Zobrazeno 1 - 10
of 31
pro vyhledávání: '"Conor C. G. Scully"'
Autor:
Anthony P. Davenport, Chris de Graaf, Alastair J. H. Brown, Janet J. Maguire, Conor C. G. Scully
Publikováno v:
Nature Reviews Drug Discovery. 19:389-413
Dysregulation of peptide-activated pathways causes a range of diseases, fostering the discovery and clinical development of peptide drugs. Many endogenous peptides activate G protein-coupled receptors (GPCRs) — nearly 50 GPCR peptide drugs have bee
Publikováno v:
Journal of medicinal chemistry. 63(3)
Glucagon-like peptide 1 (GLP-1) and glucagon-like peptide 2 (GLP-2) are proglucagon derived peptides that are released from gut endocrine cells in response to nutrient intake. These molecules are rapidly inactivated by the action of dipeptidyl peptid
Publikováno v:
Journal of the American Chemical Society. 140:8763-8770
Synthetic methods that provide control over macrocycle conformation represent valuable tools for the discovery of bioactive molecules. Incorporation of heterocycles into cyclic peptides may offer a way to stabilize their solution conformations. Herei
Publikováno v:
European Journal of Organic Chemistry. 2017:419-423
1,2-Aziridinyl propargylic amines have been obtained through a zinc-catalyzed multicomponent reaction. This process relies on the dimeric amino aldehyde assembly orchestrating the intramolecular 1,2-alkyne addition to an iminium ion. The resulting pr
Publikováno v:
Organic & Biomolecular Chemistry. 14:10230-10237
As the emerging modality in drug discovery, macrocycles represent topical targets of chemical synthesis. However, the influence of conformational effects on their reactivity has not received enough attention. We demonstrate that the regiochemistry of
Publikováno v:
Chemical Science
Regioselective ring-opening at a flexible N-acyl aziridine enables conformational control of α3β cyclic tetrapeptides through torsional strain.
Among the smallest of the macrocyclic peptides, 12- and 13-membered cyclic tetrapeptides are partic
Among the smallest of the macrocyclic peptides, 12- and 13-membered cyclic tetrapeptides are partic
Autor:
Annie Doucet, Conor C. G. Scully, Eric Marsault, Jennifer L. Hickey, John Mancuso, Andrei K. Yudin, Marie-Claude Tremblay, Serge Zaretsky, Adam P. Treder
Publikováno v:
Chemistry - A European Journal. 21:9249-9255
The first solid-phase parallel synthesis of macrocyclic peptides using three-component coupling driven by aziridine aldehyde dimers is described. The method supports the synthesis of 9- to 18-membered aziridine-containing macrocycles, which are then
Autor:
Jennifer L. Hickey, Rebecca Courtemanche, Joy C. Y. Yu, Jeffrey D. St. Denis, Shinya Adachi, Benjamin H. Rotstein, Benjamin K. W. Chung, Andrei K. Yudin, Serge Zaretsky, Conor C. G. Scully
Publikováno v:
The Journal of Organic Chemistry. 79:9948-9957
The factors determining diastereoselectivity observed in the multicomponent conversion of amino acids, aziridine aldehyde dimers, and isocyanides into chiral piperazinones have been investigated. Amino acid-dependent selectivity for either trans- or
Autor:
Jennifer L. Hickey, Andrew L. Roughton, Dean J. Tantillo, Megan A. St. Denis, Serge Zaretsky, Andrei K. Yudin, Michael W. Lodewyk, Conor C. G. Scully
Publikováno v:
Tetrahedron. 70:7655-7663
A hybrid sequential molecular mechanics and quantum mechanical approach to modeling cyclic peptides has led to an effective method for predicting their 1 H and 13 C NMR chemical shift values. The method was first developed to predict chemical shifts
Autor:
Barbara Colless, Stephanie Chaousis, Timothy A. Hill, Martin J. Stoermer, Andrew J. Lucke, Rink-Jan Lohman, Ligong Liu, Daniel S. Nielsen, Spiros Liras, Roger B. Ruggeri, Charles J. Rotter, Conor C G Scully, David J. Edmonds, Huy N. Hoang, W. Mei Kok, David Price, David P. Fairlie, Paul V. Bernhardt, David A. Griffith, Christina I. Schroeder, David J. Craik
Publikováno v:
ACS Medicinal Chemistry Letters. 5:1148-1151
Development of peptide-based drugs has been severely limited by lack of oral bioavailability with less than a handful of peptides being truly orally bioavailable, mainly cyclic peptides with N-methyl amino acids and few hydrogen bond donors. Here we