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Page 1
Noncovalent wild-type-sparing inhibitors of EGFR T790M.
Lee HJ, Schaefer G, Heffron TP, Shao L, Ye X, Sideris S, Malek S, Chan E, Merchant M, La H, Ubhayakar S, Yauch RL, Pirazzoli V, Politi K, Settleman J. Lee HJ, et al. Among authors: heffron tp. Cancer Discov. 2013 Feb;3(2):168-81. doi: 10.1158/2159-8290.CD-12-0357. Epub 2012 Dec 10. Cancer Discov. 2013. PMID: 23229345 Free PMC article.
Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.
Hanan EJ, Eigenbrot C, Bryan MC, Burdick DJ, Chan BK, Chen Y, Dotson J, Heald RA, Jackson PS, La H, Lainchbury MD, Malek S, Purkey HE, Schaefer G, Schmidt S, Seward EM, Sideris S, Tam C, Wang S, Yeap SK, Yen I, Yin J, Yu C, Zilberleyb I, Heffron TP. Hanan EJ, et al. Among authors: heffron tp. J Med Chem. 2014 Dec 11;57(23):10176-91. doi: 10.1021/jm501578n. Epub 2014 Nov 20. J Med Chem. 2014. PMID: 25383627 Free PMC article.
Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study.
Heald R, Bowman KK, Bryan MC, Burdick D, Chan B, Chan E, Chen Y, Clausen S, Dominguez-Fernandez B, Eigenbrot C, Elliott R, Hanan EJ, Jackson P, Knight J, La H, Lainchbury M, Malek S, Mann S, Merchant M, Mortara K, Purkey H, Schaefer G, Schmidt S, Seward E, Sideris S, Shao L, Wang S, Yeap K, Yen I, Yu C, Heffron TP. Heald R, et al. Among authors: heffron tp. J Med Chem. 2015 Nov 25;58(22):8877-95. doi: 10.1021/acs.jmedchem.5b01412. Epub 2015 Nov 12. J Med Chem. 2015. PMID: 26455919
4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.
Hanan EJ, Baumgardner M, Bryan MC, Chen Y, Eigenbrot C, Fan P, Gu XH, La H, Malek S, Purkey HE, Schaefer G, Schmidt S, Sideris S, Yen I, Yu C, Heffron TP. Hanan EJ, et al. Among authors: heffron tp. Bioorg Med Chem Lett. 2016 Jan 15;26(2):534-539. doi: 10.1016/j.bmcl.2015.11.078. Epub 2015 Nov 22. Bioorg Med Chem Lett. 2016. PMID: 26639762
Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.
Bryan MC, Burdick DJ, Chan BK, Chen Y, Clausen S, Dotson J, Eigenbrot C, Elliott R, Hanan EJ, Heald R, Jackson P, La H, Lainchbury M, Malek S, Mann SE, Purkey HE, Schaefer G, Schmidt S, Seward E, Sideris S, Wang S, Yen I, Yu C, Heffron TP. Bryan MC, et al. Among authors: heffron tp. ACS Med Chem Lett. 2015 Dec 17;7(1):100-4. doi: 10.1021/acsmedchemlett.5b00428. eCollection 2016 Jan 14. ACS Med Chem Lett. 2015. PMID: 26819674 Free PMC article.
RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy.
Song KW, Edgar KA, Hanan EJ, Hafner M, Oeh J, Merchant M, Sampath D, Nannini MA, Hong R, Phu L, Forrest WF, Stawiski E, Schmidt S, Endres N, Guan J, Wallin JJ, Cheong J, Plise EG, Lewis Phillips GD, Salphati L, Heffron TP, Olivero AG, Malek S, Staben ST, Kirkpatrick DS, Dey A, Friedman LS. Song KW, et al. Among authors: heffron tp. Cancer Discov. 2022 Jan;12(1):204-219. doi: 10.1158/2159-8290.CD-21-0072. Epub 2021 Sep 20. Cancer Discov. 2022. PMID: 34544753 Free PMC article.
Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor.
Chan BK, Hanan EJ, Bowman KK, Bryan MC, Burdick D, Chan E, Chen Y, Clausen S, Dela Vega T, Dotson J, Eigenbrot C, Elliott RL, Heald RA, Jackson PS, Knight JD, La H, Lainchbury MD, Malek S, Purkey HE, Schaefer G, Schmidt S, Seward EM, Sideris S, Shao L, Wang S, Yeap SK, Yen I, Yu C, Heffron TP. Chan BK, et al. Among authors: heffron tp. J Med Chem. 2016 Oct 13;59(19):9080-9093. doi: 10.1021/acs.jmedchem.6b00995. Epub 2016 Sep 12. J Med Chem. 2016. PMID: 27564586
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.
Heffron TP, Berry M, Castanedo G, Chang C, Chuckowree I, Dotson J, Folkes A, Gunzner J, Lesnick JD, Lewis C, Mathieu S, Nonomiya J, Olivero A, Pang J, Peterson D, Salphati L, Sampath D, Sideris S, Sutherlin DP, Tsui V, Wan NC, Wang S, Wong S, Zhu BY. Heffron TP, et al. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2408-11. doi: 10.1016/j.bmcl.2010.03.046. Epub 2010 Mar 12. Bioorg Med Chem Lett. 2010. PMID: 20346656
Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.
Ndubaku CO, Heffron TP, Staben ST, Baumgardner M, Blaquiere N, Bradley E, Bull R, Do S, Dotson J, Dudley D, Edgar KA, Friedman LS, Goldsmith R, Heald RA, Kolesnikov A, Lee L, Lewis C, Nannini M, Nonomiya J, Pang J, Price S, Prior WW, Salphati L, Sideris S, Wallin JJ, Wang L, Wei B, Sampath D, Olivero AG. Ndubaku CO, et al. Among authors: heffron tp. J Med Chem. 2013 Jun 13;56(11):4597-610. doi: 10.1021/jm4003632. Epub 2013 Jun 3. J Med Chem. 2013. PMID: 23662903
39 results