M
Michael F. Mesleh
Researcher at Broad Institute
Publications - 37
Citations - 2795
Michael F. Mesleh is an academic researcher from Broad Institute. The author has contributed to research in topics: Residual dipolar coupling & Nuclear magnetic resonance spectroscopy. The author has an hindex of 21, co-authored 36 publications receiving 2546 citations. Previous affiliations of Michael F. Mesleh include Cubist Pharmaceuticals & University of Maryland Biotechnology Institute.
Papers
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Journal ArticleDOI
Atropisomeric property of 1-(2,6-difluorobenzyl)-3-[(2R)-amino-2-phenethyl]-5-(2-fluoro-3-methoxyphenyl)-6-methyluracil.
Fabio C. Tucci,Tao Hu,Michael F. Mesleh,Allan Bokser,Eric Allsopp,Timothy D. Gross,Zhiqiang Guo,Yun-Fei Zhu,R. Scott Struthers,Nicholas Ling,Chen Chen +10 more
TL;DR: 1-(2,6-Difluorobenzyl)-3-[(2R)-amino-2-phenethyl]-5-(2-fluoro-3-methoxyphenyl)-6-methyluracil (6) exists as a pair of atropisomers in solution, which was detected by NMR spectroscopy, and separable by HPLC.
Journal ArticleDOI
An efficient chemical synthesis of carboxylate-isostere analogs of daptomycin
TL;DR: The present study describes an esterification protocol to overcome the possible backbone cyclization of the activated side chain carboxylic acid group of either Asp or Glu onto the backbone amide.
Journal ArticleDOI
Multimodal small-molecule screening for human prion protein binders
Andrew G. Reidenbach,Michael F. Mesleh,Dominick Casalena,Sonia M Vallabh,Jayme L. Dahlin,Jayme L. Dahlin,Alison Leed,Alix I. Chan,Dmitry L. Usanov,Jenna B. Yehl,Christopher T. Lemke,Arthur J. Campbell,Rishi N. Shah,Om K. Shrestha,Joshua R. Sacher,V.L. Rangel,Jamie A. Moroco,Murugappan Sathappa,Maria Cristina Nonato,Kong T. Nguyen,S. Kirk Wright,David R. Liu,Florence F. Wagner,Virendar K. Kaushik,Douglas S. Auld,Stuart L. Schreiber,Stuart L. Schreiber,Eric Vallabh Minikel +27 more
TL;DR: The exceptionally low hit rate observed here suggests that PrP is a difficult target for small-molecule binders, whereas orthogonal binder discovery methods could yield high-affinity compounds, non-small-Molecule modalities may offer independent paths forward against prion disease.
Journal ArticleDOI
Determination of the binding mode of thienopyrimidinedione antagonists to the human gonadotropin releasing hormone receptor using structure-activity relationships, site-directed mutagenesis, and homology modeling
Stephen F. Betz,Francisco M. Lio,Yinghong Gao,Greg J. Reinhart,Zhiqiang Guo,Michael F. Mesleh,Yun-Fei Zhu,R. Scott Struthers +7 more
TL;DR: The model is consistent with known SAR and illuminates inconsistencies with previous hypotheses regarding how this series interacts with the receptor.
Posted ContentDOI
Discovery of a first-in-class inhibitor of the PRMT5-substrate adaptor interaction
David C. McKinney,Brian J. McMillan,Matthew J. Ranaghan,Jamie A. Moroco,Merissa Brousseau,Zachary Mullin-Bernstein,Meghan O’Keefe,Patrick McCarren,Michael F. Mesleh,Kathleen M. Mulvaney,Ritu Singh,Besnik Bajrami,Adam Skepner,David E. Timm,Dale Porter,Virendar K. Kaushik,William R. Sellers,William R. Sellers,Alessandra Ianari +18 more
TL;DR: In this paper, small molecule inhibitors of the PRMT5-PBM interaction were evaluated and shown to be competitive with the first-in-class PBM-competitive small molecule, BRD0639.