis of diagnostic test accuracy. Clinical Chemistry and Laboratory Medicine 60, 961–974 (2022).
Hohlbaum, K. et al. Effects of separated pair housing of female C57BL/6JRj mice on well-being. Scientific Reports 12, 8819 (2022).
Novak, B. et al. Clinical Pharmacokinetics and Safety of a 10% Aminolevulinic Acid Hydrochloride Nanoemulsion Gel (BF-200 ALA) in Photodynamic Therapy of Patients Extensively Affected With Actinic Keratosis: Results of 2 Maximal Usage Pharmacokinetic Trials. Clinical Pharmacology in Drug Development 11, 535–550 (2022).
Alborzinia, H. et al. MYCN mediates cysteine addiction and sensitizes neuroblastoma to ferroptosis. Nature Cancer 3, 471–485 (2022).
Del Amo, E. M. et al. Ocular metabolism and distribution of drugs in the rabbit eye: Quantitative assessment after intracameral and intravitreal administrations. International Journal of Pharmaceutics 613, 121361 (2022).
Müller, S. et al. Target 2035 - update on the quest for a probe for every protein. RSC medicinal chemistry 13, 13–21 (2022).
Lerchen, H.-G. et al. A Small Molecule-Drug Conjugate (SMDC) Consisting of a Modified Camptothecin Payload Linked to an αVß3 Binder for the Treatment of Multiple Cancer Types. Cancers 14, 391 (2022).
Bobylev, D. et al. Pressure-compacted and spider silk-reinforced fibrin demonstrates sufficient biomechanical stability as cardiac patch in vitro. J Biomater Appl 36, 1126–1136 (2022).
Bertani, V., Blanck, O., Guignard, D., Schorsch, F. & Pischon, H. Artificial Intelligence in Toxicological Pathology: Quantitative Evaluation of Compound-Induced Follicular Cell Hypertrophy in Rat Thyroid Gland Using Deep Learning Models. Toxicologic Pathology 50, 23–34 (2022).
Pla, L. et al. Protocols for the Evaluation of Neurodevelopmental Alterations in Rabbit Models In Vitro and In Vivo. Frontiers in Toxicology 4, 918520 (2022).
Pinkert, J. et al. T cell-mediated elimination of cancer cells by blocking CEACAM6-CEACAM1 interaction. Oncoimmunology 11, 2008110 (2022).
Hillig, R. C. & Bader, B. Targeting RAS oncogenesis with SOS1 inhibitors. Advances in Cancer Research 153, 169–203 (2022).
2021
Lau, S., Gossen, M. & Lendlein, A. Designing Cardiovascular Implants Taking in View the Endothelial Basement Membrane. Int J Mol Sci 22, 13120 (2021).
Munday, C. et al. Feedback from the Science Café at the 7th European Bioanalysis Forum Young Scientist Symposium. Bioanalysis 13, 1793–1798 (2021).
Klaus, M. et al. Ultrahigh-Throughput Detection of Enzymatic Alcohol Dehydrogenase Activity in Microfluidic Droplets with a Direct Fluorogenic Assay. Chembiochem: A European Journal of Chemical Biology 22, 3292–3299 (2021).
Bannik, K. et al. DNA repair inhibitors sensitize cells differently to high and low LET radiation. Scientific Reports 11, 23257 (2021).
Wortmann, L. et al. Discovery and Characterization of the Potent and Highly Selective 1,7-Naphthyridine-Based Inhibitors BAY-091 and BAY-297 of the Kinase PIP4K2A. Journal of Medicinal Chemistry 64, 15883–15911 (2021).
Peirsman, A. et al. MISpheroID: a knowledgebase and transparency tool for minimum information in spheroid identity. Nature Methods 18, 1294–1303 (2021).
Timmerman, P. et al. Recommendations and discussion points on immunogenicity, biomarkers, automation/technology and protein-MS from the 2021 European Bioanalysis Forum Focus Workshops. Bioanalysis 13, 1459–1465 (2021).
Port, A. et al. Phase 1 study in healthy participants of the safety, pharmacokinetics, and pharmacodynamics of enpatoran (M5049), a dual antagonist of toll-like receptors 7 and 8. Pharmacology Research & Perspectives 9, e00842 (2021).
Davenport, A. J. et al. Eliapixant is a selective P2X3 receptor antagonist for the treatment of disorders associated with hypersensitive nerve fibers. Scientific Reports 11, 19877 (2021).
Doleschel, D. et al. Regorafenib enhances anti-PD1 immunotherapy efficacy in murine colorectal cancers and their combination prevents tumor regrowth. J Exp Clin Cancer Res 40, 288 (2021).
Gradl, S. et al. Discovery of the SMYD3 Inhibitor BAY-6035 Using Thermal Shift Assay (TSA)-Based High-Throughput Screening. SLAS discovery: advancing life sciences R & D 26, 947–960 (2021).
Berger, M. et al. BAY-8400: A Novel Potent and Selective DNA-PK Inhibitor which Shows Synergistic Efficacy in Combination with Targeted Alpha Therapies. Journal of Medicinal Chemistry 64, 12723–12737 (2021).
Lücking, U. et al. Changing for the Better: Discovery of the Highly Potent and Selective CDK9 Inhibitor VIP152 Suitable for Once Weekly Intravenous Dosing for the Treatment of Cancer. Journal of Medicinal Chemistry 64, 11651–11674 (2021).
Evans, C. M. et al. Coordination of Di-Acetylated Histone Ligands by the ATAD2 Bromodomain. International Journal of Molecular Sciences 22, 9128 (2021).
Garvie, C. W. et al. Structure of PDE3A-SLFN12 complex reveals requirements for activation of SLFN12 RNase. Nature Communications 12, 4375 (2021).
Dieter, S. M. et al. Degradation of CCNK/CDK12 is a druggable vulnerability of colorectal cancer. Cell Reports 36, 109394 (2021).
Witte, F. et al. A trans locus causes a ribosomopathy in hypertrophic hearts that affects mRNA translation in a protein length-dependent fashion. Genome Biology 22, 191 (2021).
Taavitsainen, P. et al. Metabolism and Mass Balance of the Novel Nonsteroidal Androgen Receptor Inhibitor Darolutamide in Humans. Drug Metabolism and Disposition: The Biological Fate of Chemicals 49, 420–433 (2021).
