Výsledky vyhledávání - "Craig K. Esser"

GPR109a agonists. Part 1: 5-Alkyl and 5-aryl-pyrazole–tetrazoles as agonists of the human orphan G-protein coupled receptor GPR109a

Autor: Andrew K.P. Taggart, Abby Smenton, Steven L. Colletti, Scott Tria, Subharekha Raghavan, Sookhee Chang, M. Gerard Waters, Darby Schmidt, James R. Tata, Thomas O. Schrader, Rui Liang, Jae-Kyu Jung, Craig K. Esser, Jason E. Imbriglio, Kang Cheng, Ester Carballo-Jane

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:2121-2124

5-Alkyl and aryl-pyrazole–tetrazoles have been identified as a new class of selective, small-molecule, agonists of the human G-protein-coupled receptor GPR109a, a high affinity receptor for the HDL-raising drug nicotinic acid.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b238e3d91d801b899d083671c353b8c2
https://doi.org/10.1016/j.bmcl.2009.03.014

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GPR109a agonists. Part 2: Pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a

Autor: Jason E. Imbriglio, Michael Wolff, Andrew K.P. Taggart, Abby Smenton, Subharekha Raghavan, Rui Liang, Scott Tria, Sookhee Chang, Tom G. Holt, Kang Cheng, Ester Carballo-Jane, Craig K. Esser, James R. Tata, Darby Schmidt, Thomas O. Schrader, M. Gerard Waters, Jae-Kyu Jung, Steven L. Colletti

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:4472-4474

5-Alkyl and aryl-pyrazole-acids have been identified as a new class of selective, small-molecule, agonists of the human orphan G-protein-coupled receptor GPR109a, a high affinity receptor for the HDL-raising drug nicotinic acid.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::296e7fc4523266ac3ed35e926e744fda
https://doi.org/10.1016/j.bmcl.2010.06.041

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Synthesis of di- and trisubstituted guanidines on multivalent soluble supports

Autor: Kevin T. Chapman, Ronald M. Kim, Gary S. Kath, Craig K. Esser, Gregory W. King, Jiang Chang, Oyinda Oyelaran, Zenon Konteatis, Brian G. Uhrig

Publikováno v: Tetrahedron Letters. 40:4477-4480

A library of 48 di- and trisubstituted guanidines was synthesized on a soluble, tetravalent support. Support-bound intermediates and cleaved products were isolated in parallel by size exclusion chromatography using a semiautomated system. Products we

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::43d5a0b82520ef6b8a5dd353be44dc62
https://doi.org/10.1016/s0040-4039(99)00812-6

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Solid-phase synthesis of a N-carboxyalkyl tripeptide combinatorial library

Autor: Nathan A. Yates, Kevin T. Chapman, Craig K. Esser, Nancy J. Kevin

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 7:2639-2644

A combinatorial library of N-carboxyalkyl tripeptides was prepared to generate new leads against metalloproteinases. Using the base labile TentaGel S HMB resin, an Fmoc strategy was employed to yield 100 mixtures of 200 compounds each of the general

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1506d8a0684fc30efbf74f0a5d5b0f2a
https://doi.org/10.1016/s0960-894x(97)10049-x

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Stromelysin-1: Three-dimensional structure of the inhibited catalytic domain and of the C-truncated proenzyme

Autor: Alice I. Marcy, Laura Rokosz, William K. Hagmann, Joseph W. Becker, James P. Springer, Melinda G. Axel, Craig K. Esser, Paula M.D. Fitzgerald, Jeffrey D. Hermes, Patricia M. Cameron, Jonathan J. Burbaum

Publikováno v: Protein Science. 4:1966-1976

The proteolytic enzyme stromelysin-1 is a member of the family of matrix metalloproteinases and is believed to play a role in pathological conditions such as arthritis and tumor invasion. Stromelysin-1 is synthesized as a pro-enzyme that is activated

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::992d974e8c092c7e5bed267afbab6bb2
https://doi.org/10.1002/pro.5560041002

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Inhibition of matrix metalloproteinases by N-carboxyalkyl peptides containing extended alkyl residues At P1'

Autor: Ross L. Stein, Richard K. Harrison, Maria Izquierdo-Martin, Lisa M. Niedzwiecki, Ihor E. Kopka, Craig K. Esser, Philippe L. Durette, William K. Hagmann

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 5:539-542

A series of N-carboxyalkyl peptides were prepared to test their inhibitory activity against human stromelysin (MMP-3), collagenase (MMP-1), and gelatinase A (MMP-2). Linear alkyl and ω-aminoalkyl residues were employed as replacements for a phenethy

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7c71dcc55c78c6caf0dcc96cd3cebdfa
https://doi.org/10.1016/0960-894x(95)00079-9

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Inhibition of matrix metalloproteinases by N-carboxyalkyl peptides

Autor: Thomas J. Lanza, Kuo Dw, Craig K. Esser, Kevin T. Chapman, B. Chang, Richard K. Harrison, Lisa M. Niedzwiecki, Philippe L. Durette, Ihor E. Kopka, Maria Izquierdo-Martin

Publikováno v: Journal of Medicinal Chemistry. 36:4293-4301

An extensive study of the requirements for effective binding of N-carboxyalkyl peptides to human stromelysin, collagenase, and to a lesser extent, gelatinase A has been investigated. These efforts afforded inhibitors generally in the 100-400 nM range

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b2499bfe988f356acdc669906878b157
https://doi.org/10.1021/jm00078a019

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The discovery of high affinity agonists of GPR109a with reduced serum shift and improved ADME properties

Autor: Subharekha Raghavan, James R. Tata, Tom G. Holt, Weichun Chen, Andrew K.P. Taggart, Daniel A. DiRocco, Jason E. Imbriglio, Daria M. Marley, Craig K. Esser, M. Gerard Waters, Michael Wolff, Rena Bodner, Steven L. Colletti

Publikováno v: Bioorganicmedicinal chemistry letters. 21(9)

Amino-anthranilic acid derivatives have been identified as a new class of low serum shifted, high affinity full agonists of the human orphan G-protein-coupled receptor GPR109a with improved ADME properties.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb59bbaeedee7ddfe94102bfab92afe5
https://pubmed.ncbi.nlm.nih.gov/21185185

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Substituted 2-aminopyridines as inhibitors of nitric oxide synthases

Publikováno v: Bioorganicmedicinal chemistry letters. 10(17)

A series of substituted 2-aminopyridines was prepared and evaluated as inhibitors of human nitric oxide synthases (NOS). 4,6-Disubstitution enhanced both potency and specificity for the inducible NOS with the most potent compound having an IC50 of 28

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c23c802f83be566f57866065937d3e96
https://pubmed.ncbi.nlm.nih.gov/10987430

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Remote Desymmetrization at Near-Nanometer Group Separation Catalyzed by a Miniaturized Enzyme Mimic

Autor: Karl Hansen, Robert A. Reamer, David Pollard, Scott J. Miller, Jaume Balsells, Chad A. Lewis, Craig K. Esser, Anna Chiu, Michele Kubryk, Jerry A. Murry

Publikováno v: Journal of the American Chemical Society. 128:16454-16455

The chirality of biological receptors often requires syntheses of therapeutic compounds in single enantiomer form. The field of asymmetric catalysis addresses enantioselective synthesis with chiral catalysts. Chemical differentiation of sites within

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4a56831e1a7b57f54d85e9d30bd80cd8
https://doi.org/10.1021/ja067840j

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