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Page 1
Discovery of IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R.
Czako B, Marszalek JR, Burke JP, Mandal P, Leonard PG, Cross JB, Mseeh F, Jiang Y, Chang EQ, Suzuki E, Kovacs JJ, Feng N, Gera S, Harris AL, Liu Z, Mullinax RA, Pang J, Parker CA, Spencer ND, Yu SS, Wu Q, Tremblay MR, Mikule K, Wilcoxen K, Heffernan TP, Draetta GF, Jones P. Czako B, et al. Among authors: leonard pg. J Med Chem. 2020 Sep 10;63(17):9888-9911. doi: 10.1021/acs.jmedchem.0c00936. Epub 2020 Aug 18. J Med Chem. 2020. PMID: 32787110
Identification of potent and selective MTH1 inhibitors.
Petrocchi A, Leo E, Reyna NJ, Hamilton MM, Shi X, Parker CA, Mseeh F, Bardenhagen JP, Leonard P, Cross JB, Huang S, Jiang Y, Cardozo M, Draetta G, Marszalek JR, Toniatti C, Jones P, Lewis RT. Petrocchi A, et al. Bioorg Med Chem Lett. 2016 Mar 15;26(6):1503-1507. doi: 10.1016/j.bmcl.2016.02.026. Epub 2016 Feb 11. Bioorg Med Chem Lett. 2016. PMID: 26898335
SF2312 is a natural phosphonate inhibitor of enolase.
Leonard PG, Satani N, Maxwell D, Lin YH, Hammoudi N, Peng Z, Pisaneschi F, Link TM, Lee GR 4th, Sun D, Prasad BAB, Di Francesco ME, Czako B, Asara JM, Wang YA, Bornmann W, DePinho RA, Muller FL. Leonard PG, et al. Nat Chem Biol. 2016 Dec;12(12):1053-1058. doi: 10.1038/nchembio.2195. Epub 2016 Oct 10. Nat Chem Biol. 2016. PMID: 27723749 Free PMC article.
Functional Genomics Reveals Synthetic Lethality between Phosphogluconate Dehydrogenase and Oxidative Phosphorylation.
Sun Y, Bandi M, Lofton T, Smith M, Bristow CA, Carugo A, Rogers N, Leonard P, Chang Q, Mullinax R, Han J, Shi X, Seth S, Meyers BA, Miller M, Miao L, Ma X, Feng N, Giuliani V, Geck Do M, Czako B, Palmer WS, Mseeh F, Asara JM, Jiang Y, Morlacchi P, Zhao S, Peoples M, Tieu TN, Warmoes MO, Lorenzi PL, Muller FL, DePinho RA, Draetta GF, Toniatti C, Jones P, Heffernan TP, Marszalek JR. Sun Y, et al. Cell Rep. 2019 Jan 8;26(2):469-482.e5. doi: 10.1016/j.celrep.2018.12.043. Cell Rep. 2019. PMID: 30625329 Free article.
Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib.
Sun Y, Meyers BA, Czako B, Leonard P, Mseeh F, Harris AL, Wu Q, Johnson S, Parker CA, Cross JB, Di Francesco ME, Bivona BJ, Bristow CA, Burke JP, Carrillo CC, Carroll CL, Chang Q, Feng N, Gao G, Gera S, Giuliani V, Huang JK, Jiang Y, Kang Z, Kovacs JJ, Liu CY, Lopez AM, Ma X, Mandal PK, McAfoos T, Miller MA, Mullinax RA, Peoples M, Ramamoorthy V, Seth S, Spencer ND, Suzuki E, Williams CC, Yu SS, Zuniga AM, Draetta GF, Marszalek JR, Heffernan TP, Kohl NE, Jones P. Sun Y, et al. Cancer Res. 2020 Nov 1;80(21):4840-4853. doi: 10.1158/0008-5472.CAN-20-1634. Epub 2020 Sep 14. Cancer Res. 2020. PMID: 32928921 Free PMC article.
Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties.
Soth MJ, Le K, Di Francesco ME, Hamilton MM, Liu G, Burke JP, Carroll CL, Kovacs JJ, Bardenhagen JP, Bristow CA, Cardozo M, Czako B, de Stanchina E, Feng N, Garvey JR, Gay JP, Do MKG, Greer J, Han M, Harris A, Herrera Z, Huang S, Giuliani V, Jiang Y, Johnson SB, Johnson TA, Kang Z, Leonard PG, Liu Z, McAfoos T, Miller M, Morlacchi P, Mullinax RA, Palmer WS, Pang J, Rogers N, Rudin CM, Shepard HE, Spencer ND, Theroff J, Wu Q, Xu A, Yau JA, Draetta G, Toniatti C, Heffernan TP, Jones P. Soth MJ, et al. Among authors: leonard pg. J Med Chem. 2020 Nov 12;63(21):12957-12977. doi: 10.1021/acs.jmedchem.0c01398. Epub 2020 Oct 29. J Med Chem. 2020. PMID: 33118821 Free PMC article.
An enolase inhibitor for the targeted treatment of ENO1-deleted cancers.
Lin YH, Satani N, Hammoudi N, Yan VC, Barekatain Y, Khadka S, Ackroyd JJ, Georgiou DK, Pham CD, Arthur K, Maxwell D, Peng Z, Leonard PG, Czako B, Pisaneschi F, Mandal P, Sun Y, Zielinski R, Pando SC, Wang X, Tran T, Xu Q, Wu Q, Jiang Y, Kang Z, Asara JM, Priebe W, Bornmann W, Marszalek JR, DePinho RA, Muller FL. Lin YH, et al. Among authors: leonard pg. Nat Metab. 2020 Dec;2(12):1413-1426. doi: 10.1038/s42255-020-00313-3. Epub 2020 Nov 23. Nat Metab. 2020. PMID: 33230295 Free PMC article.
Author Correction: An enolase inhibitor for the targeted treatment of ENO1-deleted cancers.
Lin YH, Satani N, Hammoudi N, Yan VC, Barekatain Y, Khadka S, Ackroyd JJ, Georgiou DK, Pham CD, Arthur K, Maxwell D, Peng Z, Leonard PG, Czako B, Pisaneschi F, Mandal P, Sun Y, Zielinski R, Pando SC, Wang X, Tran T, Xu Q, Wu Q, Jiang Y, Kang Z, Asara JM, Priebe W, Bornmann W, Marszalek JR, DePinho RA, Muller FL. Lin YH, et al. Among authors: leonard pg. Nat Metab. 2021 Jan;3(1):122. doi: 10.1038/s42255-020-00335-x. Nat Metab. 2021. PMID: 33340032 No abstract available.
69 results