Regan, J. L. et al. RNA sequencing of long-term label-retaining colon cancer stem cells identifies novel regulators of quiescence. iScience 24, 102618 (2021).
Pischon, H. et al. Artificial Intelligence in Toxicologic Pathology: Quantitative Evaluation of Compound-Induced Hepatocellular Hypertrophy in Rats. Toxicologic Pathology 49, 928–937 (2021).
Lemos, C. et al. The potent AMPK inhibitor BAY-3827 shows strong efficacy in androgen-dependent prostate cancer models. Cellular Oncology (Dordrecht) 44, 581–594 (2021).
Krause, B. C. et al. Combinatory Effects of Cerium Dioxide Nanoparticles and Acetaminophen on the Liver-A Case Study of Low-Dose Interactions in Human HuH-7 Cells. International Journal of Molecular Sciences 22, 6866 (2021).
Kammertoens, T., Jeuthe, S., Baranzke, H., Klippert, A. & Thöne-Reineke, C. Breeding and Maintenance of Immunodeficient Mouse Lines under SPF Conditions-A Call for Individualized Severity Analyses and Approval Procedures. Animals: an open access journal from MDPI 11, 1789 (2021).
Wick, A. et al. Phase I Assessment of Safety and Therapeutic Activity of BAY1436032 in Patients with IDH1-Mutant Solid Tumors. Clin Cancer Res 27, 2723–2733 (2021).
Suominen, M. I. et al. Additive Benefits of Radium-223 Dichloride and Bortezomib Combination in a Systemic Multiple Myeloma Mouse Model. International Journal of Molecular Sciences 22, 5570 (2021).
Lissy, M. et al. Thorough QT/QTc Study Evaluating the Effect of Macimorelin on Cardiac Safety Parameters in Healthy Participants. Clinical Pharmacology in Drug Development 10, 494–501 (2021).
Hahn, M. G. et al. Discovery of the Soluble Guanylate Cyclase Activator Runcaciguat (BAY 1101042). Journal of Medicinal Chemistry 64, 5323–5344 (2021).
Delahaye, L. et al. Feedback from the Sixth European Bioanalysis Forum Young Scientist Symposium. Bioanalysis 13, 669–674 (2021).
Sutherland, M. et al. Rational Design and Synthesis of Selective PRMT4 Inhibitors: A New Chemotype for Development of Cancer Therapeutics*. ChemMedChem 16, 1116–1125 (2021).
Liu, D. et al. Nickel-Catalyzed N-Arylation of NH-Sulfoximines with Aryl Halides via Paired Electrolysis. Angewandte Chemie (International Ed. in English) 60, 9444–9449 (2021).
Ede, S., Schenk, M., Bierer, D., Weinmann, H. & Graham, K. Improved Diazo-Transfer Reaction for DNA-Encoded Chemistry and Its Potential Application for Macrocyclic DEL-Libraries. Molecules (Basel, Switzerland) 26, 1790 (2021).
Chaturvedi, A. et al. Synergistic activity of IDH1 inhibitor BAY1436032 with azacitidine in IDH1 mutant acute myeloid leukemia. Haematologica 106, 565–573 (2021).
Moosmayer, D. et al. Crystal structures of the selenoprotein glutathione peroxidase 4 in its apo form and in complex with the covalently bound inhibitor ML162. Acta Crystallographica. Section D, Structural Biology 77, 237–248 (2021).
Calogero, S. et al. Feedback from the Science Café from the Sixth European Bioanalysis Forum Young Scientist Symposium. Bioanalysis 13, 129–133 (2021).
Atilaw, Y. et al. Solution Conformations Shed Light on PROTAC Cell Permeability. ACS medicinal chemistry letters 12, 107–114 (2021).
Speck, D. et al. Expression and Characterization of Relaxin Family Peptide Receptor 1 Variants. Frontiers in Pharmacology 12, 826112 (2021).
2020
Shigeta, K. et al. Regorafenib combined with PD1 blockade increases CD8 T-cell infiltration by inducing CXCL10 expression in hepatocellular carcinoma. J Immunother Cancer 8, e001435 (2020).
Hillisch, A. et al. Design, Synthesis, and Pharmacological Characterization of a Neutral, Non-Prodrug Thrombin Inhibitor with Good Oral Pharmacokinetics. Journal of Medicinal Chemistry 63, 12574–12594 (2020).
Heuser, M. et al. Safety and efficacy of BAY1436032 in IDH1-mutant AML: phase I study results. Leukemia 34, 2903–2913 (2020).
Wenger, K. J. et al. Non-Invasive Measurement of Drug and 2-HG Signals Using 19F and 1H MR Spectroscopy in Brain Tumors Treated with the Mutant IDH1 Inhibitor BAY1436032. Cancers (Basel) 12, 3175 (2020).
Panknin, O. et al. Discovery and Characterization of BAY 1214784, an Orally Available Spiroindoline Derivative Acting as a Potent and Selective Antagonist of the Human Gonadotropin-Releasing Hormone Receptor as Proven in a First-In-Human Study in Postmenopausal Women. Journal of Medicinal Chemistry 63, 11854–11881 (2020).
Goodman, J. et al. Update to the European Bioanalysis Forum recommendation on biomarkers assays; bringing context of use into practice. Bioanalysis 12, 1427–1437 (2020).
Agueusop, I., Musholt, P. B., Klaus, B., Hightower, K. & Kannt, A. Short-term variability of the human serum metabolome depending on nutritional and metabolic health status. Scientific Reports 10, 16310 (2020).
Luh, L. M. et al. Prey for the Proteasome: Targeted Protein Degradation-A Medicinal Chemist’s Perspective. Angewandte Chemie (International Ed. in English)59, 15448–15466 (2020).
Lemos, C. et al. Identification of Small Molecules that Modulate Mutant p53 Condensation. iScience 23, 101517 (2020).
Vizán, P. et al. The Polycomb-associated factor PHF19 controls hematopoietic stem cell state and differentiation. Sci Adv 6, eabb2745 (2020).
Taavitsainen, P. et al. Absorption, distribution, metabolism and excretion of darolutamide (a novel non-steroidal androgen receptor antagonist) in rats. Xenobiotica; the Fate of Foreign Compounds in Biological Systems 50, 967–979 (2020).
