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Author Details
Full Name
R Scott Lokey
Affiliation
University of California Santa Cruz
ORCID
Career Start Year
2000
Papers
80
H Index
33
Expertise
CM4AI Collaborator
Nevan J Krogan (CM4AI)
PMID
Paper Title
Journal Title
Published Year
37815526
High-Content Image-Based Screening and Deep Learning for the Detection of Anti-Inflammatory Drug Leads.
Chembiochem
2024
36932083
Amide-to-ester substitution as a stable alternative to N-methylation for increasing membrane permeability in cyclic peptides.
Nat Commun
2023
37426286
DNA-Compatible Conditions for the Formation of <i>N</i>-Methyl Peptide Bonds.
ACS Omega
2023
35275623
A New Amino Acid for Improving Permeability and Solubility in Macrocyclic Peptides through Side Chain-to-Backbone Hydrogen Bonding.
J Med Chem
2022
36480613
Getting bifunctional molecules into cells.
Science
2022
36467910
Reevaluation of a Bicyclic Pyrazoline as a Selective 15-Lipoxygenase V-Type Activator Possessing Fatty Acid Specificity.
ACS Omega
2022
36449542
High-throughput functional annotation of natural products by integrated activity profiling.
Proc Natl Acad Sci U S A
2022
33381960
Geometrically Diverse Lariat Peptide Scaffolds Reveal an Untapped Chemical Space of High Membrane Permeability.
J Am Chem Soc
2021
33875435
Developing Cyclic Peptomers as Broad-Spectrum Type III Secretion System Inhibitors in Gram-Negative Bacteria.
Antimicrob Agents Chemother
2021
34881891
Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity.
J Med Chem
2021
34672629
Cyclosporin A: Conformational Complexity and Chameleonicity.
J Chem Inf Model
2021
34251165
Identifying the Cellular Target of Cordyheptapeptide A and Synthetic Derivatives.
ACS Chem Biol
2021
32789999
Drug-Like Properties in Macrocycles above MW 1000: Backbone Rigidity versus Side-Chain Lipophilicity.
Angew Chem Int Ed Engl
2020
33139554
Evidence for aggregation-independent, PrP<sup>C</sup>-mediated Aβ cellular internalization.
Proc Natl Acad Sci U S A
2020
32939229
Understanding and Improving the Membrane Permeability of VH032-Based PROTACs.
ACS Med Chem Lett
2020
32902550
Connecting the conformational behavior of cyclic octadepsipeptides with their ionophoric property and membrane permeability.
Org Biomol Chem
2020
30657701
Macrophage Cytological Profiling and Anti-Inflammatory Drug Discovery.
Assay Drug Dev Technol
2019
31042375
Conformation and Permeability: Cyclic Hexapeptide Diastereomers.
J Chem Inf Model
2019
29459147
CycLS: Accurate, whole-library sequencing of cyclic peptides using tandem mass spectrometry.
Bioorg Med Chem
2018
34158674
The Bioactive Lipid (S)-Sebastenoic Acid Impacts Motility and Dispersion in <i>Vibrio cholerae</i>.
Can J Chem
2018
30025185
Genome-Based Identification of a Plant-Associated Marine Bacterium as a Rich Natural Product Source.
Angew Chem Int Ed Engl
2018
30395703
Lipophilic Permeability Efficiency Reconciles the Opposing Roles of Lipophilicity in Membrane Permeability and Aqueous Solubility.
J Med Chem
2018
29744489
Using <sup>1</sup>H and <sup>13</sup>C NMR chemical shifts to determine cyclic peptide conformations: a combined molecular dynamics and quantum mechanics approach.
Phys Chem Chem Phys
2018
28059508
Nonclassical Size Dependence of Permeation Defines Bounds for Passive Adsorption of Large Drug Molecules.
J Med Chem
2017
28461474
Retrospective analysis of natural products provides insights for future discovery trends.
Proc Natl Acad Sci U S A
2017
28159754
Reliance of <i>Wolbachia</i> on High Rates of Host Proteolysis Revealed by a Genome-Wide RNAi Screen of <i>Drosophila</i> Cells.
