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Bis-Heteroaryl Pyrazoles: Identification of Orally Bioavailable Inhibitors of Activin Receptor-Like Kinase-2 (R206H).
Sekimata K, Sato T, Sakai N, Watanabe H, Mishima-Tsumagari C, Taguri T, Matsumoto T, Fujii Y, Handa N, Honma T, Tanaka A, Shirouzu M, Yokoyama S, Miyazono K, Hashizume Y, Koyama H. Sekimata K, et al. Among authors: koyama h. Chem Pharm Bull (Tokyo). 2019;67(3):224-235. doi: 10.1248/cpb.c18-00598. Chem Pharm Bull (Tokyo). 2019. PMID: 30828000 Free article.
Discovery of Novel Spiroindoline Derivatives as Selective Tankyrase Inhibitors.
Shirai F, Tsumura T, Yashiroda Y, Yuki H, Niwa H, Sato S, Chikada T, Koda Y, Washizuka K, Yoshimoto N, Abe M, Onuki T, Mazaki Y, Hirama C, Fukami T, Watanabe H, Honma T, Umehara T, Shirouzu M, Okue M, Kano Y, Watanabe T, Kitamura K, Shitara E, Muramatsu Y, Yoshida H, Mizutani A, Seimiya H, Yoshida M, Koyama H. Shirai F, et al. Among authors: koyama h. J Med Chem. 2019 Apr 11;62(7):3407-3427. doi: 10.1021/acs.jmedchem.8b01888. Epub 2019 Apr 1. J Med Chem. 2019. PMID: 30883102
Identification of small molecule inhibitors of human COQ7.
Tsuganezawa K, Sekimata K, Nakagawa Y, Utata R, Nakamura K, Ogawa N, Koyama H, Shirouzu M, Fukami T, Kita K, Tanaka A. Tsuganezawa K, et al. Among authors: koyama h. Bioorg Med Chem. 2020 Jan 1;28(1):115182. doi: 10.1016/j.bmc.2019.115182. Epub 2019 Nov 9. Bioorg Med Chem. 2020. PMID: 31753803
Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer.
Shirai F, Mizutani A, Yashiroda Y, Tsumura T, Kano Y, Muramatsu Y, Chikada T, Yuki H, Niwa H, Sato S, Washizuka K, Koda Y, Mazaki Y, Jang MK, Yoshida H, Nagamori A, Okue M, Watanabe T, Kitamura K, Shitara E, Honma T, Umehara T, Shirouzu M, Fukami T, Seimiya H, Yoshida M, Koyama H. Shirai F, et al. Among authors: koyama h. J Med Chem. 2020 Apr 23;63(8):4183-4204. doi: 10.1021/acs.jmedchem.0c00045. Epub 2020 Apr 1. J Med Chem. 2020. PMID: 32202790
Structural Basis of Activin Receptor-Like Kinase 2 (R206H) Inhibition by Bis-heteroaryl Pyrazole-Based Inhibitors for the Treatment of Fibrodysplasia Ossificans Progressiva Identified by the Integration of Ligand-Based and Structure-Based Drug Design Approaches.
Sato T, Sekimata K, Sakai N, Watanabe H, Mishima-Tsumagari C, Taguri T, Matsumoto T, Fujii Y, Handa N, Tanaka A, Shirouzu M, Yokoyama S, Hashizume Y, Miyazono K, Koyama H, Honma T. Sato T, et al. Among authors: koyama h. ACS Omega. 2020 May 12;5(20):11411-11423. doi: 10.1021/acsomega.9b04245. eCollection 2020 May 26. ACS Omega. 2020. PMID: 32478230 Free PMC article.
The ubiquinone synthesis pathway is a promising drug target for Chagas disease.
Nara T, Nakagawa Y, Tsuganezawa K, Yuki H, Sekimata K, Koyama H, Ogawa N, Honma T, Shirouzu M, Fukami T, Matsuo Y, Inaoka DK, Kita K, Tanaka A. Nara T, et al. Among authors: koyama h. PLoS One. 2021 Feb 4;16(2):e0243855. doi: 10.1371/journal.pone.0243855. eCollection 2021. PLoS One. 2021. PMID: 33539347 Free PMC article.
Novel bicyclic pyrazoles as potent ALK2 (R206H) inhibitors for the treatment of fibrodysplasia ossificans progressiva.
Yamamoto H, Sakai N, Ohte S, Sato T, Sekimata K, Matsumoto T, Nakamura K, Watanabe H, Mishima-Tsumagari C, Tanaka A, Hashizume Y, Honma T, Katagiri T, Miyazono K, Tomoda H, Shirouzu M, Koyama H. Yamamoto H, et al. Among authors: koyama h. Bioorg Med Chem Lett. 2021 Apr 15;38:127858. doi: 10.1016/j.bmcl.2021.127858. Epub 2021 Feb 18. Bioorg Med Chem Lett. 2021. PMID: 33609658
1,822 results