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Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
Lee KL, Ambler CM, Anderson DR, Boscoe BP, Bree AG, Brodfuehrer JI, Chang JS, Choi C, Chung S, Curran KJ, Day JE, Dehnhardt CM, Dower K, Drozda SE, Frisbie RK, Gavrin LK, Goldberg JA, Han S, Hegen M, Hepworth D, Hope HR, Kamtekar S, Kilty IC, Lee A, Lin LL, Lovering FE, Lowe MD, Mathias JP, Morgan HM, Murphy EA, Papaioannou N, Patny A, Pierce BS, Rao VR, Saiah E, Samardjiev IJ, Samas BM, Shen MWH, Shin JH, Soutter HH, Strohbach JW, Symanowicz PT, Thomason JR, Trzupek JD, Vargas R, Vincent F, Yan J, Zapf CW, Wright SW. Lee KL, et al. Among authors: frisbie rk. J Med Chem. 2017 Jul 13;60(13):5521-5542. doi: 10.1021/acs.jmedchem.7b00231. Epub 2017 Jun 14. J Med Chem. 2017. PMID: 28498658
Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists.
Humphries PS, Benbow JW, Bonin PD, Boyer D, Doran SD, Frisbie RK, Piotrowski DW, Balan G, Bechle BM, Conn EL, Dirico KJ, Oliver RM, Soeller WC, Southers JA, Yang X. Humphries PS, et al. Among authors: frisbie rk. Bioorg Med Chem Lett. 2009 May 1;19(9):2400-3. doi: 10.1016/j.bmcl.2009.03.082. Epub 2009 Mar 25. Bioorg Med Chem Lett. 2009. PMID: 19346127
Identification and optimization of indolo[2,3-c]quinoline inhibitors of IRAK4.
Tumey LN, Boschelli DH, Bhagirath N, Shim J, Murphy EA, Goodwin D, Bennett EM, Wang M, Lin LL, Press B, Shen M, Frisbie RK, Morgan P, Mohan S, Shin J, Rao VR. Tumey LN, et al. Among authors: frisbie rk. Bioorg Med Chem Lett. 2014 May 1;24(9):2066-72. doi: 10.1016/j.bmcl.2014.03.056. Epub 2014 Mar 29. Bioorg Med Chem Lett. 2014. PMID: 24726805
Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy.
Cameron KO, Kung DW, Kalgutkar AS, Kurumbail RG, Miller R, Salatto CT, Ward J, Withka JM, Bhattacharya SK, Boehm M, Borzilleri KA, Brown JA, Calabrese M, Caspers NL, Cokorinos E, Conn EL, Dowling MS, Edmonds DJ, Eng H, Fernando DP, Frisbie R, Hepworth D, Landro J, Mao Y, Rajamohan F, Reyes AR, Rose CR, Ryder T, Shavnya A, Smith AC, Tu M, Wolford AC, Xiao J. Cameron KO, et al. J Med Chem. 2016 Sep 8;59(17):8068-81. doi: 10.1021/acs.jmedchem.6b00866. Epub 2016 Aug 20. J Med Chem. 2016. PMID: 27490827
Rational approach to highly potent and selective apoptosis signal-regulating kinase 1 (ASK1) inhibitors.
Lovering F, Morgan P, Allais C, Aulabaugh A, Brodfuehrer J, Chang J, Coe J, Ding W, Dowty H, Fleming M, Frisbie R, Guzova J, Hepworth D, Jasti J, Kortum S, Kurumbail R, Mohan S, Papaioannou N, Strohbach JW, Vincent F, Lee K, Zapf CW. Lovering F, et al. Eur J Med Chem. 2018 Feb 10;145:606-621. doi: 10.1016/j.ejmech.2017.12.041. Epub 2017 Dec 15. Eur J Med Chem. 2018. PMID: 29348070
Discovery of a Series of Pyrimidine Carboxamides as Inhibitors of Vanin-1.