Genetics
2017
28128950
Naphthablins B and C, Meroterpenoids Identified from the Marine Sediment-Derived Streptomyces sp. CP26-58 Using HeLa Cell-Based Cytological Profiling.
J Nat Prod
2017
29045152
Discovery of Potent and Orally Bioavailable Macrocyclic Peptide-Peptoid Hybrid CXCR7 Modulators.
J Med Chem
2017
28652236
Synthetic Cyclic Peptomers as Type III Secretion System Inhibitors.
Antimicrob Agents Chemother
2017
28570865
Cyclic peptide natural products chart the frontier of oral bioavailability in the pursuit of undruggable targets.
Curr Opin Chem Biol
2017
28710331
Reply to Skinnider and Magarvey: Rates of novel natural product discovery remain high.
Proc Natl Acad Sci U S A
2017
26845289
A Strategy for Direct Chemical Activation of the Retinoblastoma Protein.
ACS Chem Biol
2016
27587783
Systematic Mapping of Chemical-Genetic Interactions in Saccharomyces cerevisiae.
Cold Spring Harb Protoc
2016
27587777
A High-Throughput Yeast Halo Assay for Bioactive Compounds.
Cold Spring Harb Protoc
2016
27690434
Passive Membrane Permeability in Cyclic Peptomer Scaffolds Is Robust to Extensive Variation in Side Chain Functionality and Backbone Geometry.
J Med Chem
2016
27563399
Stereochemistry Balances Cell Permeability and Solubility in the Naturally Derived Phepropeptin Cyclic Peptides.
ACS Med Chem Lett
2016
25517352
Cell-permeable cyclic peptides from synthetic libraries inspired by natural products.
J Am Chem Soc
2015
26292657
Phenotype-Guided Natural Products Discovery Using Cytological Profiling.
J Nat Prod
2015
26308180
Going Out on a Limb: Delineating The Effects of β-Branching, N-Methylation, and Side Chain Size on the Passive Permeability, Solubility, and Flexibility of Sanguinamide A Analogues.
J Med Chem
2015
26046483
Peptide to Peptoid Substitutions Increase Cell Permeability in Cyclic Hexapeptides.
Org Lett
2015
26067057
Beyond cyclosporine A: conformation-dependent passive membrane permeabilities of cyclic peptide natural products.
Future Med Chem
2015
25950816
Probing the Physicochemical Boundaries of Cell Permeability and Oral Bioavailability in Lipophilic Macrocycles Inspired by Natural Products.
J Med Chem
2015
25699470
Biosynthetic products from a nearshore-derived gram-negative bacterium enable reassessment of the kailuin depsipeptides.
J Nat Prod
2015
25412436
Revisiting N-to-O acyl shift for synthesis of natural product-like cyclic depsipeptides.
Org Lett
2014
23578022
Designing molecules to cross biological membranes.
Curr Top Med Chem
2013
24063667
Selective, on-resin N-methylation of peptide N-trifluoroacetamides.
Org Lett
2013
24056581
Large-scale cytological profiling for functional analysis of bioactive compounds.
Mol Biosyst
2013
23771823
A high-throughput splicing assay identifies new classes of inhibitors of human and yeast spliceosomes.
J Biomol Screen
2013
23438757
"Function-first" lead discovery: mode of action profiling of natural product libraries using image-based screening.
Chem Biol
2013
23578026
Form and function in cyclic peptide natural products: a pharmacokinetic perspective.
Curr Top Med Chem
2013
1 - 50 of 80
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Co-authored papers
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Laura Kapitzky
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Joanne N Engel
University of California san francisco
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Jessica Sherry
University of California San Francisco
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David P Toczyski
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Nevan J Krogan (CM4AI)
University of California San Francisco
Co-authored papers
1
Theresa J Berens
University of California san francisco
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Kenji L Kurita
Small Molecule Pharmaceutical Sciences, Genentech Inc.
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Jack Taunton
University of California san francisco
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Stephen J Elledge
Howard Hughes Medical Institute, Brigham and Women's Hospital, Harvard Medical School
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