David E. Puleo
Yale University
12 Papers
12 Citations
David E. Puleo is an academic researcher from Yale University. The author has contributed to research in topics: Chemistry & Janus kinase. The author has an hindex of 7, co-authored 10 publications. Previous affiliations of David E. Puleo include Novartis & Boston College.
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Papers
Structure-based evaluation of non-nucleoside inhibitors with improved potency and solubility that target HIV reverse transcriptase variants.
Kathleen M. Frey,David E. Puleo,Krasimir A. Spasov,Mariella Bollini,William L. Jorgensen,Karen S. Anderson +5 more
TL;DR: Removal of the 5-Cl substitution of compound 1 on the catechol aryl ring system led to a new analogue compound 2 that maintains greater potency against Y181C and K103N/Y181C variants and better solubility and comparison of the six crystal structures will assist in the understanding of compound binding modes and future optimization of thecatechol diether series.
Toward the Validation of Maternal Embryonic Leucine Zipper Kinase: Discovery, Optimization of Highly Potent and Selective Inhibitors, and Preliminary Biology Insight
B. Barry Touré,John William Giraldes,Troy Smith,Elizabeth R. Sprague,Yaping Wang,Simon Mathieu,Zhuoliang Chen,Yuji Mishina,Yun Feng,Yan Yan-Neale,Subarna Shakya,Dongshu Chen,Matthew J. Meyer,David E. Puleo,J. Tres Brazell,Christopher Sean Straub,David Sage,Kirk Wright,Yanqiu Yuan,Xin Chen,José S. Duca,Sean Kim,Li Tian,Eric J. Martin,Kristen Hurov,Wenlin Shao +25 more
TL;DR: The discovery and optimization of novel MELK inhibitors 8a and 8b are described that recapitulate the cellular effects observed by short hairpin ribonucleic acid (shRNA)-mediated M ELK knockdown in cellular models and a novel fluorine-induced hydrophobic collapse that locked the ligand in its bioactive conformation and led to a 20-fold gain in potency.
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Identification and Characterization of JAK2 Pseudokinase Domain Small Molecule Binders.
David E. Puleo,Kaury Kucera,Henrik Hammaren,Daniela Ungureanu,Ana S. Newton,Olli Silvennoinen,William L. Jorgensen,Joseph Schlessinger +7 more
TL;DR: Development of pseudokinase-selective compounds may offer novel pharmacological opportunities for treating cancers driven by JAK2 V617F and other oncogenic JAK mutants.
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Regulated Induced Proximity Targeting Chimeras (RIPTACs): a Novel Heterobifunctional Small Molecule Therapeutic Strategy for Killing Cancer Cells Selectively
Kanak Raina,C.D. Forbes,Rebecca Stronk,Jonathan P. Rappi,Kyle J. Eastman,Samuel Gerritz,Xinheng Yu,Hao Li,Amit Bhardwaj,Mia E. Forgione,Abigail Hundt,Madeline P. King,Zoe M. Posner,Allison Denny,Andrew McGovern,David E. Puleo,Ethan Garvin,Rebekka Chenard,Nilesh Zaware,James J. Mousseau,Jen Macaluso,Michael Martin,Kyle Bassoli,Kelli Jones,Marco Garcia,K. Howard,Levi M. Smith,Jinshan Chen,Cesar A. De Leon,John Hines,Katherine J. Kayser-Bricker,Craig M. Crews +31 more
TL;DR: In this article , the authors describe a proof-of-concept study using novel heterobifunctional small molecules called Regulated Induced Proximity Targeting Chimeras or RIPTACs, which elicit a stable ternary complex between a target protein selectively expressed in cancer tissue and a pan-expressed protein essential for cell survival.
JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules
Ana S. Newton,Luca Deiana,David E. Puleo,José A. Cisneros,Kara J. Cutrona,Joseph Schlessinger,William L. Jorgensen +6 more
TL;DR: X-ray crystal structures of JAK2 JH2 in complex with NVP-BSK805, filgotinib, and diaminopyrimidine 8 elucidate the binding poses.
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