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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. Among authors: harris 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 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: harris al. 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
Discovery of 6-[(3S,4S)-4-Amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methyl-3,4-dihydropyrimidin-4-one (IACS-15414), a Potent and Orally Bioavailable SHP2 Inhibitor.
Czako B, Sun Y, McAfoos T, Cross JB, Leonard PG, Burke JP, Carroll CL, Feng N, Harris AL, Jiang Y, Kang Z, Kovacs JJ, Mandal P, Meyers BA, Mseeh F, Parker CA, Yu SS, Williams CC, Wu Q, Di Francesco ME, Draetta G, Heffernan T, Marszalek JR, Kohl NE, Jones P. Czako B, et al. Among authors: harris al. J Med Chem. 2021 Oct 28;64(20):15141-15169. doi: 10.1021/acs.jmedchem.1c01132. Epub 2021 Oct 13. J Med Chem. 2021. PMID: 34643390
Resistance to neoadjuvant chemotherapy in triple-negative breast cancer mediated by a reversible drug-tolerant state.
Echeverria GV, Ge Z, Seth S, Zhang X, Jeter-Jones S, Zhou X, Cai S, Tu Y, McCoy A, Peoples M, Sun Y, Qiu H, Chang Q, Bristow C, Carugo A, Shao J, Ma X, Harris A, Mundi P, Lau R, Ramamoorthy V, Wu Y, Alvarez MJ, Califano A, Moulder SL, Symmans WF, Marszalek JR, Heffernan TP, Chang JT, Piwnica-Worms H. Echeverria GV, et al. Sci Transl Med. 2019 Apr 17;11(488):eaav0936. doi: 10.1126/scitranslmed.aav0936. Sci Transl Med. 2019. PMID: 30996079 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. 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.
Sequential Administration of XPO1 and ATR Inhibitors Enhances Therapeutic Response in TP53-mutated Colorectal Cancer.
Inoue A, Robinson FS, Minelli R, Tomihara H, Rizi BS, Rose JL, Kodama T, Srinivasan S, Harris AL, Zuniga AM, Mullinax RA, Ma X, Seth S, Daniele JR, Peoples MD, Loponte S, Akdemir KC, Khor TO, Feng N, Roszik J, Sobieski MM, Brunell D, Stephan C, Giuliani V, Deem AK, Shingu T, Deribe YL, Menter DG, Heffernan TP, Viale A, Bristow CA, Kopetz S, Draetta GF, Genovese G, Carugo A. Inoue A, et al. Among authors: harris al. Gastroenterology. 2021 Jul;161(1):196-210. doi: 10.1053/j.gastro.2021.03.022. Epub 2021 Mar 19. Gastroenterology. 2021. PMID: 33745946 Free PMC article.
Discovery of IACS-9779 and IACS-70465 as Potent Inhibitors Targeting Indoleamine 2,3-Dioxygenase 1 (IDO1) Apoenzyme.
Hamilton MM, Mseeh F, McAfoos TJ, Leonard PG, Reyna NJ, Harris AL, Xu A, Han M, Soth MJ, Czako B, Theroff JP, Mandal PK, Burke JP, Virgin-Downey B, Petrocchi A, Pfaffinger D, Rogers NE, Parker CA, Yu SS, Jiang Y, Krapp S, Lammens A, Trevitt G, Tremblay MR, Mikule K, Wilcoxen K, Cross JB, Jones P, Marszalek JR, Lewis RT. Hamilton MM, et al. Among authors: harris al. J Med Chem. 2021 Aug 12;64(15):11302-11329. doi: 10.1021/acs.jmedchem.1c00679. Epub 2021 Jul 22. J Med Chem. 2021. PMID: 34292726
LP-925219 maximizes urinary glucose excretion in mice by inhibiting both renal SGLT1 and SGLT2.
Powell DR, Smith MG, Doree DD, Harris AL, Xiong WW, Mseeh F, Wilson A, Gopinathan S, Diaz D, Goodwin NC, Harrison B, Strobel E, Rawlins DB, Carson K, Zambrowicz B, Ding ZM. Powell DR, et al. Among authors: harris al. Pharmacol Res Perspect. 2015 Mar;3(2):e00129. doi: 10.1002/prp2.129. Epub 2015 Mar 31. Pharmacol Res Perspect. 2015. PMID: 26038705 Free PMC article.
Discovery of LX2761, a Sodium-Dependent Glucose Cotransporter 1 (SGLT1) Inhibitor Restricted to the Intestinal Lumen, for the Treatment of Diabetes.
Goodwin NC, Ding ZM, Harrison BA, Strobel ED, Harris AL, Smith M, Thompson AY, Xiong W, Mseeh F, Bruce DJ, Diaz D, Gopinathan S, Li L, O'Neill E, Thiel M, Wilson AG, Carson KG, Powell DR, Rawlins DB. Goodwin NC, et al. Among authors: harris al. J Med Chem. 2017 Jan 26;60(2):710-721. doi: 10.1021/acs.jmedchem.6b01541. Epub 2017 Jan 17. J Med Chem. 2017. PMID: 28045524
Effect of LX4211 on glucose homeostasis and body composition in preclinical models.
Powell DR, DaCosta CM, Smith M, Doree D, Harris A, Buhring L, Heydorn W, Nouraldeen A, Xiong W, Yalamanchili P, Mseeh F, Wilson A, Shadoan M, Zambrowicz B, Ding ZM. Powell DR, et al. J Pharmacol Exp Ther. 2014 Aug;350(2):232-42. doi: 10.1124/jpet.114.214304. Epub 2014 May 21. J Pharmacol Exp Ther. 2014. PMID: 24849925
1,286 results