Zobrazeno 1 - 10
of 102
pro vyhledávání: '"R. Scott Lokey"'
Autor:
Yihui Shi, Walter Bray, Alexander J Smith, Wei Zhou, Joy Calaoagan, Chandraiah Lagisetti, Lidia Sambucetti, Phillip Crews, R Scott Lokey, Thomas R Webb
Publikováno v:
PLoS ONE, Vol 15, Iss 5, p e0233672 (2020)
Agents that modulate pre-mRNA splicing are of interest in multiple therapeutic areas, including cancer. We report our recent screening results with the application of a cell-based Triple Exon Skipping Luciferase Reporter (TESLR) using a library that
Externí odkaz:
https://doaj.org/article/aee47b160f21479b987ca0add01dfec1
Autor:
R. Scott Lokey, Cameron Pye
Publikováno v:
Science (New York, N.Y.). 378(6624)
A class of transmembrane proteins helps shuttle large drugs across the cell membrane
Autor:
Christopher van Hoorebeke, Kevin Yang, Samuel J. Mussetter, Grant Koch, Natalie Rutz, R. Scott Lokey, Phillip Crews, Theodore R. Holman
Publikováno v:
ACS omega. 7(47)
Regulation of lipoxygenase (LOX) activity is of great interest due to the involvement of the various LOX isoforms in the inflammatory process and hence many diseases. The bulk of investigations have centered around the discovery and design of inhibit
Autor:
Alexandra C Turmon, Matthew R. Naylor, R. Scott Lokey, Okimasa Okada, Hao-Yuan Wang, Walter M. Bray, Joshua Schwochert, Quinn Edmondson, Satoshi Ono, Jack Taunton, Victoria G. Klein, Justin H Faris
Publikováno v:
ACS Chem Biol
Cordyheptapeptide A is a lipophilic cyclic peptide from the prized Cordyceps fungal genus that shows potent cytotoxicity in multiple cancer cell lines. To better understand the bioactivity and physicochemical properties of cordyheptapeptide A with th
Autor:
Alejandro R. Foley, Glenn L. Millhauser, Amanda Smart, Thomas S. Finn, R. Scott Lokey, Ka Chan, Kevin Yang, Jevgenij A. Raskatov, Graham Roseman
Publikováno v:
Proceedings of the National Academy of Sciences. 117:28625-28631
Evidence linking amyloid beta (Aβ) cellular uptake and toxicity has burgeoned, and mechanisms underlying this association are subjects of active research. Two major, interconnected questions are whether Aβ uptake is aggregation-dependent and whethe
Publikováno v:
Journal of medicinal chemistry, vol 65, iss 6
Despite the notoriously poor membrane permeability of peptides in general, many cyclic peptide natural products show high passive membrane permeability and potently inhibit a variety of “undruggable” intracellular targets. A major impediment to d
Drug‐Like Properties in Macrocycles above MW 1000: Backbone Rigidity versus Side‐Chain Lipophilicity
Autor:
R. Scott Lokey, Victoria G. Klein, Daigo Asano, Quinn Edmondson, Cameron R. Pye, Akihiro Furukawa, Joshua Schwochert, Satoshi Ono, Okimasa Okada, Alexandra C Turmon
Publikováno v:
Angew Chem Int Ed Engl
Large, macrocyclic peptides can achieve surprisingly high membrane permeability, although the properties that govern permeability in this chemical space are only beginning to come into focus. We generated two libraries of cyclic decapeptides with sta
Autor:
Matthew R. Naylor, Okimasa Okada, Chad E. Townsend, Chieko Okumura, R. Scott Lokey, Satoshi Ono, Hsiau-Wei Lee
Publikováno v:
J Chem Inf Model
The chameleonic behavior of cyclosporin A (CsA) was investigated through conformational ensembles employing multicanonical molecular dynamics simulations that could sample the cis and trans isomers of N-methylated amino acids; these assessments were
Publikováno v:
Journal of Medicinal Chemistry
Bifunctional PROTAC degraders belong to "beyond Rule of 5" chemical space, and criteria for predicting their drug-like properties are underdeveloped. PROTAC components are often combined via late-stage amide couplings, due to the reliability and robu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::226920245ada52fb4ef09296381b6379
https://doi.org/10.26434/chemrxiv-2021-47tqn
https://doi.org/10.26434/chemrxiv-2021-47tqn
Autor:
Alejandro Cabrera-Cortez, Annalyse Lalljie, Karen Hug, Hanh Lam, Jessica Sherry, Victoria Auerbuch, R. Scott Lokey, Joanne N. Engel, Tannia Lau, Adam Lentz
Publikováno v:
Antimicrobial Agents and Chemotherapy
Antibiotic-resistant bacteria are an emerging global health threat. New antimicrobials are urgently needed. The injectisome type III secretion system (T3SS), required by dozens of Gram-negative bacteria for virulence but largely absent from nonpathog