Schulze, V. K. et al. Treating Cancer by Spindle Assembly Checkpoint Abrogation: Discovery of Two Clinical Candidates, BAY 1161909 and BAY 1217389, Targeting MPS1 Kinase. Journal of Medicinal Chemistry 63, 8025–8042 (2020).
Werbeck, N. D. et al. A distal regulatory region of a class I human histone deacetylase. Nature Communications 11, 3841 (2020).
Lücking, U. et al. Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models. Journal of Medicinal Chemistry 63, 7293–7325 (2020).
Huetter, J. et al. Characterization of BAY 1905254, an Immune Checkpoint Inhibitor Targeting the Immunoglobulin-Like Domain Containing Receptor 2 (ILDR2). Cancer Immunol Res 8, 895–911 (2020).
Zhao, X.-Y. et al. Targeted inhibition of activated protein C by a non-active-site inhibitory antibody to treat hemophilia. Nature Communications 11, 2992 (2020).
Klaus, B., Sachse, R., Ammer, N., Kelepouris, N. & Ostrow, V. Safety, tolerability, pharmacokinetics, and pharmacodynamics of macimorelin in healthy adults: Results of a single-dose, randomized controlled study. Growth hormone & IGF research: official journal of the Growth Hormone Research Society and the International IGF Research Society 52, 101321 (2020).
Gupta, C. et al. Combination treatment of an IDH1 inhibitor with chemotherapy in IDH1 mutant acute myeloid leukemia. Ann Hematol 99, 1415–1417 (2020).
Friberg, A. et al. Structural Evidence for Isoform-Selective Allosteric Inhibition of Lactate Dehydrogenase A. ACS omega 5, 13034–13041 (2020).
Mortier, J. et al. Computationally Empowered Workflow Identifies Novel Covalent Allosteric Binders for KRASG12C. ChemMedChem 15, 827–832 (2020).
Eaton, J. K. et al. Selective covalent targeting of GPX4 using masked nitrile-oxide electrophiles. Nature Chemical Biology 16, 497–506 (2020).
Hammer, S. et al. Preclinical Efficacy of a PSMA-Targeted Thorium-227 Conjugate (PSMA-TTC), a Targeted Alpha Therapy for Prostate Cancer. Clin Cancer Res 26, 1985–1996 (2020).
Khan, M. et al. Hepatocyte Growth Factor Receptor overexpression predicts reduced survival but its targeting is not effective in unselected HNSCC patients. Head Neck 42, 625–635 (2020).
Boulard, E. et al. Increasing Complexity: A Practical Synthetic Approach to Three-Dimensional, Cyclic Sulfoximines and First Insights into Their in Vitro Properties. Chemistry (Weinheim an Der Bergstrasse, Germany) 26, 4378–4388 (2020).
Tarantelli, C. et al. Copanlisib synergizes with conventional and targeted agents including venetoclax in B- and T-cell lymphoma models. Blood Adv 4, 819–829 (2020).
Wu, X. et al. Mechanistic insights into cancer cell killing through interaction of phosphodiesterase 3A and schlafen family member 12. The Journal of Biological Chemistry 295, 3431–3446 (2020).
Timmerman, P. et al. European Bioanalysis Forum feedback on draft ICH M10 guideline on bioanalytical method validation during the Step 2b public consultation period. Bioanalysis 12, 1–11 (2020).
Parker, V. E. R. et al. Efficacy, Safety, and Mechanistic Insights of Cotadutide, a Dual Receptor Glucagon-Like Peptide-1 and Glucagon Agonist. The Journal of Clinical Endocrinology and Metabolism 105, dgz047 (2020).
Wengner, A. M. et al. The Novel ATR Inhibitor BAY 1895344 Is Efficacious as Monotherapy and Combined with DNA Damage-Inducing or Repair-Compromising Therapies in Preclinical Cancer Models. Molecular Cancer Therapeutics 19, 26–38 (2020).
Lefranc, J. et al. Discovery of BAY-985, a Highly Selective TBK1/IKKε Inhibitor. Journal of Medicinal Chemistry 63, 601–612 (2020).
for The European Childhood Obesity Trial Study Group et al. Impact of infant protein supply and other early life factors on plasma metabolome at 5.5 and 8 years of age: a randomized trial. Int J Obes 44, 69–81 (2020).
Brzezinka, K. et al. Characterization of the Menin-MLL Interaction as Therapeutic Cancer Target. Cancers 12, E201 (2020).
2019
Zurth, C. et al. Drug-Drug Interaction Potential of Darolutamide: In Vitro and Clinical Studies. European Journal of Drug Metabolism and Pharmacokinetics 44, 747–759 (2019).
Werner, S. et al. Discovery and Characterization of the Potent and Selective P2X4 Inhibitor N-[4-(3-Chlorophenoxy)-3-sulfamoylphenyl]-2-phenylacetamide (BAY-1797) and Structure-Guided Amelioration of Its CYP3A4 Induction Profile. Journal of Medicinal Chemistry 62, 11194–11217 (2019).
Schaefer, M., Buchmueller, A., Dittmer, F., Straßburger, J. & Wilmen, A. Allosteric Inhibition as a New Mode of Action for BAY 1213790, a Neutralizing Antibody Targeting the Activated Form of Coagulation Factor XI. Journal of Molecular Biology 431, 4817–4833 (2019).
Rauschert, S. et al. Phospholipids in lipoproteins: compositional differences across VLDL, LDL, and HDL in pregnant women. Lipids Health Dis 18, 20 (2019).
Marchioro, L. et al. Effect of a low glycaemic index diet during pregnancy on maternal and cord blood metabolomic profiles: results from the ROLO randomized controlled trial. Nutr Metab (Lond) 16, 59 (2019).
Li, Y. et al. Metabolic labelling of choline phospholipids probes ABCA3 transport in lamellar bodies. Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids 1864, 158516 (2019).
Georgi, V., Dubrovskiy, A., Steigele, S. & Fernández‐Montalván, A. E. Considerations for improved performance of competition association assays analysed with the Motulsky–Mahan’s “kinetics of competitive binding” model. Br J Pharmacol 176, 4731–4744 (2019).
Bagheri, M. et al. Plasma metabolomic profiling of amino acids and polar lipids in Iranian obese adults. Lipids Health Dis 18, 94 (2019).
Wortmann, L. et al. Discovery of BAY-298 and BAY-899: Tetrahydro-1,6-naphthyridine-Based, Potent, and Selective Antagonists of the Luteinizing Hormone Receptor Which Reduce Sex Hormone Levels in Vivo. Journal of Medicinal Chemistry 62, 10321–10341 (2019).
