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Page 1
Discovery of TRPA1 Antagonist GDC-6599: Derisking Preclinical Toxicity and Aldehyde Oxidase Metabolism with a Potential First-in-Class Therapy for Respiratory Disease.
Terrett JA, Ly JQ, Katavolos P, Hasselgren C, Laing S, Zhong F, Villemure E, Déry M, Larouche-Gauthier R, Chen H, Shore DG, Lee WP, Suto E, Johnson K, Brooks M, Stablein A, Beaumier F, Constantineau-Forget L, Grand-Maître C, Lépissier L, Ciblat S, Sturino C, Chen Y, Hu B, Elstrott J, Gandham V, Joseph V, Booler H, Cain G, Chou C, Fullerton A, Lepherd M, Stainton S, Torres E, Urban K, Yu L, Zhong Y, Bao L, Chou KJ, Lin J, Zhang W, La H, Liu L, Mulder T, Chen J, Chernov-Rogan T, Johnson AR, Hackos DH, Leahey R, Shields SD, Balestrini A, Riol-Blanco L, Safina BS, Volgraf M, Magnuson S, Kakiuchi-Kiyota S. Terrett JA, et al. Among authors: kakiuchi kiyota s. J Med Chem. 2024 Mar 14;67(5):3287-3306. doi: 10.1021/acs.jmedchem.3c02121. Epub 2024 Mar 3. J Med Chem. 2024. PMID: 38431835
Optimization of a Novel DEL Hit That Binds in the Cbl-b SH2 Domain and Blocks Substrate Binding.
Liang J, Lambrecht MJ, Arenzana TL, Aubert-Nicol S, Bao L, Broccatelli F, Cai J, Eidenschenk C, Everett C, Garner T, Gruber F, Haghshenas P, Huestis MP, Hsu PL, Kou P, Jakalian A, Larouche-Gauthier R, Leclerc JP, Leung DH, Martin A, Murray J, Prangley M, Rutz S, Kakiuchi-Kiyota S, Satz AL, Skelton NJ, Steffek M, Stoffler D, Sudhamsu J, Tan S, Wang J, Wang S, Wang Q, Wendorff TJ, Wichert M, Yadav A, Yu C, Wang X. Liang J, et al. Among authors: kakiuchi kiyota s. ACS Med Chem Lett. 2024 May 29;15(6):864-872. doi: 10.1021/acsmedchemlett.4c00068. eCollection 2024 Jun 13. ACS Med Chem Lett. 2024. PMID: 38894924
Discovery of GNE-6893, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of HPK1.
Tellis JC, Wei B, Siu M, An L, Chan GK, Chen Y, Du X, Gazzard L, Hu B, Kiefer J, Kakiuchi-Kiyota S, Lainchbury M, Linehan JL, Luo X, Malhotra S, Mendonca R, Pang J, Ran Y, Sethuraman V, Seward E, Sneeringer C, Su D, Wang W, Wu P, Moffat JG, Heffron TP, Choo EF, Chan BK. Tellis JC, et al. Among authors: kakiuchi kiyota s. ACS Med Chem Lett. 2024 Sep 3;15(9):1606-1614. doi: 10.1021/acsmedchemlett.4c00319. eCollection 2024 Sep 12. ACS Med Chem Lett. 2024. PMID: 39291002
A BCMA/CD16A bispecific innate cell engager for the treatment of multiple myeloma.
Kakiuchi-Kiyota S, Ross T, Wallweber HA, Kiefer JR, Schutten MM, Adedeji AO, Cai H, Hendricks R, Cohen S, Myneni S, Liu L, Fullerton A, Corr N, Yu L, de Almeida Nagata D, Zhong S, Leong SR, Li J, Nakamura R, Sumiyoshi T, Li J, Ovacik AM, Zheng B, Dillon M, Spiess C, Wingert S, Rajkovic E, Ellwanger K, Reusch U, Polson AG. Kakiuchi-Kiyota S, et al. Leukemia. 2022 Apr;36(4):1006-1014. doi: 10.1038/s41375-021-01478-w. Epub 2022 Jan 10. Leukemia. 2022. PMID: 35001074
A Non-covalent Ligand Reveals Biased Agonism of the TRPA1 Ion Channel.
Liu C, Reese R, Vu S, Rougé L, Shields SD, Kakiuchi-Kiyota S, Chen H, Johnson K, Shi YP, Chernov-Rogan T, Greiner DMZ, Kohli PB, Hackos D, Brillantes B, Tam C, Li T, Wang J, Safina B, Magnuson S, Volgraf M, Payandeh J, Zheng J, Rohou A, Chen J. Liu C, et al. Among authors: kakiuchi kiyota s. Neuron. 2021 Jan 20;109(2):273-284.e4. doi: 10.1016/j.neuron.2020.10.014. Epub 2020 Nov 4. Neuron. 2021. PMID: 33152265 Free PMC article.
Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity.
Crawford JJ, Lee W, Johnson AR, Delatorre KJ, Chen J, Eigenbrot C, Heidmann J, Kakiuchi-Kiyota S, Katewa A, Kiefer JR, Liu L, Lubach JW, Misner D, Purkey H, Reif K, Vogt J, Wong H, Yu C, Young WB. Crawford JJ, et al. Among authors: kakiuchi kiyota s. ACS Med Chem Lett. 2020 Jul 13;11(8):1588-1597. doi: 10.1021/acsmedchemlett.0c00249. eCollection 2020 Aug 13. ACS Med Chem Lett. 2020. PMID: 32832028 Free PMC article.
29 results