K
Kanak Raina
Researcher at Yale University
Publications - 23
Citations - 2922
Kanak Raina is an academic researcher from Yale University. The author has contributed to research in topics: Proteolysis targeting chimera & Ubiquitin ligase. The author has an hindex of 15, co-authored 20 publications receiving 2156 citations.
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Journal ArticleDOI
Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4
Jing Lu,Yimin Qian,Martha Altieri,Hanqing Dong,Jing Wang,Kanak Raina,John Hines,James D. Winkler,Andrew P. Crew,Kevin Coleman,Craig M. Crews +10 more
TL;DR: ARV-825 is designed, a hetero-bifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation ofBRD4 in all BL cell lines tested.
Journal ArticleDOI
PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer.
Kanak Raina,Jing Lu,Yimin Qian,Martha Altieri,Deborah M. Gordon,Ann Marie Rossi,Jing Wang,Xin Chen,Hanqing Dong,Kam W. Siu,James D. Winkler,Andrew P. Crew,Craig M. Crews,Kevin Coleman +13 more
TL;DR: This study proves that ARV-771, a small-molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacy in cellular models of CRPC as compared with BET inhibition.
Journal ArticleDOI
Small-molecule hydrophobic tagging–induced degradation of HaloTag fusion proteins
Taavi K. Neklesa,Hyun Seop Tae,Ashley R. Schneekloth,Michael J. Stulberg,Timothy W. Corson,Timothy W. Corson,Thomas B. Sundberg,Kanak Raina,Scott A. Holley,Craig M. Crews +9 more
TL;DR: In vivo utility of hydrophobic tagging of HaloTag fusion proteins affords small molecule control over any protein of interest, making it an ideal system for validating potential drug targets in disease models.
Journal ArticleDOI
HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins
Dennis L. Buckley,Kanak Raina,Nicole Darricarrère,John Hines,Jeffrey L. Gustafson,Ian Edward David Smith,Afjal Hussain Miah,John D. Harling,Craig M. Crews +8 more
TL;DR: The design of a novel class of PROTACs are reported that incorporate small molecule VHL ligands to successfully degrade HaloTag7 fusion proteins and are useful chemical genetic tools, due to their ability to chemically knock down widely used HaloTag 7 fusion proteins in a general fashion.
Journal ArticleDOI
Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1
Andrew P. Crew,Kanak Raina,Hanqing Dong,Yimin Qian,Jing Wang,Dominico Vigil,Yevgeniy V. Serebrenik,Brian D. Hamman,Alicia Morgan,Caterina Ferraro,Kam W. Siu,Taavi K. Neklesa,James D. Winkler,Kevin Coleman,Craig M. Crews +14 more
TL;DR: This article describes a broadly applicable process for identifying degrader hits based on the serine/threonine kinase TANK-binding kinase 1 (TBK1) and has generalized the key structural elements associated with degradation activities.