Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Stacey M, Southall"'
Autor:
Stacey M. Southall, Joydeep Banerjee, Jason Brown, Kristina Butkovic, Andrew D. Cansfield, Julie E. Cansfield, Miles S. Congreve, Gabriella Cseke, Francesca Deflorian, Martina Petrovic Hunjadi, Antun Hutinec, Trinadh Kumar Inturi, Renata Rupcic, Gordon Saxty, Stephen P. Watson
Publikováno v:
ACS Medicinal Chemistry Letters. 13:1776-1782
The diastereomeric macrocyclic calcitonin generelated peptide (CGRP) antagonists HTL0029881 (3) and HTL0029882 (4), in which the stereochemistry of a spiro center is reversed, surprisingly demonstrate comparable potency. X-ray crystallographic charac
Autor:
Andrew D. Cansfield, Mark A. Ator, Joydeep Banerjee, Michael Bestwick, Andrea Bortolato, Giles A. Brown, Jason Brown, Kristina Butkovic, Julie E. Cansfield, John A. Christopher, Miles Congreve, Gabriella Cseke, Francesca Deflorian, Benjamin Dugan, Martina Petrovic Hunjadi, Antun Hutinec, Trinadh Kumar Inturi, Goran Landek, Jonathan Mason, Alistair O’Brien, Gregory R. Ott, Renata Rupcic, Gordon Saxty, Stacey M. Southall, Rahela Zadravec, Stephen P. Watson
Publikováno v:
ACS Chemical Neuroscience. 13:751-765
A series of macrocyclic calcitonin gene-related peptide (CGRP) receptor antagonists identified using structure-based design principles, exemplified by HTL0028016 (1) and HTL0028125 (2), is described. Structural characterization by X-ray crystallograp
Autor:
Sarah J, Bucknell, Mark A, Ator, Alastair J H, Brown, Jason, Brown, Andrew D, Cansfield, Julie E, Cansfield, John A, Christopher, Miles, Congreve, Gabriella, Cseke, Francesca, Deflorian, Christopher R, Jones, Jonathan S, Mason, M Alistair, O'Brien, Gregory R, Ott, Mark, Pickworth, Stacey M, Southall
Publikováno v:
Journal of medicinal chemistry. 63(14)
Structure-based drug design enabled the discovery of
Autor:
Robert M. Cooke, Nathan Robertson, Markus Koglin, Harini Krishnamurthy, Ali Jazayeri, Asma H. Baig, Andrea Bortolato, Malcolm Peter Weir, A.S. Dore, Stacey M. Southall, Fiona H. Marshall, Iryna Teobald, Alastair J. H. Brown, Daniel Lamb, James C. Errey, Stephen P. Andrews
Publikováno v:
Nature. 533:274-277
Glucagon is a 29-amino-acid peptide released from the α-cells of the islet of Langerhans, which has a key role in glucose homeostasis. Glucagon action is transduced by the class B G-protein-coupled glucagon receptor (GCGR), which is located on liver
Autor:
Fiona H. Marshall, Juan Carlos Mobarec, Susan H. Brown, James C. Errey, Stephen P. Andrews, Jonathan S. Mason, Malcolm Peter Weir, Kelly N. Steele, Ali Jazayeri, Robert M. Cooke, A. O'Brien, Charlotte Fieldhouse, Iryna Teobald, Alastair J. H. Brown, Brown Giles Albert, Bortolato Andrea, John A. Christopher, Asma H. Baig, Chris de Graaf, Stacey M. Southall, Steve P. Watson, Krzysztof Okrasa, Miles Congreve
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:126611
A series of novel allosteric antagonists of the GLP-1 receptor (GLP-1R), exemplified by HTL26119, are described. SBDD approaches were employed to identify HTL26119, exploiting structural understanding of the allosteric binding site of the closely rel
Publikováno v:
Nucleic Acids Research
The delivery of site-specific post-translational modifications to histones generates an epigenetic regulatory network that directs fundamental DNA-mediated processes and governs key stages in development. Methylation of histone H4 lysine-20 has been
Publikováno v:
Journal of Biological Chemistry. 285:32967-32976
Histone modification is well established as a fundamental mechanism driving the regulation of transcription, replication, and DNA repair through the control of chromatin structure. Likewise, it is apparent that incorrect targeting of histone modifica
Publikováno v:
Molecular Cell. 33(2):181-191
The mixed-lineage leukemia protein MLL1 is a transcriptional regulator with an essential role in early development and hematopoiesis. The biological function of MLL1 is mediated by the histone H3K4 methyltransferase activity of the carboxyl-terminal
Publikováno v:
Journal of Biological Chemistry. 281:30650-30659
A water-soluble aldose sugar dehydrogenase (Asd) has been purified for the first time from Escherichia coli. The enzyme is able to act upon a broad range of aldose sugars, encompassing hexoses, pentoses, disaccharides, and trisaccharides, and is able
Publikováno v:
Acta Crystallographica Section F: Structural Biology and Crystallization Communications
Three mutants of the soluble quinoprotein glucose dehydrogenase and two homologues from E. coli and S. coelicolor have been crystallized using an efficient microseeding method.
The soluble quinoprotein glucose dehydrogenase oxidizes glucose, mal
The soluble quinoprotein glucose dehydrogenase oxidizes glucose, mal