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Page 1
Preclinical evaluation of proteolytic targeting of LCK as a therapeutic approach in T cell acute lymphoblastic leukemia.
Hu J, Jarusiewicz J, Du G, Nishiguchi G, Yoshimura S, Panetta JC, Li Z, Min J, Yang L, Chepyala D, Actis M, Reyes N, Smart B, Pui CH, Teachey DT, Rankovic Z, Yang JJ. Hu J, et al. Among authors: nishiguchi g. Sci Transl Med. 2022 Aug 24;14(659):eabo5228. doi: 10.1126/scitranslmed.abo5228. Epub 2022 Aug 24. Sci Transl Med. 2022. PMID: 36001679 Free PMC article.
Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators.
Nishiguchi G, Keramatnia F, Min J, Chang Y, Jonchere B, Das S, Actis M, Price J, Chepyala D, Young B, McGowan K, Slavish PJ, Mayasundari A, Jarusiewicz JA, Yang L, Li Y, Fu X, Garrett SH, Papizan JB, Kodali K, Peng J, Pruett Miller SM, Roussel MF, Mullighan C, Fischer M, Rankovic Z. Nishiguchi G, et al. J Med Chem. 2021 Jun 10;64(11):7296-7311. doi: 10.1021/acs.jmedchem.0c01313. Epub 2021 May 27. J Med Chem. 2021. PMID: 34042448 Free PMC article.
Phenyl-Glutarimides: Alternative Cereblon Binders for the Design of PROTACs.
Min J, Mayasundari A, Keramatnia F, Jonchere B, Yang SW, Jarusiewicz J, Actis M, Das S, Young B, Slavish J, Yang L, Li Y, Fu X, Garrett SH, Yun MK, Li Z, Nithianantham S, Chai S, Chen T, Shelat A, Lee RE, Nishiguchi G, White SW, Roussel MF, Potts PR, Fischer M, Rankovic Z. Min J, et al. Among authors: nishiguchi g. Angew Chem Int Ed Engl. 2021 Dec 13;60(51):26663-26670. doi: 10.1002/anie.202108848. Epub 2021 Nov 16. Angew Chem Int Ed Engl. 2021. PMID: 34614283 Free PMC article.
Development of Potent and Selective Janus Kinase 2/3 Directing PG-PROTACs.
Alcock LJ, Chang Y, Jarusiewicz JA, Actis M, Nithianantham S, Mayasundari A, Min J, Maxwell D, Hunt J, Smart B, Yang JJ, Nishiguchi G, Fischer M, Mullighan CG, Rankovic Z. Alcock LJ, et al. Among authors: nishiguchi g. ACS Med Chem Lett. 2022 Feb 21;13(3):475-482. doi: 10.1021/acsmedchemlett.1c00650. eCollection 2022 Mar 10. ACS Med Chem Lett. 2022. PMID: 35300081 Free PMC article.
Phenyl Dihydrouracil: An Alternative Cereblon Binder for PROTAC Design.
Jarusiewicz JA, Yoshimura S, Mayasundari A, Actis M, Aggarwal A, McGowan K, Yang L, Li Y, Fu X, Mishra V, Heath R, Narina S, Pruett-Miller SM, Nishiguchi G, Yang JJ, Rankovic Z. Jarusiewicz JA, et al. Among authors: nishiguchi g. ACS Med Chem Lett. 2023 Jan 4;14(2):141-145. doi: 10.1021/acsmedchemlett.2c00436. eCollection 2023 Feb 9. ACS Med Chem Lett. 2023. PMID: 36793425 Free PMC article.
Development of an Orally Bioavailable LCK PROTAC Degrader as a Potential Therapeutic Approach to T-Cell Acute Lymphoblastic Leukemia.
Jarusiewicz JA, Yoshimura S, Actis M, Li Y, Fu X, Yang L, Narina S, Pruett-Miller SM, Zhou S, Wang X, High AA, Nishiguchi G, Yang JJ, Rankovic Z. Jarusiewicz JA, et al. Among authors: nishiguchi g. J Med Chem. 2024 Jul 25;67(14):11868-11884. doi: 10.1021/acs.jmedchem.4c00481. Epub 2024 Jul 8. J Med Chem. 2024. PMID: 38973320
Synthesis and Structure-Activity Relationship of Tetra-Substituted Cyclohexyl Diol Inhibitors of Proviral Insertion of Moloney Virus (PIM) Kinases.
Han W, Ding Y, Chen Z, Langowski JL, Bellamacina C, Rico A, Nishiguchi GA, Lan J, Atallah G, Lindvall M, Lin S, Zang R, Feucht P, Zavorotinskaya T, Dai Y, Garcia P, Burger MT. Han W, et al. Among authors: nishiguchi ga. J Med Chem. 2020 Dec 10;63(23):14885-14904. doi: 10.1021/acs.jmedchem.0c01279. Epub 2020 Dec 1. J Med Chem. 2020. PMID: 33258605
Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.
Burger MT, Nishiguchi G, Han W, Lan J, Simmons R, Atallah G, Ding Y, Tamez V, Zhang Y, Mathur M, Muller K, Bellamacina C, Lindvall MK, Zang R, Huh K, Feucht P, Zavorotinskaya T, Dai Y, Basham S, Chan J, Ginn E, Aycinena A, Holash J, Castillo J, Langowski JL, Wang Y, Chen MY, Lambert A, Fritsch C, Kauffmann A, Pfister E, Vanasse KG, Garcia PD. Burger MT, et al. Among authors: nishiguchi g. J Med Chem. 2015 Nov 12;58(21):8373-86. doi: 10.1021/acs.jmedchem.5b01275. Epub 2015 Oct 27. J Med Chem. 2015. PMID: 26505898
26 results