Shokry, E. et al. Prolonged monitoring of postprandial lipid metabolism after a western meal rich in linoleic acid and carbohydrates. Appl. Physiol. Nutr. Metab. 44, 1189–1198 (2019).
Lewis, T. A. et al. Optimization of PDE3A Modulators for SLFN12-Dependent Cancer Cell Killing. ACS medicinal chemistry letters 10, 1537–1542 (2019).
Shore, N. et al. Evaluation of Clinically Relevant Drug-Drug Interactions and Population Pharmacokinetics of Darolutamide in Patients with Nonmetastatic Castration-Resistant Prostate Cancer: Results of Pre-Specified and Post Hoc Analyses of the Phase III ARAMIS Trial. Targeted Oncology 14, 527–539 (2019).
Pihl, S. et al. EBF recommendation on practical management of critical reagents for antidrug antibody ligand-binding assays. Bioanalysis 11, 1787–1798 (2019).
Christian, S. et al. The novel dihydroorotate dehydrogenase (DHODH) inhibitor BAY 2402234 triggers differentiation and is effective in the treatment of myeloid malignancies. Leukemia 33, 2403–2415 (2019).
Lexhaller, B., Ludwig, C. & Scherf, K. A. Comprehensive Detection of Isopeptides between Human Tissue Transglutaminase and Gluten Peptides. Nutrients 11, 2263 (2019).
Caldwell, R. D. et al. Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton’s Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases. J. Med. Chem. 62, 7643–7655 (2019).
Shokry, E. et al. Transgenerational cycle of obesity and diabetes: investigating possible metabolic precursors in cord blood from the PREOBE study. Acta Diabetol 56, 1073–1082 (2019).
Shokry, E. et al. Investigation of the impact of birth by cesarean section on fetal and maternal metabolism. Arch Gynecol Obstet 300, 589–600 (2019).
Koppitz, M. et al. Discovery and optimization of pyridyl-cycloalkyl-carboxylic acids as inhibitors of microsomal prostaglandin E synthase-1 for the treatment of endometriosis. Bioorganic & Medicinal Chemistry Letters 29, 2700–2705 (2019).
Grünewald, S. et al. Rogaratinib: A potent and selective pan-FGFR inhibitor with broad antitumor activity in FGFR-overexpressing preclinical cancer models. International Journal of Cancer 145, 1346–1357 (2019).
Sebert, S. et al. Cohort Profile: The DynaHEALTH consortium – a European consortium for a life-course bio-psychosocial model of healthy ageing of glucose homeostasis. International Journal of Epidemiology 48, 1051–1051k (2019).
Hagemann, U. B. et al. Mesothelin-Targeted Thorium-227 Conjugate (MSLN-TTC): Preclinical Evaluation of a New Targeted Alpha Therapy for Mesothelin-Positive Cancers. Clin Cancer Res 25, 4723–4734 (2019).
Zahner, C. et al. No Clinically Relevant Interactions of St. John’s Wort Extract Ze 117 Low in Hyperforin With Cytochrome P450 Enzymes and P-glycoprotein. Clinical Pharmacology and Therapeutics 106, 432–440 (2019).
Protti, M. et al. Feedback from the Fifth European Bioanalysis Forum Young Scientist Symposium. Bioanalysis 11, 1453–1458 (2019).
Möller, P. et al. The RNase YbeY Is Vital for Ribosome Maturation, Stress Resistance, and Virulence of the Natural Genetic Engineer Agrobacterium tumefaciens. J Bacteriol 201, (2019).
Brzezinka, K. et al. Functional diversity of inhibitors tackling the differentiation blockage of MLL-rearranged leukemia. Journal of Hematology & Oncology 12, 66 (2019).
Bosma, R. et al. Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor. Sci Rep 9, 7906 (2019).
Shokry, E. et al. Impact of maternal BMI and gestational diabetes mellitus on maternal and cord blood metabolome: results from the PREOBE cohort study. Acta Diabetol 56, 421–430 (2019).
Hellmuth, C. et al. An individual participant data meta-analysis on metabolomics profiles for obesity and insulin resistance in European children. Sci Rep 9, 5053 (2019).
Bäurle, S. et al. Identification of a Benzimidazolecarboxylic Acid Derivative ( BAY 1316957 ) as a Potent and Selective Human Prostaglandin E2 Receptor Subtype 4 (hEP4-R) Antagonist for the Treatment of Endometriosis. J. Med. Chem. 62, 2541–2563 (2019).
Siemeister, G. et al. Inhibition of BUB1 Kinase by BAY 1816032 Sensitizes Tumor Cells toward Taxanes, ATR, and PARP Inhibitors In Vitro and In Vivo. Clin Cancer Res 25, 1404–1414 (2019).
Vriens, K. et al. Evidence for an alternative fatty acid desaturation pathway increasing cancer plasticity. Nature 566, 403–406 (2019).
Hillig, R. C. et al. Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1 interaction. Proceedings of the National Academy of Sciences of the United States of America 116, 2551–2560 (2019).
Wilson, A. et al. European Bioanalysis Forum recommendation on the best practices to demonstrate processed sample stability. Bioanalysis 11, 7–11 (2019).
Nguyen, D. et al. Discovery and Characterization of the Potent and Highly Selective (Piperidin-4-yl)pyrido[3,2- d]pyrimidine Based in Vitro Probe BAY-885 for the Kinase ERK5. Journal of Medicinal Chemistry 62, 928–940 (2019).
Hellmuth, C. et al. Maternal Metabolomic Profile and Fetal Programming of Offspring Adiposity: Identification of Potentially Protective Lipid Metabolites. Mol. Nutr. Food Res. 63, 1700889 (2019).
Farinacci, M. et al. Circulating endothelial cells as biomarker for cardiovascular diseases. Res Pract Thromb Haemost 3, 49–58 (2019).
Renders, L. et al. First-in-human Phase I studies of PRS-080#22, a hepcidin antagonist, in healthy volunteers and patients with chronic kidney disease undergoing hemodialysis. PloS One 14, e0212023 (2019).
2018
Georgi, V. et al. Binding Kinetics Survey of the Drugged Kinome. J. Am. Chem. Soc. 140, 15774–15782 (2018).
