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Joshua Schwochert
Joshua Schwochert
Co-founder and CSO, Unnatural Products
Verified email at unnaturalproducts.com
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Year
Probing the physicochemical boundaries of cell permeability and oral bioavailability in lipophilic macrocycles inspired by natural products
AT Bockus, KW Lexa, CR Pye, AS Kalgutkar, JW Gardner, KCR Hund, ...
Journal of Medicinal Chemistry 58 (11), 4581-4589, 2015
1502015
Nonclassical size dependence of permeation defines bounds for passive adsorption of large drug molecules
CR Pye, WM Hewitt, J Schwochert, TD Haddad, CE Townsend, L Etienne, ...
Journal of medicinal chemistry 60 (5), 1665-1672, 2017
1332017
Lipophilic permeability efficiency reconciles the opposing roles of lipophilicity in membrane permeability and aqueous solubility
MR Naylor, AM Ly, MJ Handford, DP Ramos, CR Pye, A Furukawa, ...
Journal of medicinal chemistry 61 (24), 11169-11182, 2018
1302018
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 …
AT Bockus, JA Schwochert, CR Pye, CE Townsend, V Sok, MA Bednarek, ...
Journal of Medicinal Chemistry 58 (18), 7409-7418, 2015
1232015
Passive membrane permeability in cyclic peptomer scaffolds is robust to extensive variation in side chain functionality and backbone geometry
A Furukawa, CE Townsend, J Schwochert, CR Pye, MA Bednarek, ...
Journal of Medicinal Chemistry 59 (20), 9503-9512, 2016
922016
Peptide to peptoid substitutions increase cell permeability in cyclic hexapeptides
J Schwochert, R Turner, M Thang, RF Berkeley, AR Ponkey, ...
Organic letters 17 (12), 2928-2931, 2015
902015
Stereochemistry balances cell permeability and solubility in the naturally derived phepropeptin cyclic peptides
J Schwochert, Y Lao, CR Pye, MR Naylor, PV Desai, ...
ACS Medicinal Chemistry Letters 7 (8), 757-761, 2016
612016
Drug‐like properties in macrocycles above MW 1000: backbone rigidity versus side‐chain lipophilicity
A Furukawa, J Schwochert, CR Pye, D Asano, QD Edmondson, ...
Angewandte Chemie International Edition 59 (48), 21571-21577, 2020
542020
Geometrically diverse lariat peptide scaffolds reveal an untapped chemical space of high membrane permeability
CN Kelly, CE Townsend, AN Jain, MR Naylor, CR Pye, J Schwochert, ...
Journal of the American Chemical Society 143 (2), 705-714, 2020
332020
Using 1 H and 13 C NMR chemical shifts to determine cyclic peptide conformations: a combined molecular dynamics and quantum mechanics approach
QNN Nguyen, J Schwochert, DJ Tantillo, RS Lokey
Physical Chemistry Chemical Physics 20 (20), 14003-14012, 2018
312018
Synthetic cyclic peptomers as type III secretion system inhibitors
H Lam, J Schwochert, Y Lao, T Lau, C Lloyd, J Luu, O Kooner, J Morgan, ...
Antimicrobial agents and chemotherapy 61 (9), 10.1128/aac. 00060-17, 2017
192017
Revisiting N-to-O acyl shift for synthesis of natural product-like cyclic depsipeptides
J Schwochert, C Pye, C Ahlbach, Y Abdollahian, K Farley, B Khunte, ...
Organic letters 16 (23), 6088-6091, 2014
162014
CycLS: Accurate, whole-library sequencing of cyclic peptides using tandem mass spectrometry
C Townsend, A Furukawa, J Schwochert, CR Pye, Q Edmondson, ...
Bioorganic & Medicinal Chemistry 26 (6), 1232-1238, 2018
142018
Biosynthetic products from a nearshore-derived gram-negative bacterium enable reassessment of the kailuin depsipeptides
CM Theodore, N Lorig-Roach, PC Still, TA Johnson, M Drašković, ...
Journal of natural products 78 (3), 441-452, 2015
122015
Identifying the cellular target of cordyheptapeptide A and synthetic derivatives
VG Klein, WM Bray, HY Wang, Q Edmondson, J Schwochert, S Ono, ...
ACS chemical biology 16 (8), 1354-1364, 2021
62021
The passive permeability landscape around geometrically diverse hexa-and heptapeptide macrocycles
C Townsend, E Jason, MR Naylor, CR Pye, JA Schwochert, ...
52020
Amide-to-ester substitutions modify the permeability and ADME properties of natural and synthetic cyclic peptides
M Naylor, A Ly, J Schwochert, P Desai, ICG Valcarcel, J Barrett, ...
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY 252, 2016
12016
DNA-Encoded Macrocyclic Peptide Libraries Enable the Discovery of a Neutral MDM2–p53 Inhibitor
AP Silvestri, Q Zhang, Y Ping, EW Muir, J Zhao, SK Chakka, G Wang, ...
ACS Medicinal Chemistry Letters 14 (6), 820-826, 2023
2023
Abstract B018: The development of macrocyclic peptide Ras inhibitors
K Josephson, A Silvestri, JL Fribourgh, WM Bray, B David, CC Hanna, ...
Molecular Cancer Research 21 (5_Supplement), B018-B018, 2023
2023
Cell-permeable cyclic peptides and uses thereof
PYE Cameron, J Schwochert, S Rubin, A Silvestri
US Patent App. 17/750,110, 2022
2022
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