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Page 1
Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.
Lu J, Qian Y, Altieri M, Dong H, Wang J, Raina K, Hines J, Winkler JD, Crew AP, Coleman K, Crews CM. Lu J, et al. Among authors: crew ap. Chem Biol. 2015 Jun 18;22(6):755-63. doi: 10.1016/j.chembiol.2015.05.009. Epub 2015 Jun 4. Chem Biol. 2015. PMID: 26051217 Free PMC article.
Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells.
Saenz DT, Fiskus W, Qian Y, Manshouri T, Rajapakshe K, Raina K, Coleman KG, Crew AP, Shen A, Mill CP, Sun B, Qiu P, Kadia TM, Pemmaraju N, DiNardo C, Kim MS, Nowak AJ, Coarfa C, Crews CM, Verstovsek S, Bhalla KN. Saenz DT, et al. Among authors: crew ap. Leukemia. 2017 Sep;31(9):1951-1961. doi: 10.1038/leu.2016.393. Epub 2017 Feb 2. Leukemia. 2017. PMID: 28042144 Free PMC article.
The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study.
Burslem GM, Smith BE, Lai AC, Jaime-Figueroa S, McQuaid DC, Bondeson DP, Toure M, Dong H, Qian Y, Wang J, Crew AP, Hines J, Crews CM. Burslem GM, et al. Among authors: crew ap. Cell Chem Biol. 2018 Jan 18;25(1):67-77.e3. doi: 10.1016/j.chembiol.2017.09.009. Epub 2017 Nov 9. Cell Chem Biol. 2018. PMID: 29129716 Free PMC article.
Imidazo[1,5-a]pyrazines: orally efficacious inhibitors of mTORC1 and mTORC2.
Crew AP, Bhagwat SV, Dong H, Bittner MA, Chan A, Chen X, Coate H, Cooke A, Gokhale PC, Honda A, Jin M, Kahler J, Mantis C, Mulvihill MJ, Tavares-Greco PA, Volk B, Wang J, Werner DS, Arnold LD, Pachter JA, Wild R, Gibson NW. Crew AP, et al. Bioorg Med Chem Lett. 2011 Apr 1;21(7):2092-7. doi: 10.1016/j.bmcl.2011.01.139. Epub 2011 Feb 3. Bioorg Med Chem Lett. 2011. PMID: 21353551
Discovery and optimization of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1.
Hornberger KR, Berger DM, Crew AP, Dong H, Kleinberg A, Li AH, Medeiros MR, Mulvihill MJ, Siu K, Tarrant J, Wang J, Weng F, Wilde VL, Albertella M, Bittner M, Cooke A, Gray MJ, Maresca P, May E, Meyn P, Peick W Jr, Romashko D, Tanowitz M, Tokar B. Hornberger KR, et al. Among authors: crew ap. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4517-22. doi: 10.1016/j.bmcl.2013.06.053. Epub 2013 Jun 25. Bioorg Med Chem Lett. 2013. PMID: 23850198
Discovery of potent, selective and orally bioavailable imidazo[1,5-a]pyrazine derived ACK1 inhibitors.
Jin M, Wang J, Kleinberg A, Kadalbajoo M, Siu KW, Cooke A, Bittner MA, Yao Y, Thelemann A, Ji Q, Bhagwat S, Mulvihill KM, Rechka JA, Pachter JA, Crew AP, Epstein D, Mulvihill MJ. Jin M, et al. Among authors: crew ap. Bioorg Med Chem Lett. 2013 Feb 15;23(4):979-84. doi: 10.1016/j.bmcl.2012.12.042. Epub 2012 Dec 21. Bioorg Med Chem Lett. 2013. PMID: 23317569
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