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Paradoxical Increase of Permeability and Lipophilicity with the Increasing Topological Polar Surface Area within a Series of PRMT5 Inhibitors.
Argikar U, Blatter M, Bednarczyk D, Chen Z, Cho YS, Doré M, Dumouchel JL, Ho S, Hoegenauer K, Kawanami T, Mathieu S, Meredith E, Möbitz H, Murphy SK, Parthasarathy S, Soldermann CP, Santos J, Silver S, Skolnik S, Stojanovic A. Argikar U, et al. Among authors: kawanami t. J Med Chem. 2022 Sep 22;65(18):12386-12402. doi: 10.1021/acs.jmedchem.2c01068. Epub 2022 Sep 7. J Med Chem. 2022. PMID: 36069672
Structure based design of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors from a phenotypic screen.
Palacios DS, Meredith E, Kawanami T, Adams C, Chen X, Darsigny V, Geno E, Palermo M, Baird D, Boynton G, Busby SA, George EL, Guy C, Hewett J, Tierney L, Thigale S, Weihofen W, Wang L, White N, Yin M, Argikar UA. Palacios DS, et al. Among authors: kawanami t. Bioorg Med Chem Lett. 2018 Feb 1;28(3):365-370. doi: 10.1016/j.bmcl.2017.12.037. Epub 2017 Dec 18. Bioorg Med Chem Lett. 2018. PMID: 29275937
Optimization of Allosteric With-No-Lysine (WNK) Kinase Inhibitors and Efficacy in Rodent Hypertension Models.
Yamada K, Levell J, Yoon T, Kohls D, Yowe D, Rigel DF, Imase H, Yuan J, Yasoshima K, DiPetrillo K, Monovich L, Xu L, Zhu M, Kato M, Jain M, Idamakanti N, Taslimi P, Kawanami T, Argikar UA, Kunjathoor V, Xie X, Yagi YI, Iwaki Y, Robinson Z, Park HM. Yamada K, et al. Among authors: kawanami t. J Med Chem. 2017 Aug 24;60(16):7099-7107. doi: 10.1021/acs.jmedchem.7b00708. Epub 2017 Aug 3. J Med Chem. 2017. PMID: 28771350
Scaffold Morphing Identifies 3-Pyridyl Azetidine Ureas as Inhibitors of Nicotinamide Phosphoribosyltransferase (NAMPT).
Palacios DS, Meredith EL, Kawanami T, Adams CM, Chen X, Darsigny V, Palermo M, Baird D, George EL, Guy C, Hewett J, Tierney L, Thigale S, Wang L, Weihofen WA. Palacios DS, et al. Among authors: kawanami t. ACS Med Chem Lett. 2019 Oct 10;10(11):1524-1529. doi: 10.1021/acsmedchemlett.9b00325. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 31749905 Free PMC article.
Discovery of 4-((2S,4S)-4-Ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases.
Mainolfi N, Ehara T, Karki RG, Anderson K, Mac Sweeney A, Liao SM, Argikar UA, Jendza K, Zhang C, Powers J, Klosowski DW, Crowley M, Kawanami T, Ding J, April M, Forster C, Serrano-Wu M, Capparelli M, Ramqaj R, Solovay C, Cumin F, Smith TM, Ferrara L, Lee W, Long D, Prentiss M, De Erkenez A, Yang L, Liu F, Sellner H, Sirockin F, Valeur E, Erbel P, Ostermeier D, Ramage P, Gerhartz B, Schubart A, Flohr S, Gradoux N, Feifel R, Vogg B, Wiesmann C, Maibaum J, Eder J, Sedrani R, Harrison RA, Mogi M, Jaffee BD, Adams CM. Mainolfi N, et al. Among authors: kawanami t. J Med Chem. 2020 Jun 11;63(11):5697-5722. doi: 10.1021/acs.jmedchem.9b01870. Epub 2020 Feb 19. J Med Chem. 2020. PMID: 32073845
Discovery of a Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma.
Yamada K, Brousseau M, Honma W, Iimura A, Imase H, Iwaki Y, Kawanami T, LaSala D, Liang G, Mitani H, Nonomura K, Ohmori O, Pan M, Rigel DF, Umemura I, Yasoshima K, Zhu G, Mogi M. Yamada K, et al. Among authors: kawanami t. J Med Chem. 2017 Oct 26;60(20):8466-8481. doi: 10.1021/acs.jmedchem.7b00900. Epub 2017 Oct 16. J Med Chem. 2017. PMID: 29035537
Structure-Guided Design of Substituted Biphenyl Butanoic Acid Derivatives as Neprilysin Inhibitors.
Kawanami T, Karki RG, Cody E, Liu Q, Liang G, Ksander GM, Rigel DF, Schiering N, Gong Y, Coppola GM, Iwaki Y, Sun R, Neubert A, Fan L, Ingles S, D'Arcy A, Villard F, Ramage P, Jeng AY, Leung-Chu J, Liu J, Beil M, Fu F, Chen W, Cumin F, Wiesmann C, Mogi M. Kawanami T, et al. ACS Med Chem Lett. 2020 Jan 27;11(2):188-194. doi: 10.1021/acsmedchemlett.9b00578. eCollection 2020 Feb 13. ACS Med Chem Lett. 2020. PMID: 32071687 Free PMC article.
Discovery and Characterization of Allosteric WNK Kinase Inhibitors.
Yamada K, Zhang JH, Xie X, Reinhardt J, Xie AQ, LaSala D, Kohls D, Yowe D, Burdick D, Yoshisue H, Wakai H, Schmidt I, Gunawan J, Yasoshima K, Yue QK, Kato M, Mogi M, Idamakanti N, Kreder N, Drueckes P, Pandey P, Kawanami T, Huang W, Yagi YI, Deng Z, Park HM. Yamada K, et al. Among authors: kawanami t. ACS Chem Biol. 2016 Dec 16;11(12):3338-3346. doi: 10.1021/acschembio.6b00511. Epub 2016 Oct 19. ACS Chem Biol. 2016. PMID: 27712055
380 results