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Blake E. Smith
Researcher at Yale University
Publications - 5
Citations - 1279
Blake E. Smith 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 5 publications receiving 812 citations. Previous affiliations of Blake E. Smith include Icahn School of Medicine at Mount Sinai.
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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
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
Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
Blake E. Smith,Stephen Wang,Saul Jaime-Figueroa,Alicia Harbin,Jing Wang,Brian D. Hamman,Craig M. Crews +6 more
TL;DR: It is shown that varying the linker between warhead and E3 ligand and the orientation of the E3ligase allow tuning PROTAC selectivity toward different p38 isoforms, resulting in degradation of p38α or p38δ.
Journal ArticleDOI
Activation of tumor suppressor protein PP2A inhibits KRAS-driven tumor growth
Jaya Sangodkar,Abbey L. Perl,Rita Tohme,Janna Kiselar,David B. Kastrinsky,Nilesh Zaware,Sudeh Izadmehr,Sahar Mazhar,Danica Wiredja,Caitlin M. O’Connor,Divya Hoon,Neil S. Dhawan,Daniela Schlatzer,Shen Yao,Daniel Leonard,Alain C. Borczuk,Giridharan Gokulrangan,Lifu Wang,Elena Svenson,Caroline C. Farrington,Eric Yuan,Rita A. Avelar,Agnes Stachnik,Blake E. Smith,Vickram Gidwani,Heather M. Giannini,Daniel McQuaid,Kimberly McClinch,Zhizhi Wang,Alice C. Levine,Rosalie C. Sears,Edward Y. Chen,Qiaonan Duan,Manish Datt,Shozeb Haider,Shozeb Haider,Avi Ma'ayan,Analisa DiFeo,Neelesh Sharma,Matthew D. Galsky,David L. Brautigan,Yiannis A. Ioannou,Wenqing Xu,Mark R. Chance,Michael Ohlmeyer,Goutham Narla +45 more
TL;DR: It is demonstrated that activation of the tumor suppressor protein phosphatase 2A (PP2A), a negative regulator of multiple oncogenic signaling proteins, is a promising therapeutic approach for the treatment of cancers.
Proceedings ArticleDOI
Abstract 1885: Targeting the FOXO1/KLF6 transcriptional network to modulate response to anti-EGFR based therapy
Jaya Sangodkar,Neil S. Dhawan,Heather Melville,Varan J. Singh,Caroline C. Farrington,Eric Yuan,Huma Q. Rana,Blake E. Smith,Vickram Gidwani,Rachel Okrent,David Burstein,Michael Ohlmeyer,Katerina Politi,Analisa DiFeo,Goutham Narla +14 more
TL;DR: It is demonstrated that an FDA-approved drug, trifluoperazine hydrochloride (TFP), which has been shown to inhibit FOXO1 nuclear export, restores sensitivity to AKT-driven erlotinib-resistance through modulation of the KLF6/FOXO1 signaling cascade in both cell culture and xenograft models.