Andrew P Crew
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Explore the profile of Andrew P Crew including associated specialties, affiliations and a list of published articles.
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15
Citations
1453
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Recent Articles
1.
Salami J, Alabi S, Willard R, Vitale N, Wang J, Dong H, et al.
Commun Biol
. 2018 Oct;
1:100.
PMID: 30271980
The androgen receptor is a major driver of prostate cancer and inhibition of its transcriptional activity using competitive antagonists, such as enzalutamide remains a frontline therapy for prostate cancer management....
2.
Burslem G, Smith B, Lai A, Jaime-Figueroa S, McQuaid D, Bondeson D, et al.
Cell Chem Biol
. 2017 Nov;
25(1):67-77.e3.
PMID: 29129716
Proteolysis targeting chimera (PROTAC) technology has emerged over the last two decades as a powerful tool for targeted degradation of endogenous proteins. Herein we describe the development of PROTACs for...
3.
Crew A, Raina K, Dong H, Qian Y, Wang J, Vigil D, et al.
J Med Chem
. 2017 Jul;
61(2):583-598.
PMID: 28692295
Proteolysis targeting chimeras (PROTACs) are bifunctional molecules that recruit an E3 ligase to a target protein to facilitate ubiquitination and subsequent degradation of that protein. While the field of targeted...
4.
Raina K, Lu J, Qian Y, Altieri M, Gordon D, Rossi A, et al.
Proc Natl Acad Sci U S A
. 2016 Jun;
113(26):7124-9.
PMID: 27274052
Prostate cancer has the second highest incidence among cancers in men worldwide and is the second leading cause of cancer deaths of men in the United States. Although androgen deprivation...
5.
Lu J, Qian Y, Altieri M, Dong H, Wang J, Raina K, et al.
Chem Biol
. 2015 Jun;
22(6):755-63.
PMID: 26051217
BRD4, a bromodomain and extraterminal domain (BET) family member, is an attractive target in multiple pathological settings, particularly cancer. While BRD4 inhibitors have shown some promise in MYC-driven malignancies such...
6.
Hornberger K, Chen X, Crew A, Kleinberg A, Ma L, Mulvihill M, et al.
Bioorg Med Chem Lett
. 2013 Jul;
23(16):4511-6.
PMID: 23856049
The kinase selectivity and pharmacokinetic optimization of a series of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1 is described. The intersection of insights from molecular modeling, computational prediction of metabolic sites, and in...
7.
Hornberger K, Berger D, Crew A, Dong H, Kleinberg A, Li A, et al.
Bioorg Med Chem Lett
. 2013 Jul;
23(16):4517-22.
PMID: 23850198
The discovery and potency optimization of a series of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1 is described. Micromolar hits taken from high-throughput screening were optimized for biochemical and cellular mechanistic potency to...
8.
Jin M, Wang J, Kleinberg A, Kadalbajoo M, Siu K, Cooke A, et al.
Bioorg Med Chem Lett
. 2013 Jan;
23(4):979-84.
PMID: 23317569
This Letter describes the medicinal chemistry effort towards a series of novel imidazo[1,5-a]pyrazine derived inhibitors of ACK1. Virtual screening led to the discovery of the initial hit, and subsequent exploration...
9.
Bhagwat S, Gokhale P, Crew A, Cooke A, Yao Y, Mantis C, et al.
Mol Cancer Ther
. 2011 Jun;
10(8):1394-406.
PMID: 21673091
The phosphoinositide 3-kinase (PI3K)/AKT/mTOR pathway is frequently activated in human cancers, and mTOR is a clinically validated target. mTOR forms two distinct multiprotein complexes, mTORC1 and mTORC2, which regulate cell...
10.
Crew A, Bhagwat S, Dong H, Bittner M, Chan A, Chen X, et al.
Bioorg Med Chem Lett
. 2011 Mar;
21(7):2092-7.
PMID: 21353551
The discovery and optimization of a series of imidazo[1,5-a]pyrazine inhibitors of mTOR is described. HTS hits were optimized for potency, selectivity and metabolic stability to provide the orally bioavailable proof...