J
John Hines
Researcher at Yale University
Publications - 46
Citations - 4206
John Hines is an academic researcher from Yale University. The author has contributed to research in topics: Proteolysis targeting chimera & Protein degradation. The author has an hindex of 23, co-authored 39 publications receiving 2990 citations. Previous affiliations of John Hines include St Bartholomew's Hospital & National Health Service.
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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
Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead
Daniel P. Bondeson,Blake E. Smith,George M. Burslem,Alexandru D. Buhimschi,John Hines,Saul Jaime-Figueroa,Jing Wang,Brian D. Hamman,Alexey Ishchenko,Craig M. Crews +9 more
TL;DR: A previously understudied benefit of small molecule proteolysis-targeting chimeras (PROTACs) that recruit E3 ubiquitin ligases to target proteins for their ubiquitination and subsequent proteasome-mediated degradation is reported.
Journal ArticleDOI
Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL
Ashton C. Lai,Momar Toure,Doris Hellerschmied,Jemilat Salami,Saul Jaime-Figueroa,Ko Eunhwa,John Hines,Craig M. Crews +7 more
TL;DR: During the course of their development, it was discovered that the capacity of a PROTAC to induce degradation involves more than just target binding: the identity of the inhibitor warhead and the recruited E3 ligase largely determine the degradation profiles of the compounds.
Journal ArticleDOI
The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study
George M. Burslem,Blake E. Smith,Ashton C. Lai,Saul Jaime-Figueroa,Daniel McQuaid,Daniel P. Bondeson,Momar Toure,Hanqing Dong,Yimin Qian,Jing Wang,Andrew P. Crew,John Hines,Craig M. Crews +12 more
TL;DR: The ability to target receptor tyrosine kinases for degradation using the PROTAC technology is demonstrated and the advantages of this degradation-based approach are outlined.
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.