A
Alexandru D. Buhimschi
Researcher at Yale University
Publications - 7
Citations - 803
Alexandru D. Buhimschi is an academic researcher from Yale University. The author has contributed to research in topics: Protein degradation & Ubiquitin ligase. The author has an hindex of 4, co-authored 7 publications receiving 487 citations. Previous affiliations of Alexandru D. Buhimschi include Northwestern University.
Papers
More filters
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
Targeting the C481S Ibrutinib-Resistance Mutation in Bruton’s Tyrosine Kinase Using PROTAC-Mediated Degradation
Alexandru D. Buhimschi,Haley A Armstrong,Momar Toure,Saul Jaime-Figueroa,Timothy L. Chen,Amy Lehman,Jennifer A. Woyach,Amy J. Johnson,John C. Byrd,Craig M. Crews +9 more
TL;DR: A PROteolysis TArgeting Chimera (PROTAC) that induces degradation of both wild-type and C481S mutant BTK, and a lead PROTAC, MT-802, from several candidates on the basis of its potency to induce BTK knockdown.
Journal ArticleDOI
Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties.
TL;DR: A new series of Proteolysis Targeting Chimeras (PROTACs) targeting Bruton's Tyrosine Kinase (BTK) was synthesized with structural modifications to the linker and E3-recruiting ligand, resulting in an equally potent PROTAC, SJF620, with a significantly better pharmacokinetic profile than MT802.
Journal ArticleDOI
Psoralen Derivatives with Enhanced Potency
Alexandru D. Buhimschi,David M. Gooden,Hongwu Jing,Diane Renee Fels,Katherine S. Hansen,Wayne F. Beyer,Mark W. Dewhirst,Harold Walder,Francis P. Gasparro +8 more
TL;DR: A rational approach is provided to guide efforts toward further optimizing psoralens to fully capitalize on this drug class’ therapeutic potential and shed light on several opportunities to study currently underappreciated aspects of psoralen's mechanism.