Quanz, M. et al. Preclinical Efficacy of the Novel Monocarboxylate Transporter 1 Inhibitor BAY-8002 and Associated Markers of Resistance. Molecular Cancer Therapeutics 17, 2285–2296 (2018).
Kall, M. A. et al. Incurred sample reproducibility: 10 years of experiences: views and recommendations from the European Bioanalysis Forum. Bioanalysis 10, 1723–1732 (2018).
de Witte, W. E. A. et al. In vitro and in silico analysis of the effects of D 2 receptor antagonist target binding kinetics on the cellular response to fluctuating dopamine concentrations: The D 2 antagonist k off and cAMP response. British Journal of Pharmacology 175, 4121–4136 (2018).
Pihl, S. et al. EBF recommendation on practical management of critical reagents for PK ligand-binding assays. Bioanalysis 10, 1557–1565 (2018).
Bagheri, M. et al. Effectiveness of vitamin D therapy in improving metabolomic biomarkers in obesity phenotypes: Two randomized clinical trials. Int J Obes 42, 1782–1796 (2018).
Quanz, M. et al. Anetumab ravtansine inhibits tumor growth and shows additive effect in combination with targeted agents and chemotherapy in mesothelin-expressing human ovarian cancer models. Oncotarget 9, 34103–34121 (2018).
Gázquez, A. et al. Placental lipid droplet composition: Effect of a lifestyle intervention (UPBEAT) in obese pregnant women. Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids 1863, 998–1005 (2018).
Timmerman, P. et al. Toward decision-based acceptance criteria for Bioanalytical Method Validation: a proposal for discussion from the European Bioanalysis Forum. Bioanalysis 10, 1255–1259 (2018).
Schultze-Mosgau, M.-H. et al. Characterization of the Pharmacokinetics of Vilaprisan: Bioavailability, Excretion, Biotransformation, and Drug-Drug Interaction Potential. Clinical Pharmacokinetics 57, 1001–1015 (2018).
Bunse, L. et al. Suppression of antitumor T cell immunity by the oncometabolite (R)-2-hydroxyglutarate. Nat Med 24, 1192–1203 (2018).
Khaznadar, S. S. et al. EGFR overexpression is not common in patients with head and neck cancer. Cell lines are not representative for the clinical situation in this indication. Oncotarget 9, 28965–28975 (2018).
Heroven, C. et al. Halogen-Aromatic π Interactions Modulate Inhibitor Residence Times. Angew. Chem. Int. Ed. 57, 7220–7224 (2018).
Hellmuth, C. et al. The impact of human breast milk components on the infant metabolism. PLoS ONE 13, e0197713 (2018).
Ulbrich, S. et al. Alterations in the brain interactome of the intrinsically disordered N-terminal domain of the cellular prion protein (PrPC) in Alzheimer’s disease. PLoS ONE 13, e0197659 (2018).
Engelke, A. D. et al. Dimerization of the cellular prion protein inhibits propagation of scrapie prions. Journal of Biological Chemistry 293, 8020–8031 (2018).
Bagheri, M. et al. Obesity-Related Metabolomic Profiles and Discrimination of Metabolically Unhealthy Obesity. J. Proteome Res. 17, 1452–1462 (2018).
Klutzny, S. et al. PDE5 inhibition eliminates cancer stem cells via induction of PKA signaling. Cell Death & Disease 9, 192 (2018).
Goodman, J. et al. Feedback from the European Bioanalysis Forum: focus workshop on current analysis of immunogenicity: best practices and regulatory hurdles. Bioanalysis 10, 197–204 (2018).
Patel, N. et al. Cord Metabolic Profiles in Obese Pregnant Women: Insights Into Offspring Growth and Body Composition. J Clin Endocrinol Metab 103, 346–355 (2018).
Botzenhardt, S. et al. Long-term safety of deferiprone treatment in children from the Mediterranean region with beta-thalassemia major: the DEEP-3 multi-center observational safety study. Haematologica 103, e1–e4 (2018).
Koletzko, B. et al. Metabolic Regulation of Pre- and Postnatal Growth. in Nestlé Nutrition Institute Workshop Series (eds. Colombo, J., Koletzko, B. & Lampl, M.) vol. 89 79–91 (S. Karger AG, 2018).
2017
Lexhaller, B., Tompos, C. & Scherf, K. A. Fundamental study on reactivities of gluten protein types from wheat, rye and barley with five sandwich ELISA test kits. Food Chem 237, 320–330 (2017).
Regan, J. L. et al. Non-Canonical Hedgehog Signaling Is a Positive Regulator of the WNT Pathway and Is Required for the Survival of Colon Cancer Stem Cells. Cell Rep 21, 2813–2828 (2017).
Kissel, M. et al. Antitumor effects of regorafenib and sorafenib in preclinical models of hepatocellular carcinoma. Oncotarget 8, 107096–107108 (2017).
Lücking, U. et al. Identification of Atuveciclib (BAY 1143572), the First Highly Selective, Clinical PTEFb/CDK9 Inhibitor for the Treatment of Cancer. ChemMedChem 12, 1776–1793 (2017).
Brychta, N. et al. Isolation of circulating tumor cells from pancreatic cancer by automated filtration. Oncotarget 8, 86143–86156 (2017).
Chaturvedi, A. et al. Pan-mutant-IDH1 inhibitor BAY1436032 is highly effective against human IDH1 mutant acute myeloid leukemia in vivo. Leukemia 31, 2020–2028 (2017).
Ellermann, M. et al. Novel Class of Potent and Cellularly Active Inhibitors Devalidates MTH1 as Broad-Spectrum Cancer Target. ACS chemical biology 12, 1986–1992 (2017).
Schuetz, D. A. et al. Kinetics for Drug Discovery: an industry-driven effort to target drug residence time. Drug Discovery Today 22, 896–911 (2017).
Ericzon, B.-G. et al. Pharmacokinetics of prolonged-release tacrolimus versus immediate-release tacrolimus in de novo liver transplantation: A randomized phase III substudy. Clinical Transplantation 31, (2017).
Willuda, J. et al. Preclinical Antitumor Efficacy of BAY 1129980-a Novel Auristatin-Based Anti-C4.4A (LYPD3) Antibody-Drug Conjugate for the Treatment of Non-Small Cell Lung Cancer. Molecular Cancer Therapeutics 16, 893–904 (2017).
