Multivalent bicyclic peptides are an effective antiviral modality that can potently inhibit SARS-CoV-2

Autor: Katherine U. Gaynor, Marina Vaysburd, Maximilian A. J. Harman, Anna Albecka, Phillip Jeffrey, Paul Beswick, Guido Papa, Liuhong Chen, Donna Mallery, Brian McGuinness, Katerine Van Rietschoten, Steven Stanway, Paul Brear, Aleksei Lulla, Katarzyna Ciazynska, Veronica T. Chang, Jo Sharp, Megan Neary, Helen Box, Jo Herriott, Edyta Kijak, Lee Tatham, Eleanor G. Bentley, Parul Sharma, Adam Kirby, Ximeng Han, James P. Stewart, Andrew Owen, John A. G. Briggs, Marko Hyvönen, Michael J. Skynner, Leo C. James

Publikováno v: Nature Communications, Vol 14, Iss 1, Pp 1-15 (2023)

Abstract COVID-19 has stimulated the rapid development of new antibody and small molecule therapeutics to inhibit SARS-CoV-2 infection. Here we describe a third antiviral modality that combines the drug-like advantages of both. Bicycles are entropica

Externí odkaz: https://doaj.org/article/83eee9acaa674188b99a7694be9c0c15

Development of a LC-MS/MS method for the quantification of toxic payload DM1 cleaved from BT1718 in a Phase I study

Autor: Catherine Gowland, Gareth J. Veal, Philip Berry, Phillip Jeffrey, Marc Pittman, Andrew Niewiarowski, Julie Errington, Lisa Godfrey, Stefan Symeonides, Gavin Bennett

Publikováno v: Gowland, C, Berry, P, Errington, J, Jeffrey, P, Bennett, G, Godfrey, L, Pittman, M, Niewiarowski, A, Symeonides, S N & J Veal, G 2021, ' Development of a LC-MS/MS method for the quantification of toxic payload DM1 cleaved from BT1718 in a Phase I study ', Bioanalysis . https://doi.org/10.4155/bio-2020-0256

Background: BT1718 is a novel bicyclic peptide anticancer drug targeting membrane type I matrix metalloproteinase to release its toxic payload DM1. A LC–MS/MS method was validated to quantify DM1 generated from BT1718 in a Phase I/IIa clinical tria

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::36599a3457cfaf8735151c04f4ff372d
https://pubmed.ncbi.nlm.nih.gov/33496610

how to ORGANIZE EVERYTHING.

Autor: PHILLIP, JEFFREY

Publikováno v: Good Housekeeping. Mar2017, Vol. 264 Issue 3, p47-52B. 5p. 20 Color Photographs.

Human microdose evaluation of the novel EP1 receptor antagonist GSK269984A

Autor: Phillip Jeffrey, Claire Beaumont, Thor Ostenfeld, Maria Beaumont, Jonathan Bullman

Publikováno v: British Journal of Clinical Pharmacology. 74:1033-1044

WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT • The microdose administration of novel drug candidates to humans in early development is currently undergoing evaluation as a cost-efficient approach to the early assessment of pharmacokinetics (PK) before

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e24f6a8ef64332f74b6f8d20744124f7
https://doi.org/10.1111/j.1365-2125.2012.04296.x

SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): Discovery of antagonist SB-568849

Autor: Alison I. Muir, Shelagh Wilson, Christopher N. Johnson, Kim Winborn, Alex J. Stevens, Guillaume J. Hervieu, Peter J. O'Hanlon, Phillip Jeffrey, John H. Bateson, Kevin M. Thewlis, David R. Witty, Geoffrey Stemp

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 16:4865-4871

We report here the discovery of a class of MCH R1 ligands based on a biphenyl carboxamide template. A docked-in model is presented indicating key interactions in the putative binding site of the receptor. Parallel high throughput synthetic techniques

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0fe6fee21c10df4d340450ebe71920d0
https://doi.org/10.1016/j.bmcl.2006.06.056