Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Alan V. Wallace"'
Autor:
Stephen Connolly, Antonio Mete, Glen Andrews, Nigel Gensmantel, Gunilla Andersson, Matt D. Kroeger, Andrew S. Arvai, Peter Hamley, Stephen A. St-Gallay, Brian R. Crane, Elizabeth D. Getzoff, Alan V. Wallace, Anders Åberg, Robin J. Rosenfeld, Philip Mallinder, David J. Nicholls, John A. Tainer, Dennis J. Stuehr, Elsa D. Garcin, Tinker Alan, David Cheshire
Publikováno v:
Nature chemical biology
Nitric oxide synthase (NOS) enzymes synthesize nitric oxide, a signal for vasodilatation and neurotransmission at low concentrations and a defensive cytotoxin at higher concentrations. The high active site conservation among all three NOS isozymes hi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::26e76851585f29d2b5622fd30eb7ee73
http://europepmc.org/articles/PMC2868503
http://europepmc.org/articles/PMC2868503
Autor:
David Cox, Alan V. Wallace, Anthony Ronald Cook, Anders Åberg, and Alan C. Tinker, John A. Tainer, David Cheshire, Haydn Beaton, Phil Mallinder, Ian Millichip, David J. Nicholls, Stephen A. St-Gallay, Sally L. Cooper, Robin J. Rosenfeld, Stephen Connolly, Andrew S. Arvai, Peter Hamley
Publikováno v:
Journal of Medicinal Chemistry. 47:3320-3323
4-Methylaminopyridine (4-MAP) (5) is a potent but nonselective nitric oxide synthase (NOS) inhibitor. While simple N-methylation in this series results in poor activity, more elaborate N-substitution such as with 4-piperidine carbamate or amide resul
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bbfd3e7f451affb3e932af18fb27fc41
https://doi.org/10.1021/jm031035n
https://doi.org/10.1021/jm031035n
Autor:
Rupert P. Austin, Karl Edman, Hitesh J. Sanganee, Raj Beri, Peter Cage, Christopher A. Luckhurst, Jason Breed, Ian Millichip, Victor I. C. Oreffo, Bob Thong, Antonio Mete, Kamaldeep K. Chohan, Steve T. Harper, Alan V. Wallace, Elizabeth Kinchin, Lisa Wissler, Judit E. Debreczeni, Andrew Mather, Anna-Karin Tidén, Mark Furber, Rhonan Ford, Ray Hutchinson, Simon Barber, Philip Gardiner, Linda Stein
Publikováno v:
Journal of medicinal chemistry. 57(6)
A lead generation and optimization program delivered the highly selective and potent CatC inhibitor 10 as an in vivo tool compound and potential development candidate. Structural studies were undertaken to generate SAR understanding.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eda9c1a5aff14abe1c0e7c7ba7f3ddb3
https://pubmed.ncbi.nlm.nih.gov/24592859
https://pubmed.ncbi.nlm.nih.gov/24592859
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:1023-1026
3-Phenyl-3.4-dihydro-1-isoquinolinamine is a weak inhibitor of iNOS and nNOS. Structural variation of 5a results in inhibitors with a range of potency and selectivity for the NOS enzymes, including a potent and very selective iNOS inhibitor 5j.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99a1b021ba648f38714dddd7c1e2b2aa
https://doi.org/10.1016/s0960-894x(01)00119-6
https://doi.org/10.1016/s0960-894x(01)00119-6
Publikováno v:
Bioorganic & Medicinal Chemistry. 7:1891-1896
Reperfusion of the ischaemic myocardium leads to intracellular calcium overload followed by mitochondrial dysfunction, resulting in insufficient energy supply and ultimately myocardial necrosis. Ruthenium red (RR), a potent mitochondrial calcium upta
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9db5c760ac5a1c9467036831517fa252
https://doi.org/10.1016/s0968-0896(99)00166-2
https://doi.org/10.1016/s0968-0896(99)00166-2
Autor:
Stephen Connolly, Nigel Gensmantel, Peter Hamley, Richard P. Harrison, Paul Hartopp, Nigel Boughton-Smith, Timothy Nicholas Birkinshaw, Antonio Mete, Haydn Beaton, Sally L. Cooper, Austen Pimm, David Cheshire, Gunilla Andersson, Alan V. Wallace, Anders Åberg, Paul D. Leeson, John Dixon, David Cox, Timothy Jon Luker, Helena Käck, Ian Millichip, Steve St-Gallay, David J. Nicholls, Anne Cooper, Glen Andrews, Tony R. Cook
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(8)
By careful analysis of experimental X-ray ligand crystallographic protein data across several inhibitor series we have discovered a novel, potent and selective series of iNOS inhibitors exemplified by compound 8.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::899f9ebccc5f546ea9baf51a82b87d1e
https://pubmed.ncbi.nlm.nih.gov/21398123
https://pubmed.ncbi.nlm.nih.gov/21398123
Publikováno v:
ChemInform. 32
3-Phenyl-3,4-dihydro-1-isoquinolinamine is a weak inhibitor of iNOS and nNOS. Structural variation of 5a results in inhibitors with a range of potency and selectivity for the NOS enzymes, including a potent and very selective iNOS inhibitor 5j.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::416c875f93db2c455d8d3150c62aba2b
https://doi.org/10.1002/chin.200132147
https://doi.org/10.1002/chin.200132147
Autor:
Anant M. Ghelani, Alan V. Wallace, Nigel Boughton-Smith, Peter Hamley, Tinker Alan, Haydn Beaton, David J. Nicholls
Publikováno v:
ChemInform. 32
5-Substituted 7-amino-4,5-tetrahydrothieno[2,3-c]pyridines and 6-substituted 4-amino-6,7-dihydrothieno[3,2-c]pyridines were shown to be exceptionally potent inhibitors of inducible and neuronal nitric oxide synthase. Selectivity and potency could be
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::679edcf99439d10a1b14d445a5c7f14b
https://doi.org/10.1002/chin.200132150
https://doi.org/10.1002/chin.200132150
Publikováno v:
Journal of biomolecular screening. 14(3)
Inducible nitric oxide synthase (iNOS) is active as a homodimer. A cell-based assay suitable for high-throughput screening (HTS) was generated to identify inhibitors of iNOS dimerization using the InteraX enzyme complementation technology of Applied
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::51080c794696d9d7754f2967735a1de2
https://pubmed.ncbi.nlm.nih.gov/19211775
https://pubmed.ncbi.nlm.nih.gov/19211775
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(4)
A Hit-to-Lead optimisation programme was carried out on a high throughput screening hit, the thiazolopyrimidine 1, resulting in the discovery of the potent, orally bioavailable CXCR2 antagonist 29.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c133ed676a65ba42091ce1f91c5d01b1
https://pubmed.ncbi.nlm.nih.gov/16297626
https://pubmed.ncbi.nlm.nih.gov/16297626