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Page 1
Mass Balance of the Indoleamine 2,3-Dioxygenase Inhibitor Navoximod (GDC-0919) in Rats and Dogs: Unexpected Cyanide Release from Imidazo[5,1-a]isoindole and Species Differences in Glucuronidation.
Wang S, Ma S, Chen E, Wang J, Le H, Hanlon SP, Binder M, Lee W, Khojasteh SC, Salphati L. Wang S, et al. Among authors: salphati l. Drug Metab Dispos. 2023 Jul;51(7):862-872. doi: 10.1124/dmd.123.001289. Epub 2023 Apr 14. Drug Metab Dispos. 2023. PMID: 37059472
GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway.
Wallin JJ, Edgar KA, Guan J, Berry M, Prior WW, Lee L, Lesnick JD, Lewis C, Nonomiya J, Pang J, Salphati L, Olivero AG, Sutherlin DP, O'Brien C, Spoerke JM, Patel S, Lensun L, Kassees R, Ross L, Lackner MR, Sampath D, Belvin M, Friedman LS. Wallin JJ, et al. Among authors: salphati l. Mol Cancer Ther. 2011 Dec;10(12):2426-36. doi: 10.1158/1535-7163.MCT-11-0446. Epub 2011 Oct 13. Mol Cancer Ther. 2011. PMID: 21998291
The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α.
Heffron TP, Salphati L, Alicke B, Cheong J, Dotson J, Edgar K, Goldsmith R, Gould SE, Lee LB, Lesnick JD, Lewis C, Ndubaku C, Nonomiya J, Olivero AG, Pang J, Plise EG, Sideris S, Trapp S, Wallin J, Wang L, Zhang X. Heffron TP, et al. Among authors: salphati l. J Med Chem. 2012 Sep 27;55(18):8007-20. doi: 10.1021/jm300867c. Epub 2012 Sep 11. J Med Chem. 2012. PMID: 22946614
Targeting the PI3K pathway in the brain--efficacy of a PI3K inhibitor optimized to cross the blood-brain barrier.
Salphati L, Heffron TP, Alicke B, Nishimura M, Barck K, Carano RA, Cheong J, Edgar KA, Greve J, Kharbanda S, Koeppen H, Lau S, Lee LB, Pang J, Plise EG, Pokorny JL, Reslan HB, Sarkaria JN, Wallin JJ, Zhang X, Gould SE, Olivero AG, Phillips HS. Salphati L, et al. Clin Cancer Res. 2012 Nov 15;18(22):6239-48. doi: 10.1158/1078-0432.CCR-12-0720. Epub 2012 Sep 19. Clin Cancer Res. 2012. PMID: 22992516
Distribution of the phosphatidylinositol 3-kinase inhibitors Pictilisib (GDC-0941) and GNE-317 in U87 and GS2 intracranial glioblastoma models-assessment by matrix-assisted laser desorption ionization imaging.
Salphati L, Shahidi-Latham S, Quiason C, Barck K, Nishimura M, Alicke B, Pang J, Carano RA, Olivero AG, Phillips HS. Salphati L, et al. Drug Metab Dispos. 2014 Jul;42(7):1110-6. doi: 10.1124/dmd.114.057513. Epub 2014 Apr 22. Drug Metab Dispos. 2014. PMID: 24754926
Strategically Timing Inhibition of Phosphatidylinositol 3-Kinase to Maximize Therapeutic Index in Estrogen Receptor Alpha-Positive, PIK3CA-Mutant Breast Cancer.
Yang W, Hosford SR, Dillon LM, Shee K, Liu SC, Bean JR, Salphati L, Pang J, Zhang X, Nannini MA, Demidenko E, Bates D, Lewis LD, Marotti JD, Eastman AR, Miller TW. Yang W, et al. Among authors: salphati l. Clin Cancer Res. 2016 May 1;22(9):2250-60. doi: 10.1158/1078-0432.CCR-15-2276. Epub 2016 Jan 5. Clin Cancer Res. 2016. PMID: 26733612 Free PMC article.
The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).
Heffron TP, Heald RA, Ndubaku C, Wei B, Augistin M, Do S, Edgar K, Eigenbrot C, Friedman L, Gancia E, Jackson PS, Jones G, Kolesnikov A, Lee LB, Lesnick JD, Lewis C, McLean N, Mörtl M, Nonomiya J, Pang J, Price S, Prior WW, Salphati L, Sideris S, Staben ST, Steinbacher S, Tsui V, Wallin J, Sampath D, Olivero AG. Heffron TP, et al. Among authors: salphati l. J Med Chem. 2016 Feb 11;59(3):985-1002. doi: 10.1021/acs.jmedchem.5b01483. Epub 2016 Jan 20. J Med Chem. 2016. PMID: 26741947
Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.
Heffron TP, Ndubaku CO, Salphati L, Alicke B, Cheong J, Drobnick J, Edgar K, Gould SE, Lee LB, Lesnick JD, Lewis C, Nonomiya J, Pang J, Plise EG, Sideris S, Wallin J, Wang L, Zhang X, Olivero AG. Heffron TP, et al. Among authors: salphati l. ACS Med Chem Lett. 2016 Feb 16;7(4):351-6. doi: 10.1021/acsmedchemlett.6b00005. eCollection 2016 Apr 14. ACS Med Chem Lett. 2016. PMID: 27096040 Free PMC article.
96 results