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Small molecule branched-chain ketoacid dehydrogenase kinase (BDK) inhibitors with opposing effects on BDK protein levels.
Roth Flach RJ, Bollinger E, Reyes AR, Laforest B, Kormos BL, Liu S, Reese MR, Martinez Alsina LA, Buzon L, Zhang Y, Bechle B, Rosado A, Sahasrabudhe PV, Knafels J, Bhattacharya SK, Omoto K, Stansfield JC, Hurley LD, Song L, Luo L, Breitkopf SB, Monetti M, Cunio T, Tierney B, Geoly FJ, Delmore J, Siddall CP, Xue L, Yip KN, Kalgutkar AS, Miller RA, Zhang BB, Filipski KJ. Roth Flach RJ, et al. Among authors: knafels j. Nat Commun. 2023 Aug 9;14(1):4812. doi: 10.1038/s41467-023-40536-y. Nat Commun. 2023. PMID: 37558654 Free PMC article.
Structure based design of an in vivo active hydroxamic acid inhibitor of P. aeruginosa LpxC.
Warmus JS, Quinn CL, Taylor C, Murphy ST, Johnson TA, Limberakis C, Ortwine D, Bronstein J, Pagano P, Knafels JD, Lightle S, Mochalkin I, Brideau R, Podoll T. Warmus JS, et al. Among authors: knafels jd. Bioorg Med Chem Lett. 2012 Apr 1;22(7):2536-43. doi: 10.1016/j.bmcl.2012.01.140. Epub 2012 Feb 16. Bioorg Med Chem Lett. 2012. PMID: 22401863
Complete sequence of the bithorax complex of Drosophila.
Martin CH, Mayeda CA, Davis CA, Ericsson CL, Knafels JD, Mathog DR, Celniker SE, Lewis EB, Palazzolo MJ. Martin CH, et al. Among authors: knafels jd. Proc Natl Acad Sci U S A. 1995 Aug 29;92(18):8398-402. doi: 10.1073/pnas.92.18.8398. Proc Natl Acad Sci U S A. 1995. PMID: 7667301 Free PMC article.
Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus.
Pfefferkorn JA, Guzman-Perez A, Litchfield J, Aiello R, Treadway JL, Pettersen J, Minich ML, Filipski KJ, Jones CS, Tu M, Aspnes G, Risley H, Bian J, Stevens BD, Bourassa P, D'Aquila T, Baker L, Barucci N, Robertson AS, Bourbonais F, Derksen DR, Macdougall M, Cabrera O, Chen J, Lapworth AL, Landro JA, Zavadoski WJ, Atkinson K, Haddish-Berhane N, Tan B, Yao L, Kosa RE, Varma MV, Feng B, Duignan DB, El-Kattan A, Murdande S, Liu S, Ammirati M, Knafels J, Dasilva-Jardine P, Sweet L, Liras S, Rolph TP. Pfefferkorn JA, et al. Among authors: knafels j. J Med Chem. 2012 Feb 9;55(3):1318-33. doi: 10.1021/jm2014887. Epub 2012 Jan 24. J Med Chem. 2012. PMID: 22196621
Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif.
Filipski KJ, Guzman-Perez A, Bian J, Perreault C, Aspnes GE, Didiuk MT, Dow RL, Hank RF, Jones CS, Maguire RJ, Tu M, Zeng D, Liu S, Knafels JD, Litchfield J, Atkinson K, Derksen DR, Bourbonais F, Gajiwala KS, Hickey M, Johnson TO, Humphries PS, Pfefferkorn JA. Filipski KJ, et al. Among authors: knafels jd. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4571-8. doi: 10.1016/j.bmcl.2013.06.036. Epub 2013 Jun 20. Bioorg Med Chem Lett. 2013. PMID: 23831135
Casein kinase 1δ/ε inhibitor PF-5006739 attenuates opioid drug-seeking behavior.
Wager TT, Chandrasekaran RY, Bradley J, Rubitski D, Berke H, Mente S, Butler T, Doran A, Chang C, Fisher K, Knafels J, Liu S, Ohren J, Marconi M, DeMarco G, Sneed B, Walton K, Horton D, Rosado A, Mead A. Wager TT, et al. Among authors: knafels j. ACS Chem Neurosci. 2014 Dec 17;5(12):1253-65. doi: 10.1021/cn500201x. Epub 2014 Oct 28. ACS Chem Neurosci. 2014. PMID: 25299732 Clinical Trial.
Structural studies identify angiotensin II receptor blocker-like compounds as branched-chain ketoacid dehydrogenase kinase inhibitors.
Liu S, Kormos BL, Knafels JD, Sahasrabudhe PV, Rosado A, Sommese RF, Reyes AR, Ward J, Roth Flach RJ, Wang X, Buzon LM, Reese MR, Bhattacharya SK, Omoto K, Filipski KJ. Liu S, et al. Among authors: knafels jd. J Biol Chem. 2023 Mar;299(3):102959. doi: 10.1016/j.jbc.2023.102959. Epub 2023 Jan 28. J Biol Chem. 2023. PMID: 36717078 Free PMC article.
Ligand-protein interactions of selective casein kinase 1δ inhibitors.
Mente S, Arnold E, Butler T, Chakrapani S, Chandrasekaran R, Cherry K, DiRico K, Doran A, Fisher K, Galatsis P, Green M, Hayward M, Humphrey J, Knafels J, Li J, Liu S, Marconi M, McDonald S, Ohren J, Paradis V, Sneed B, Walton K, Wager T. Mente S, et al. Among authors: knafels j. J Med Chem. 2013 Sep 12;56(17):6819-28. doi: 10.1021/jm4006324. Epub 2013 Aug 28. J Med Chem. 2013. PMID: 23919824
31 results