Undre, N. & Dickinson, J. Relative bioavailability of single doses of prolonged-release tacrolimus administered as a suspension, orally or via a nasogastric tube, compared with intact capsules: a phase 1 study in healthy participants. BMJ open 7, e012252 (2017).
Santag, S. et al. BAY 1143269, a novel MNK1 inhibitor, targets oncogenic protein expression and shows potent anti-tumor activity. Cancer Letters 390, 21–29 (2017).
Pusch, S. et al. Pan-mutant IDH1 inhibitor BAY 1436032 for effective treatment of IDH1 mutant astrocytoma in vivo. Acta Neuropathologica 133, 629–644 (2017).
Klutzny, S. et al. Functional inhibition of acid sphingomyelinase by Fluphenazine triggers hypoxia-specific tumor cell death. Cell Death & Disease 8, e2709 (2017).
Botzenhardt, S. et al. Safety profiles of iron chelators in young patients with haemoglobinopathies. Eur J Haematol 98, 198–217 (2017).
Basit, F. et al. Mitochondrial complex I inhibition triggers a mitophagy-dependent ROS increase leading to necroptosis and ferroptosis in melanoma cells. Cell Death & Disease 8, e2716 (2017).
Schütte, M. et al. Molecular dissection of colorectal cancer in pre-clinical models identifies biomarkers predicting sensitivity to EGFR inhibitors. Nat Commun 8, 14262 (2017).
Henze, D. et al. Endometriosis Leads to an Increased Trefoil Factor 3 Concentration in the Peritoneal Cavity but Does Not Alter Systemic Levels. Reprod Sci 24, 258–267 (2017).
Paul, J. et al. Simultaneous Inhibition of PI3Kδ and PI3Kα Induces ABC-DLBCL Regression by Blocking BCR-Dependent and -Independent Activation of NF-κB and AKT. Cancer Cell 31, 64–78 (2017).
Politz, O. et al. BAY 1125976, a selective allosteric AKT1/2 inhibitor, exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models. International Journal of Cancer 140, 449–459 (2017).
Schmid, E. et al. Detection of MET mRNA in gastric cancer in situ. Comparison with immunohistochemistry and sandwich immunoassays. Biotech Histochem 92, 425–435 (2017).
Schalk, K., Lexhaller, B., Koehler, P. & Scherf, K. A. Isolation and characterization of gluten protein types from wheat, rye, barley and oats for use as reference materials. PLoS One 12, e0172819 (2017).
Georgi, V. et al. Binding kinetics in drug discovery - A current perspective. Front Biosci 22, 21–47 (2017).
2016
Botzenhardt, S., Rashed, A. N., Wong, I. C. K., Tomlin, S. & Neubert, A. Analgesic Drug Prescription Patterns on Five International Paediatric Wards. Paediatr Drugs 18, 465–473 (2016).
Zopf, D. et al. Pharmacologic activity and pharmacokinetics of metabolites of regorafenib in preclinical models. Cancer Med 5, 3176–3185 (2016).
Sommer, A. et al. Preclinical Efficacy of the Auristatin-Based Antibody-Drug Conjugate BAY 1187982 for the Treatment of FGFR2-Positive Solid Tumors. Cancer Research 76, 6331–6339 (2016).
Brychta, N., Krahn, T. & von Ahsen, O. Detection of KRAS Mutations in Circulating Tumor DNA by Digital PCR in Early Stages of Pancreatic Cancer. Clin Chem 62, 1482–1491 (2016).
Koo, S. J. et al. ATAD2 is an epigenetic reader of newly synthesized histone marks during DNA replication. Oncotarget 7, 70323–70335 (2016).
Zhao, X.-Y., Subramanyam, B., Sarapa, N., Golfier, S. & Dinter, H. Novel Antibody Therapeutics Targeting Mesothelin In Solid Tumors. Clin Cancer Drugs 3, 76–86 (2016).
Boehnke, K. et al. Assay Establishment and Validation of a High-Throughput Screening Platform for Three-Dimensional Patient-Derived Colon Cancer Organoid Cultures. J Biomol Screen 21, 931–941 (2016).
Lexhaller, B., Tompos, C. & Scherf, K. A. Comparative analysis of prolamin and glutelin fractions from wheat, rye, and barley with five sandwich ELISA test kits. Anal Bioanal Chem 408, 6093–6104 (2016).
Schütt, B. et al. Pharmacodynamics and safety of the novel selective progesterone receptor modulator vilaprisan: a double-blind, randomized, placebo-controlled phase 1 trial in healthy women. Human Reproduction (Oxford, England) 31, 1703–1712 (2016).
Gorges, T. M. et al. Heterogeneous PSMA expression on circulating tumor cells: a potential basis for stratification and monitoring of PSMA-directed therapies in prostate cancer. Oncotarget 7, 34930–34941 (2016).
Gorges, T. M. et al. Enumeration and Molecular Characterization of Tumor Cells in Lung Cancer Patients Using a Novel In Vivo Device for Capturing Circulating Tumor Cells. Clin Cancer Res 22, 2197–2206 (2016).
Eggert, E. et al. Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2. Journal of Medicinal Chemistry 59, 4578–4600 (2016).
Wengner, A. M. et al. Novel Mps1 Kinase Inhibitors with Potent Antitumor Activity. Molecular Cancer Therapeutics 15, 583–592 (2016).
Reynoird, N. et al. Coordination of stress signals by the lysine methyltransferase SMYD2 promotes pancreatic cancer. Genes & Development 30, 772–785 (2016).
Kapoor, K. et al. Mechanism of inhibition of human glucose transporter GLUT1 is conserved between cytochalasin B and phenylalanine amides. Proceedings of the National Academy of Sciences of the United States of America 113, 4711–4716 (2016).
Sugawara, T. et al. BAY 1024767 blocks androgen receptor mutants found in castration-resistant prostate cancer patients. Oncotarget 7, 6015–6028 (2016).
Hernando, H. et al. EZH2 Inhibition Blocks Multiple Myeloma Cell Growth through Upregulation of Epithelial Tumor Suppressor Genes. Molecular Cancer Therapeutics 15, 287–298 (2016).
Ferreira de Freitas, R. et al. Discovery of a Potent Class I Protein Arginine Methyltransferase Fragment Inhibitor. Journal of Medicinal Chemistry 59, 1176–1183 (2016).
