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Discovery of 1-[2-(1-methyl-1H-pyrazol-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-6-yl]-3-(pyridin-4-ylmethyl)urea as a potent NAMPT (nicotinamide phosphoribosyltransferase) activator with attenuated CYP inhibition.
Akiu M, Tsuji T, Sogawa Y, Terayama K, Yokoyama M, Tanaka J, Asano D, Sakurai K, Sergienko E, Sessions EH, Gardell SJ, Pinkerton AB, Nakamura T. Akiu M, et al. Among authors: tanaka j. Bioorg Med Chem Lett. 2021 Jul 1;43:128048. doi: 10.1016/j.bmcl.2021.128048. Epub 2021 Apr 19. Bioorg Med Chem Lett. 2021. PMID: 33887438
Optimization of a urea-containing series of nicotinamide phosphoribosyltransferase (NAMPT) activators.
Pinkerton AB, Sessions EH, Hershberger P, Maloney PR, Peddibhotla S, Hopf M, Sergienko E, Ma CT, Smith LH, Jackson MR, Tanaka J, Tsuji T, Akiu M, Cohen SE, Nakamura T, Gardell SJ. Pinkerton AB, et al. Among authors: tanaka j. Bioorg Med Chem Lett. 2021 Jun 1;41:128007. doi: 10.1016/j.bmcl.2021.128007. Epub 2021 Mar 31. Bioorg Med Chem Lett. 2021. PMID: 33798699
Boosting NAD+ with a small molecule that activates NAMPT.
Gardell SJ, Hopf M, Khan A, Dispagna M, Hampton Sessions E, Falter R, Kapoor N, Brooks J, Culver J, Petucci C, Ma CT, Cohen SE, Tanaka J, Burgos ES, Hirschi JS, Smith SR, Sergienko E, Pinkerton AB. Gardell SJ, et al. Among authors: tanaka j. Nat Commun. 2019 Jul 19;10(1):3241. doi: 10.1038/s41467-019-11078-z. Nat Commun. 2019. PMID: 31324777 Free PMC article.
Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
Shinozuka T, Tsukada T, Fujii K, Tokumaru E, Shimada K, Onishi Y, Matsui Y, Wakimoto S, Kuroha M, Ogata T, Araki K, Ohsumi J, Sawamura R, Watanabe N, Yamamoto H, Fujimoto K, Tani Y, Mori M, Tanaka J. Shinozuka T, et al. Among authors: tanaka j. Bioorg Med Chem. 2018 Oct 1;26(18):5079-5098. doi: 10.1016/j.bmc.2018.09.006. Epub 2018 Sep 8. Bioorg Med Chem. 2018. PMID: 30241907
Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
Shinozuka T, Tsukada T, Fujii K, Tokumaru E, Shimada K, Onishi Y, Matsui Y, Wakimoto S, Kuroha M, Ogata T, Araki K, Ohsumi J, Sawamura R, Watanabe N, Yamamoto H, Fujimoto K, Tani Y, Mori M, Tanaka J. Shinozuka T, et al. Among authors: tanaka j. Bioorg Med Chem. 2018 Oct 1;26(18):5099-5117. doi: 10.1016/j.bmc.2018.09.005. Epub 2018 Sep 8. Bioorg Med Chem. 2018. PMID: 30220602
Discovery of potent and orally active tricyclic-based FBPase inhibitors.
Tsukada T, Kanno O, Yamane T, Tanaka J, Yoshida T, Okuno A, Shiiki T, Takahashi M, Nishi T. Tsukada T, et al. Among authors: tanaka j. Bioorg Med Chem. 2010 Jul 15;18(14):5346-51. doi: 10.1016/j.bmc.2010.05.041. Epub 2010 May 20. Bioorg Med Chem. 2010. PMID: 20542703
3,210 results