Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Pat Prodanovich"'
Autor:
Adam J. Stein, Ranjinder S. Sidhu, Lance Goulet, Jilly F. Evans, Jeffrey M. Schaub, Dave Lonergan, Janice Darlington, Gretchen Bain, Nina M. P. Stelzer, Imelda Calderon, Angelina M. Santini, John H. Hutchinson, Pat Prodanovich
Publikováno v:
Molecular Pharmacology. 88:982-992
Autotaxin (ATX) is a secreted enzyme that hydrolyzes lysophosphatidylcholine to lysophosphatidic acid (LPA). LPA is a bioactive phospholipid that regulates diverse biological processes, including cell proliferation, migration, and survival/apoptosis,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a6791e4072e6e2dc892dc384baa160e6
https://doi.org/10.1124/mol.115.100404
https://doi.org/10.1124/mol.115.100404
Autor:
Gretchen Bain, David Lonergan, Jilly F. Evans, Christopher D. King, Martin W. Rowbottom, John H. Hutchinson, Pat Prodanovich, Janice Darlington
Publikováno v:
ACS medicinal chemistry letters. 8(4)
Two series of novel LOXL2 enzyme inhibitors are described: benzylamines substituted with electron withdrawing groups at the para-position and 2-substituted pyridine-4-ylmethanamines. The most potent compound, (2-chloropyridin-4-yl)methanamine 20 (hLO
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56a71d6663f4f9b872f646bf2fcb6880
https://pubmed.ncbi.nlm.nih.gov/28435530
https://pubmed.ncbi.nlm.nih.gov/28435530
Autor:
Charles Chapman, Alex R. Broadhead, Peppi Prasit, Christopher Baccei, Nicholas Simon Stock, Yiwei Li, Jeffrey Roger Roppe, Angelina M. Santini, Dan Lorrain, Lucia Correa, Gretchen Bain, Jasmine Eleanor Zunic, Jeannie Ziff, Christopher D. King, Catherine Lee, Pat Prodanovich, Janice Darlington, Haojing Rong, Jilly F. Evans, Hutchinson John H
Publikováno v:
Journal of Medicinal Chemistry. 54:8013-8029
The potent 5-lipoxygenase-activating protein (FLAP) inhibitor 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid 11cc is described (AM803, now GSK2190915). Building upo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2fbf179f44ba2592906663a125ace36d
https://doi.org/10.1021/jm2008369
https://doi.org/10.1021/jm2008369
Autor:
Christopher Baccei, Jilly F. Evans, Daniel S. Lorrain, Yen Troung, Hutchinson John H, Peppi Prasit, Janice Darlington, Gretchen Bain, Brian Andrew Stearns, Christopher D. King, Catherine Lee, Karin J. Stebbins, Alex R. Broadhead, Angelina M. Santini, Pat Prodanovich
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 338:290-301
The prostaglandin D(2) (PGD(2)) receptor type 2 (DP2) is a G protein-coupled receptor that has been shown to be involved in a variety of allergic diseases, including allergic rhinitis, asthma, and atopic dermatitis. In this study, we describe the pre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6712b393e7da1ebfb64225ffc12e7bfe
https://doi.org/10.1124/jpet.111.180430
https://doi.org/10.1124/jpet.111.180430
Autor:
Timothy Parr, Jeffrey Roger Roppe, Christopher Baccei, Gretchen Bain, Janice Darlington, Nicholas Simon Stock, Charles Chapman, Lucia Correa, Alex R. Broadhead, Hutchinson John H, Daniel S. Lorrain, Brian Andrew Stearns, Christopher D. King, Angelina M. Santini, Catherine Lee, Karin J. Stebbins, Pat Prodanovich, Peppi Prasit, Jilly F. Evans, Deborah Volkots
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1036-1040
Compound 21 (AM432) was identified as a potent and selective antagonist of the DP2 receptor (CRTH2). Modification of a bi-aryl core identified a series of tri-aryl antagonists of which compound 21 proved a viable clinical candidate. AM432 shows excel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c61da34684106e4141e51f6fe39171d6
https://doi.org/10.1016/j.bmcl.2010.12.016