Baron, A. P. et al. Probing the catalytic functions of Bub1 kinase using the small molecule inhibitors BAY-320 and BAY-524. eLife 5, e12187 (2016).
Nederpelt, I. et al. Characterization of 12 GnRH peptide agonists - a kinetic perspective. British Journal of Pharmacology 173, 128–141 (2016).
Hartung, I. V. et al. Optimization of allosteric MEK inhibitors. Part 2: Taming the sulfamide group balances compound distribution properties. Bioorganic & Medicinal Chemistry Letters 26, 186–193 (2016).
Botzenhardt, S. et al. Safety Profile of Oral Iron Chelator Deferiprone in Chinese Children with Transfusion-Dependent Thalassaemia. Curr Drug Saf 11, 137–144 (2016).
2015
Pihl, S., Andersen, L., Bruzelius, K., Schiebl, C. & Golob, M. An alternative design for long-term stability testing of large molecules: a scientific discussion paper from an EBF Topic Team. Bioanalysis 7, 3073–3083 (2015).
Hartung, I. V. et al. Modular Assembly of Allosteric MEK Inhibitor Structural Elements Unravels Potency and Feedback-Modulation Handles. ChemMedChem 10, 2004–2013 (2015).
Wenzel, C., Otto, S., Prechtl, S., Parczyk, K. & Steigemann, P. A novel 3D high-content assay identifies compounds that prevent fibroblast invasion into tissue surrogates. Experimental Cell Research 339, 35–43 (2015).
Huynh, H., Ong, R. & Zopf, D. Antitumor activity of the multikinase inhibitor regorafenib in patient-derived xenograft models of gastric cancer. J Exp Clin Cancer Res 34, 132 (2015).
von Nussbaum, F. & Li, V. M.-J. Neutrophil elastase inhibitors for the treatment of (cardio)pulmonary diseases: Into clinical testing with pre-adaptive pharmacophores. Bioorganic & Medicinal Chemistry Letters 25, 4370–4381 (2015).
Nakamaru, Y. et al. Investigation of Potential Pharmacokinetic Interactions Between Teneligliptin and Metformin in Steady-state Conditions in Healthy Adults. Clinical Therapeutics 37, 2007–2018 (2015).
von Nussbaum, F. et al. Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 85-8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases. ChemMedChem 10, 1163–1173 (2015).
Marek, I. et al. [Phosphate Intoxication after Application of Enema--a Life-threatening Iatrogenic Complication]. Klin Padiatr 227, 235–238 (2015).
Kelley, M. et al. Workshop Report: AAPS Workshop on Method Development, Validation, and Troubleshooting of Ligand-Binding Assays in the Regulated Environment. AAPS J 17, 1019–1024 (2015).
von Nussbaum, F. & Süssmuth, R. D. Multiple attack on bacteria by the new antibiotic teixobactin. Angewandte Chemie (International Ed. in English) 54, 6684–6686 (2015).
Schulze, J. et al. Cell-based protein stabilization assays for the detection of interactions between small-molecule inhibitors and BRD4. Journal of Biomolecular Screening 20, 180–189 (2015).
Meier, J. C. et al. Knockdown of platinum-induced growth differentiation factor 15 abrogates p27-mediated tumor growth delay in the chemoresistant ovarian cancer model A2780cis. Cancer Medicine 4, 253–267 (2015).
Luense, S. et al. Quantification of histone H3 Lys27 trimethylation (H3K27me3) by high-throughput microscopy enables cellular large-scale screening for small-molecule EZH2 inhibitors. Journal of Biomolecular Screening 20, 190–201 (2015).
Gentili, C. et al. Chromosome Missegregation Associated with RUVBL1 Deficiency. PloS One 10, e0133576 (2015).
Flügel, E. A., Aronson, M. T., Junggeburth, S. C., Chmelka, B. F. & Lotsch, B. V. Surfactant-directed syntheses of mesostructured zinc imidazolates: formation mechanism and structural insights. CrystEngComm 17, 463–470 (2015).
Daudigeos-Dubus, E. et al. Regorafenib: Antitumor Activity upon Mono and Combination Therapy in Preclinical Pediatric Malignancy Models. PLoS One 10, e0142612 (2015).
2014
Timmerman, P. et al. Introduction to the proposals from the global bioanalysis consortium harmonization team. AAPS J 16, 1159–1161 (2014).
von Nussbaum, F. & Schiffer, G. Aspergillomarasmine A, an inhibitor of bacterial metallo-β-lactamases conferring blaNDM and blaVIM resistance. Angewandte Chemie (International Ed. in English) 53, 11696–11698 (2014).
Schmieder, R. et al. Regorafenib (BAY 73-4506): antitumor and antimetastatic activities in preclinical models of colorectal cancer. Int J Cancer 135, 1487–1496 (2014).
Winsemius, A. et al. Pharmacokinetic interaction between simvastatin and fenofibrate with staggered and simultaneous dosing: Does it matter? J Clin Pharmacol 54, 1038–1047 (2014).
Cohen, E. E. W. et al. Phase III randomized trial of induction chemotherapy in patients with N2 or N3 locally advanced head and neck cancer. Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology 32, 2735–2743 (2014).
Jongen, P. J. et al. Fatigue and health-related quality of life in relapsing-remitting multiple sclerosis after 2 years glatiramer acetate treatment are predicted by changes at 6 months: an observational multi-center study. J Neurol 261, 1469–1476 (2014).
Peluffo, M. C. et al. A prostaglandin E2 receptor antagonist prevents pregnancies during a preclinical contraceptive trial with female macaques. Human Reproduction 29, 1400–1412 (2014).
Golfier, S. et al. Anetumab ravtansine: a novel mesothelin-targeting antibody-drug conjugate cures tumors with heterogeneous target expression favored by bystander effect. Molecular Cancer Therapeutics 13, 1537–1548 (2014).
Nakamaru, Y. et al. Effect of ketoconazole on the pharmacokinetics of the dipeptidyl peptidase-4 inhibitor teneligliptin: an open-label study in healthy white subjects in Germany. Clinical Therapeutics 36, 760–769 (2014).
Dudal, S. et al. How the bioanalytical scientist plays a key role in interdisciplinary project teams in the development of biotherapeutics - a reflection of the European Bioanalysis Forum. Bioanalysis 6, 1339–1348 (2014).
Wenzel, C. et al. 3D high-content screening for the identification of compounds that target cells in dormant tumor spheroid regions. Experimental Cell Research 323, 131–143 (2014).
