Modulating Androgen Receptor-Driven Transcription in Prostat…

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Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors

Article 2020 EN Hybrid

Castration-resistant prostate cancers (CRPCs) lose sensitivity to androgen-deprivation therapies but frequently remain dependent on oncogenic transcription driven by the androgen receptor (AR) and its splice variants. To discover modulators of AR-variant activity, we used a lysate-based small-molecule microarray assay and identified KI-ARv-03 as an AR-variant complex binder that reduces AR-driven…

86

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82

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39

Authors

6.62

FWCI

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39 authors
#AuthorInstitutionsORCID
1 André Richters Broad Institute (US) Koch Institute for Integrative… (US) +1 —
2 Shelby K. Doyle Broad Institute (US) Koch Institute for Integrative… (US) +1
3 David B. Freeman Cambridge Intellectual Propert… (GB)
4 Christina Lai Ling Lee Cambridge Intellectual Propert… (GB)
5 Becky S. Leifer Broad Institute (US) Koch Institute for Integrative… (US) +1
6 Sajjeev Jagannathan Baylor College of Medicine (US)
7 Florian Kabinger Broad Institute (US) Koch Institute for Integrative… (US) +1
8 Jošt Vrabič Koren Baylor College of Medicine (US)
9 Nicholas B. Struntz Broad Institute (US) Koch Institute for Integrative… (US) +1 —
10 Julie Urgiles Koch Institute for Integrative… (US) Massachusetts Institute of Tec… (US)
11 Ryan A. Stagg Boston University (US) Koch Institute for Integrative… (US) +1 —
12 Brice H. Curtin Broad Institute (US) Koch Institute for Integrative… (US) +1 —
13 Deep Chatterjee Goethe University Frankfurt (DE)
14 Sebastian Mathea Goethe University Frankfurt (DE)
15 Peter J. Mikochik Cambridge Intellectual Propert… (GB)
16 Tamara D. Hopkins Cambridge Intellectual Propert… (GB)
17 Hua Gao Cambridge Intellectual Propert… (GB)
18 Jonathan R. Branch —
19 Hong Xin —
20 Lori Westover — —
21 Gilles C. Bignan — —
22 Brent A. Rupnow —
23 Kristen L. Karlin Baylor College of Medicine (US) —
24 Calla M. Olson Baylor College of Medicine (US) —
25 Thomas F. Westbrook Baylor College of Medicine (US)
26 Joseph P. Vacca Cambridge Intellectual Propert… (GB)
27 Chris M. Wilfong Cambridge Intellectual Propert… (GB)
28 Benjamin Wesley Trotter Cambridge Intellectual Propert… (GB)
29 Douglas C. Saffran Cambridge Intellectual Propert… (GB) —
30 Norbert Bischofberger Cambridge Intellectual Propert… (GB) —

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