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133 results

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Discovery of EP300/CBP histone acetyltransferase inhibitors through scaffold hopping of 1,4-oxazepane ring.
Kanada R, Kagoshima Y, Asano M, Suzuki T, Murata T, Haruta M, Takahashi M, Ubukata O, Hashimoto K, Obata K, Kihara K, Kuroha M, Banjo T, Togashi N, Sato K, Yamamoto Y, Suzuki K, Isoyama T, Tominaga Y, Higuchi S, Naito H. Kanada R, et al. Among authors: isoyama t. Bioorg Med Chem Lett. 2022 Jun 15;66:128726. doi: 10.1016/j.bmcl.2022.128726. Epub 2022 Apr 9. Bioorg Med Chem Lett. 2022. PMID: 35413416
Discovery of DS-9300: A Highly Potent, Selective, and Once-Daily Oral EP300/CBP Histone Acetyltransferase Inhibitor.
Kanada R, Kagoshima Y, Suzuki T, Nakamura A, Funami H, Watanabe J, Asano M, Takahashi M, Ubukata O, Suzuki K, Aikawa T, Sato K, Goto M, Setsu G, Ito K, Kihara K, Kuroha M, Kohno T, Ogiwara H, Isoyama T, Tominaga Y, Higuchi S, Naito H. Kanada R, et al. Among authors: isoyama t. J Med Chem. 2023 Jan 12;66(1):695-715. doi: 10.1021/acs.jmedchem.2c01641. Epub 2022 Dec 26. J Med Chem. 2023. PMID: 36572866
A novel inhibitor stabilizes the inactive conformation of MAPK-interacting kinase 1.
Matsui Y, Yasumatsu I, Yoshida KI, Iimura S, Ikeno Y, Nawano T, Fukano H, Ubukata O, Hanzawa H, Tanzawa F, Isoyama T. Matsui Y, et al. Among authors: isoyama t. Acta Crystallogr F Struct Biol Commun. 2018 Mar 1;74(Pt 3):156-160. doi: 10.1107/S2053230X18002108. Epub 2018 Feb 26. Acta Crystallogr F Struct Biol Commun. 2018. PMID: 29497019 Free PMC article.
The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models.
Katayama R, Gong B, Togashi N, Miyamoto M, Kiga M, Iwasaki S, Kamai Y, Tominaga Y, Takeda Y, Kagoshima Y, Shimizu Y, Seto Y, Oh-Hara T, Koike S, Nakao N, Hanzawa H, Watanabe K, Yoda S, Yanagitani N, Hata AN, Shaw AT, Nishio M, Fujita N, Isoyama T. Katayama R, et al. Among authors: isoyama t. Nat Commun. 2019 Aug 9;10(1):3604. doi: 10.1038/s41467-019-11496-z. Nat Commun. 2019. PMID: 31399568 Free PMC article.
DS-1205b, a novel selective inhibitor of AXL kinase, blocks resistance to EGFR-tyrosine kinase inhibitors in a non-small cell lung cancer xenograft model.
Jimbo T, Hatanaka M, Komatsu T, Taira T, Kumazawa K, Maeda N, Suzuki T, Ota M, Haginoya N, Isoyama T, Fujiwara K. Jimbo T, et al. Among authors: isoyama t. Oncotarget. 2019 Aug 27;10(50):5152-5167. doi: 10.18632/oncotarget.27114. eCollection 2019 Aug 27. Oncotarget. 2019. PMID: 31497246 Free PMC article.
U.S. Phase I First-in-human Study of Taletrectinib (DS-6051b/AB-106), a ROS1/TRK Inhibitor, in Patients with Advanced Solid Tumors.
Papadopoulos KP, Borazanci E, Shaw AT, Katayama R, Shimizu Y, Zhu VW, Sun TY, Wakelee HA, Madison R, Schrock AB, Senaldi G, Nakao N, Hanzawa H, Tachibana M, Isoyama T, Nakamaru K, Deng C, Li M, Fan F, Zhao Q, Gao Y, Seto T, Jänne PA, Ou SI. Papadopoulos KP, et al. Among authors: isoyama t. Clin Cancer Res. 2020 Sep 15;26(18):4785-4794. doi: 10.1158/1078-0432.CCR-20-1630. Epub 2020 Jun 26. Clin Cancer Res. 2020. PMID: 32591465 Clinical Trial.
133 results