https://doi.org/10.1016/j.bmcl.2010.12.016
Autor:
Ryan C. Clark, Daniel S. Lorrain, Gretchen Bain, Jill Melissa Scott, Hutchinson John H, Alex R. Broadhead, Brian A. Stearns, Nicholas Simon Stock, Patrick Fagan, Yen Pham Truong, Angelina M. Santini, Heather Coate, Christopher Baccei, Christopher D. King, Jilly F. Evans, Catherine Lee, Peppi Prasit, Pat Prodanovich
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4647-4651
The synthesis of a series of tricyclic antagonists for the prostaglandin D(2) receptor DP2 (CRTH2) is disclosed. The activities of the compounds were evaluated in a human DP2 binding assay and a human whole blood eosinophil shape change assay. Potent
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f3c1e4e6de423e3948f39109431fbe4d
https://doi.org/10.1016/j.bmcl.2009.06.085
https://doi.org/10.1016/j.bmcl.2009.06.085
Autor:
Daniel S. Lorrain, Jill Melissa Scott, Angelina M. Santini, Patrick Fagan, Brian Andrew Stearns, Christopher D. King, Catherine Lee, Christopher Baccei, Hutchinson John H, Pat Prodanovich, Jilly F. Evans, Peppi Prasit, Alex R. Broadhead, Gretchen Bain
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(21)
Biphenylacetic acid (5) was identified through a library screen as an inhibitor of the prostaglandin D(2) receptor DP2 (CRTH2). Optimization for potency and pharmacokinetic properties led to a series of selective CRTH2 antagonists. Compounds demonstr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9ff8ab52068f800b3a676abebe5fa4b6
https://pubmed.ncbi.nlm.nih.gov/21958540
https://pubmed.ncbi.nlm.nih.gov/21958540
Autor:
Janice Darlington, Daniel S. Lorrain, Christopher Baccei, Charles Chapman, Hutchinson John H, Christopher D. King, Catherine Lee, Lucia Correa, Gretchen Bain, Pat Prodanovich, Peppi Prasit, Kevin Murray Schaab, Nicholas Simon Stock, Angelina M. Santini, Jilly F. Evans
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(15)
AM643 (compound 6, 3-{3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid) was identified as a potential candidate for formulation as a topical agent for the treatme
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ea4ab92cc9d6890c4b51d62c60d545a6
https://pubmed.ncbi.nlm.nih.gov/20566292
https://pubmed.ncbi.nlm.nih.gov/20566292
Autor:
Nicholas Simon Stock, Angelina M. Santini, Jilly F. Evans, Hutchinson John H, Daniel S. Lorrain, Yiwei Li, Christopher Baccei, Christopher D. King, Catherine Lee, Jasmine Eleanor Zunic, Gretchen Bain, Charles Chapman, Alex R. Broadhead, Peppi Prasit, Pat Prodanovich, Haojing Rong, Janice Darlington
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(1)
A series of potent 5-lipoxygenase-activating protein (FLAP) inhibitors are herein described. SAR studies focused on the discovery of novel alicyclic moieties appended to an indole core to optimize potency, physical properties and off-target activitie
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf952f810739e642c36f04480c561554
https://pubmed.ncbi.nlm.nih.gov/19914828
https://pubmed.ncbi.nlm.nih.gov/19914828
Autor:
Jeannie M. Arruda, Charles Chapman, Dan Lorrain, Peppi Prasit, Lucia Correa, John H. Hutchinson, Pat Prodanovich, Jilly F. Evans, Catherine Lee, Christopher Baccei, Christopher D. King, Janice Darlington, Haojing Rong, Nicholas Simon Stock, Angelina M. Santini, Yiwei Li, Gretchen Bain
Publikováno v:
Journal of medicinal chemistry. 52(19)
The potent and selective 5-lipoxygenase-activating protein leukotriene synthesis inhibitor 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (11j) is described. Lead optim
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d9ffcbc1edef19346c0f376fb1128af
https://pubmed.ncbi.nlm.nih.gov/19739647
https://pubmed.ncbi.nlm.nih.gov/19739647