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The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer.
Folkes AJ, Ahmadi K, Alderton WK, Alix S, Baker SJ, Box G, Chuckowree IS, Clarke PA, Depledge P, Eccles SA, Friedman LS, Hayes A, Hancox TC, Kugendradas A, Lensun L, Moore P, Olivero AG, Pang J, Patel S, Pergl-Wilson GH, Raynaud FI, Robson A, Saghir N, Salphati L, Sohal S, Ultsch MH, Valenti M, Wallweber HJ, Wan NC, Wiesmann C, Workman P, Zhyvoloup A, Zvelebil MJ, Shuttleworth SJ. Folkes AJ, et al. Among authors: saghir n. J Med Chem. 2008 Sep 25;51(18):5522-32. doi: 10.1021/jm800295d. J Med Chem. 2008. PMID: 18754654
Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941.
Raynaud FI, Eccles SA, Patel S, Alix S, Box G, Chuckowree I, Folkes A, Gowan S, De Haven Brandon A, Di Stefano F, Hayes A, Henley AT, Lensun L, Pergl-Wilson G, Robson A, Saghir N, Zhyvoloup A, McDonald E, Sheldrake P, Shuttleworth S, Valenti M, Wan NC, Clarke PA, Workman P. Raynaud FI, et al. Among authors: saghir n. Mol Cancer Ther. 2009 Jul;8(7):1725-38. doi: 10.1158/1535-7163.MCT-08-1200. Epub 2009 Jul 7. Mol Cancer Ther. 2009. PMID: 19584227 Free PMC article.
Preparation and evaluation of trisubstituted pyrimidines as phosphatidylinositol 3-kinase inhibitors. 3-Hydroxyphenol analogues and bioisosteric replacements.
Large JM, Torr JE, Raynaud FI, Clarke PA, Hayes A, Stefano Fd, Urban F, Shuttleworth SJ, Saghir N, Sheldrake P, Workman P, McDonald E. Large JM, et al. Among authors: saghir n. Bioorg Med Chem. 2011 Jan 15;19(2):836-51. doi: 10.1016/j.bmc.2010.12.006. Epub 2010 Dec 9. Bioorg Med Chem. 2011. PMID: 21216151
Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases.
Raynaud FI, Eccles S, Clarke PA, Hayes A, Nutley B, Alix S, Henley A, Di-Stefano F, Ahmad Z, Guillard S, Bjerke LM, Kelland L, Valenti M, Patterson L, Gowan S, de Haven Brandon A, Hayakawa M, Kaizawa H, Koizumi T, Ohishi T, Patel S, Saghir N, Parker P, Waterfield M, Workman P. Raynaud FI, et al. Among authors: saghir n. Cancer Res. 2007 Jun 15;67(12):5840-50. doi: 10.1158/0008-5472.CAN-06-4615. Cancer Res. 2007. PMID: 17575152 Free article.
Exploring the specificity of the PI3K family inhibitor LY294002.
Gharbi SI, Zvelebil MJ, Shuttleworth SJ, Hancox T, Saghir N, Timms JF, Waterfield MD. Gharbi SI, et al. Among authors: saghir n. Biochem J. 2007 May 15;404(1):15-21. doi: 10.1042/BJ20061489. Biochem J. 2007. PMID: 17302559 Free PMC article.
Republication: Targeting PI3KC2β Impairs Proliferation and Survival in Acute Leukemia, Brain Tumours and Neuroendocrine Tumours.
Boller D, Doepfner KT, Laurentiis A, Guerreiro AS, Marinov M, Shalaby T, Depledge P, Robson A, Saghir N, Hayakawa M, Kaizawa H, Koizumi T, Ohishi T, Fattet S, Delattre O, Schweri-Olac A, Höland K, Grotzer MA, Frei K, Spertini O, Waterfield MD, Arcaro A. Boller D, et al. Among authors: saghir n. Anticancer Res. 2022 Jun;42(6):3217-3230. doi: 10.21873/anticanres.15812. Anticancer Res. 2022. PMID: 35641277 Free article.
Targeting PI3KC2β impairs proliferation and survival in acute leukemia, brain tumours and neuroendocrine tumours.
Boller D, Doepfner KT, De Laurentiis A, Guerreiro AS, Marinov M, Shalaby T, Depledge P, Robson A, Saghir N, Hayakawa M, Kaizawa H, Koizumi T, Ohishi T, Fattet S, Delattre O, Schweri-Olac A, Höland K, Grotzer MA, Frei K, Spertini O, Waterfield MD, Arcaro A. Boller D, et al. Among authors: saghir n. Anticancer Res. 2012 Aug;32(8):3015-27. Anticancer Res. 2012. PMID: 22843869 Retracted.
Systemic Treatment of Patients With Metastatic Breast Cancer: ASCO Resource-Stratified Guideline.
Al Sukhun S, Temin S, Barrios CH, Antone NZ, Guerra YC, Chavez-MacGregor M, Chopra R, Danso MA, Gomez HL, Homian NM, Kandil A, Kithaka B, Koczwara B, Moy B, Nakigudde G, Petracci FE, Rugo HS, El Saghir NS, Arun BK. Al Sukhun S, et al. Among authors: el saghir ns. JCO Glob Oncol. 2024 Jan;10:e2300285. doi: 10.1200/GO.23.00285. JCO Glob Oncol. 2024. PMID: 38206277 Free PMC article.
175 results