Zobrazeno 1 - 8 of 8 pro vyhledávání: '"Blair G. Stuart"'
2
Molecular modeling: a search for a calpain inhibitor as a new treatment for cataractogenesis
Autor: James D. Morton, Andrew D. Abell, Roy Bickerstaffe, Blair G. Stuart, Matthew A. Jones, James M. Coxon, D. Quentin McDonald, Steven G. Aitken
Publikováno v: Journal of medicinal chemistry. 54(21)
Studies of 17 analoges of 3 (SJA6017) in an in silico calpain model are reconciled to measured IC(50) values against ovine calpain. The studies validate the potential of the "model" and criteria established for inhibition as a tool to select structur
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a9be34f4d6ea6274e16988e6be5f90ac
https://pubmed.ncbi.nlm.nih.gov/21955158
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3
Molecular modeling, synthesis, and biological evaluation of macrocyclic calpain inhibitors
Autor: Axel T. Neffe, Blair G. Stuart, James D. Morton, Janna M. Mehrtens, James M. Coxon, Andrew D. Abell, Roy Bickerstaffe, Hannah Y.-Y. Lee, Matthew A. Jones, Steven G. Aitken, Stephen B. McNabb, Nathan A. Alexander
Publikováno v: Angewandte Chemie (International ed. in English). 48(8)
The design and elaboration of a series of macrocyclic templates that exhibit a propensity to adopt a beta-strand-like peptide-backbone conformation led to potent and selective inhibitors of calpain 2. Macrocycle 1 retarded calcium-induced opacificati
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e2ee0f1debd297feb2cc9b2dfa873f0e
https://pubmed.ncbi.nlm.nih.gov/19145612
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4
Investigation into the P3 binding domain of m-calpain using photoswitchable diazo- and triazene-dipeptide aldehydes: new anticataract agents
Autor: James M. Coxon, Stephen B. McNabb, Hannah Y.-Y. Lee, Thomas P. Cain, Axel T. Neffe, Blair G. Stuart, James D. Morton, Richard J. Payne, Andrew D. Abell, David Pearson, Matthew A. Jones, Steven G. Aitken
Publikováno v: Journal of medicinal chemistry. 50(12)
The photoswitchable N-terminal diazo and triazene-dipeptide aldehydes 8a−d, 10a,b, and 17a,b present predominantly as the (E)-isomer, which purportedly binds deep in the S3 pocket of calpain. All compounds are potent inhibitors of m-calpain, with 8
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a70ca77e1a4f5c9335432bd6c44d4c12
https://pubmed.ncbi.nlm.nih.gov/17497840
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5
Chrysosporide, a cyclic pentapeptide from a New Zealand sample of the fungus Sepedonium chrysospermum
Autor: Murray H. G. Munro, and Anthony L. J. Cole, John W. Blunt, Grace H. Cao, Blair G. Stuart, Maya I. Mitova
Publikováno v: Journal of natural products. 69(10)
A new cyclic pentapeptide, chrysosporide (1), was isolated from a New Zealand sample of the mycoparasitic fungus Sepedonium chrysospermum by bioactivity-guided fractionation. The planar structure was deduced by detailed spectroscopic analysis, and th
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::034ca3838b59ef7ea9e51f5304c8a7f6
https://pubmed.ncbi.nlm.nih.gov/17067166
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6
Synthesis and evaluation of eight-membered cyclic pseudo-dipeptides
Autor: Sigeru Miyamoto, Axel T. Neffe, Karina M. Brown, Blair G. Stuart, Andrew D. Abell, Janna M. Nikkel, James M. Coxon, Matthew A. Jones
Publikováno v: Peptides. 26(2)
In the course of the development of calpain inhibitors, we report the synthesis of eight-membered cyclic pseudo dipeptides closely related to the known inhibitor SJA6017. The ring closure was effected by metathesis of the diallyl-substituted dipeptid
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99c2e49173e9e6de322d33284cc28b56
https://pubmed.ncbi.nlm.nih.gov/15629536
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