Casimiro-Garcia A, Allais C, Brennan A, Choi C, Dower G, Farley KA, Fleming M, Flick A, Frisbie RK, Hall J, Hepworth D, Jones H, Knafels JD, Kortum S, Lovering FE, Mathias JP, Mohan S, Morgan PM, Parng C, Parris K, Pullen N, Schlerman F, Stansfield J, Strohbach JW, Vajdos FF, Vincent F, Wang H, Wang X, Webster R, Wright SW. Casimiro-Garcia A, et al. Among authors: frisbie rk. J Med Chem. 2022 Jan 13;65(1):757-784. doi: 10.1021/acs.jmedchem.1c01849. Epub 2021 Dec 30. J Med Chem. 2022. PMID: 34967602
A Novel C-C Chemoattractant Cytokine (Chemokine) Receptor 6 (CCR6) Antagonist (PF-07054894) Distinguishes between Homologous Chemokine Receptors, Increases Basal Circulating CCR6+ T Cells, and Ameliorates Interleukin-23-Induced Skin Inflammation.
Li W, Crouse KK, Alley J, Frisbie RK, Fish SC, Andreyeva TA, Reed LA, Thorn M, DiMaggio G, Donovan CB, Bennett D, Garren J, Oziolor E, Qian J, Newman L, Vargas AP, Kumpf SW, Steyn SJ, Schnute ME, Thorarensen A, Hegen M, Stevens E, Collinge M, Lanz TA, Vincent F, Vincent MS, Berstein G. Li W, et al. Among authors: frisbie rk. J Pharmacol Exp Ther. 2023 Jul;386(1):80-92. doi: 10.1124/jpet.122.001452. Epub 2023 May 4. J Pharmacol Exp Ther. 2023. PMID: 37142443
Structural basis for AMPK activation: natural and synthetic ligands regulate kinase activity from opposite poles by different molecular mechanisms.
Calabrese MF, Rajamohan F, Harris MS, Caspers NL, Magyar R, Withka JM, Wang H, Borzilleri KA, Sahasrabudhe PV, Hoth LR, Geoghegan KF, Han S, Brown J, Subashi TA, Reyes AR, Frisbie RK, Ward J, Miller RA, Landro JA, Londregan AT, Carpino PA, Cabral S, Smith AC, Conn EL, Cameron KO, Qiu X, Kurumbail RG. Calabrese MF, et al. Among authors: frisbie rk. Structure. 2014 Aug 5;22(8):1161-1172. doi: 10.1016/j.str.2014.06.009. Epub 2014 Jul 24. Structure. 2014. PMID: 25066137 Free article.
Escherichia coli expression, purification and characterization of functional full-length recombinant alpha2beta2gamma3 heterotrimeric complex of human AMP-activated protein kinase.
Rajamohan F, Harris MS, Frisbie RK, Hoth LR, Geoghegan KF, Valentine JJ, Reyes AR, Landro JA, Qiu X, Kurumbail RG. Rajamohan F, et al. Among authors: frisbie rk. Protein Expr Purif. 2010 Oct;73(2):189-97. doi: 10.1016/j.pep.2010.04.022. Epub 2010 May 6. Protein Expr Purif. 2010. PMID: 20451617
Probing the enzyme kinetics, allosteric modulation and activation of α1- and α2-subunit-containing AMP-activated protein kinase (AMPK) heterotrimeric complexes by pharmacological and physiological activators.
Rajamohan F, Reyes AR, Frisbie RK, Hoth LR, Sahasrabudhe P, Magyar R, Landro JA, Withka JM, Caspers NL, Calabrese MF, Ward J, Kurumbail RG. Rajamohan F, et al. Among authors: frisbie rk. Biochem J. 2016 Mar 1;473(5):581-92. doi: 10.1042/BJ20151051. Epub 2015 Dec 3. Biochem J. 2016. PMID: 26635351 Free PMC article.