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Screening through Lead Optimization of High Affinity, Allosteric Cyclin-Dependent Kinase 2 (CDK2) Inhibitors as Male Contraceptives That Reduce Sperm Counts in Mice.
Faber EB, Wang N, John K, Sun L, Wong HL, Burban D, Francis R, Tian D, Hong KH, Yang A, Wang L, Elsaid M, Khalid H, Levinson NM, Schönbrunn E, Hawkinson JE, Georg GI. Faber EB, et al. Among authors: john k. J Med Chem. 2023 Feb 9;66(3):1928-1940. doi: 10.1021/acs.jmedchem.2c01731. Epub 2023 Jan 26. J Med Chem. 2023. PMID: 36701569 Free PMC article.
Discovery of a Pan-Melanocortin Receptor Antagonist [Ac-DPhe(pI)-Arg-Nal(2')-Orn-NH2] at the MC1R, MC3R, MC4R, and MC5R that Mediates an Increased Feeding Response in Mice and a 40-Fold Selective MC1R Antagonist [Ac-DPhe(pI)-DArg-Nal(2')-Arg-NH2].
Ericson MD, Tran LT, Mathre SS, Freeman KT, Holdaway K, John K, Lunzer MM, Bouchard JL, Haskell-Luevano C. Ericson MD, et al. Among authors: john k. J Med Chem. 2023 Jun 22;66(12):8103-8117. doi: 10.1021/acs.jmedchem.3c00432. Epub 2023 Jun 12. J Med Chem. 2023. PMID: 37307241 Free PMC article.
Development of allosteric and selective CDK2 inhibitors for contraception with negative cooperativity to cyclin binding.
Faber EB, Sun L, Tang J, Roberts E, Ganeshkumar S, Wang N, Rasmussen D, Majumdar A, Hirsch LE, John K, Yang A, Khalid H, Hawkinson JE, Levinson NM, Chennathukuzhi V, Harki DA, Schönbrunn E, Georg GI. Faber EB, et al. Among authors: john k. Nat Commun. 2023 Jun 3;14(1):3213. doi: 10.1038/s41467-023-38732-x. Nat Commun. 2023. PMID: 37270540 Free PMC article.
661 results