Smeraglia, J. et al. Conference report: AAPS and US FDA Crystal City V meeting on Quantitative Bioanalytical Method Validation and Implementation: feedback from the EBF. Bioanalysis 6, 729–732 (2014).
Jung, M. et al. Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1. The Journal of Biological Chemistry 289, 9304–9319 (2014).
2013
Toni, I., Neubert, A., Botzenhardt, S., Gratzki, N. & Rascher, W. Venous thromboembolism in adolescents associated with drospirenone-containing oral contraceptives - two case reports. Klin Padiatr 225, 266–267 (2013).
de Vries, R. et al. The effect of hematocrit on bioanalysis of DBS: results from the EBF DBS-microsampling consortium. Bioanalysis 5, 2147–2160 (2013).
Cobb, Z. et al. In-depth study of homogeneity in DBS using two different techniques: results from the EBF DBS-microsampling consortium. Bioanalysis 5, 2161–2169 (2013).
Botzenhardt, S., Toni, I., Rascher, W. & Neubert, A. [Venous thromboembolism in adolescents associated with fourth-generation oral contraceptives]. Klin Padiatr 225, 268–276 (2013).
Abou-Elkacem, L. et al. Regorafenib inhibits growth, angiogenesis, and metastasis in a highly aggressive, orthotopic colon cancer model. Mol Cancer Ther 12, 1322–1331 (2013).
Junggeburth, S. C. et al. Ultrathin 2D Coordination Polymer Nanosheets by Surfactant-Mediated Synthesis. J. Am. Chem. Soc. 135, 6157–6164 (2013).
Wiehr, S. et al. Preclinical evaluation of a novel c-Met inhibitor in a gastric cancer xenograft model using small animal PET. Mol Imaging Biol 15, 203–211 (2013).
Hartung, I. V. et al. Optimization of allosteric MEK inhibitors. Part 1: Venturing into underexplored SAR territories. Bioorganic & Medicinal Chemistry Letters 23, 2384–2390 (2013).
van Amsterdam, P. et al. The European Bioanalysis Forum community’s evaluation, interpretation and implementation of the European Medicines Agency guideline on Bioanalytical Method Validation. Bioanalysis 5, 645–659 (2013).
Seithel-Keuth, A. et al. Absolute Bioavailability and Effect of Food on the Disposition of Safinamide Immediate Release Tablets in Healthy Adult Subjects. Clinical Pharmacology in Drug Development 2, 79–89 (2013).
Diefenbach, K. et al. EE-drospirenone-levomefolate calcium versus EE-drospirenone + folic acid: folate status during 24 weeks of treatment and over 20 weeks following treatment cessation. Int J Womens Health 5, 149–163 (2013).
2012
Grismayer, B. et al. Overexpression of the urokinase receptor splice variant uPAR-del4/5 in breast cancer cells affects cell adhesion and invasion in a dose-dependent manner and modulates transcription of tumor-associated genes. Biological Chemistry 393, 1449–1455 (2012).
Friedrich, M. et al. Regression of human prostate cancer xenografts in mice by AMG 212/BAY2010112, a novel PSMA/CD3-Bispecific BiTE antibody cross-reactive with non-human primate antigens. Mol Cancer Ther 11, 2664–2673 (2012).
Brockschnieder, D. et al. Preclinical characterization of a novel class of 18F-labeled PET tracers for amyloid-β. Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine 53, 1794–1801 (2012).
Gorges, T. M. et al. Cancer therapy monitoring in xenografts by quantitative analysis of circulating tumor DNA. Biomarkers 17, 498–506 (2012).
Klotz, M. et al. Preclinical evaluation of biomarkers for response monitoring to the MET inhibitor BAY-853474. Biomarkers 17, 325–335 (2012).
Gorges, T. M. et al. Circulating tumour cells escape from EpCAM-based detection due to epithelial-to-mesenchymal transition. BMC Cancer 12, 178 (2012).
Kirchhoff, D., Kaulfuss, S., Fuhrmann, U., Maurer, M. & Zollner, T. M. Mast cells in endometriosis: guilty or innocent bystanders? Expert Opin Ther Targets 16, 237–241 (2012).
Dijksman, J. et al. ‘Less is More’: defining modern bioanalysis. Bioanalysis 4, 633–642 (2012).
Junggeburth, S. C., Schwinghammer, K., Virdi, K. S., Scheu, C. & Lotsch, B. V. Towards Mesostructured Zinc Imidazolate Frameworks. Chem. Eur. J. 18, 2143–2152 (2012).
Petrul, H. M. et al. Therapeutic mechanism and efficacy of the antibody-drug conjugate BAY 79-4620 targeting human carbonic anhydrase 9. Molecular Cancer Therapeutics 11, 340–349 (2012).
Hagemann, S. et al. Antiproliferative effects of DNA methyltransferase 3B depletion are not associated with DNA demethylation. PloS One 7, e36125 (2012).
2011
White, J. T., Golob, M. & Sailstad, J. Understanding and mitigating impact of immunogenicity on pharmacokinetic assays. Bioanalysis 3, 1799–1803 (2011).
Wilhelm, S. M. et al. Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int J Cancer 129, 245–255 (2011).
Sato, S. et al. Overexpression of the urokinase receptor mRNA splice variant uPAR-del4/5 affects tumor-associated processes of breast cancer cells in vitro and in vivo. Breast Cancer Research and Treatment 127, 649–657 (2011).
Abbott, R. W. et al. From challenges to solutions. European Bioanalysis Forum 3rd Annual Open Symposium, Hesperia Towers, Barcelona, Spain, 1-3 December 2010. Bioanalysis 3, 833–838 (2011).
Schulz, M. N. et al. A crystallographic fragment screen identifies cinnamic acid derivatives as starting points for potent Pim-1 inhibitors. Acta Crystallographica. Section D, Biological Crystallography 67, 156–166 (2011).
von Bonin, A. et al. Inhibition of the IL-2-inducible tyrosine kinase (Itk) activity: a new concept for the therapy of inflammatory skin diseases. Exp Dermatol 20, 41–47 (2011).
Lissy, M., Ode, M. & Roth, K. Comparison of the pharmacokinetic and pharmacodynamic profiles of one US-marketed and two European-marketed epoetin alfas: a randomized prospective study. Drugs in R&D 11, 61–75 (2011).
