Výsledky vyhledávání - "Julia M. Ayala"

Design, synthesis, and structure–activity relationship of novel CCR2 antagonists

Autor: Richard Jiao, Pasquale P. Vicario, Gabor Butora, Shankaran Kothandaraman, Stephen D. Goble, Mary Struthers, Gregori J. Morriello, Julie A. DeMartino, Sander G. Mills, Malcolm MacCoss, Julia M. Ayala, Margaret A. Cascieri, Karla L. Donnely, Changyou Zhou, Lihu Yang, Alexander Pasternak

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:1830-1834

A series of novel 1-aminocyclopentyl-3-carboxyamides incorporating substituted tetrahydropyran moieties have been synthesized and subsequently evaluated for their antagonistic activity against the human CCR2 receptor. Among them analog 59 was found t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::37cf3150520d0f4c125edd804b8e5959
https://doi.org/10.1016/j.bmcl.2008.12.050

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Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists

Autor: Julie A. DeMartino, Stephen D. Goble, Mary Struthers, Jerry Di Salvo, Pasquale P. Vicario, Alexander Pasternak, Julia M. Ayala, Sander G. Mills, Lihu Yang

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 18:994-998

This report describes replacement of the 4-(4-fluorophenyl)piperidine moiety in our CCR2 antagonists with 4-heteroaryl piperidine and 4-(carboxyphenyl)-piperidine subunits. Some of the resulting analogs retained potency in our CCR2 binding assay and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::04e9718f074913bae396e0a7019b2df3
https://doi.org/10.1016/j.bmcl.2007.12.029

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Diaryl substituted pyrazoles as potent CCR2 receptor antagonists

Autor: Pasquale P. Vicario, Thomas Wisniewski, Sima R. Patel, Julia M. Ayala, Julie A. DeMartino, Anthony B. Pinkerton, Jean-Michel Vernier, Hutchinson John H, Dehua Huang, Rowena V. Cube, Mary Struthers

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 17:807-813

We have identified and synthesized a series of diaryl substituted pyrazoles as potent antagonists of the chemokine receptor subtype 2. Structure-activity relationship studies directed toward improving the potency led to the discovery of 23 (IC50 = 6

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17d94f6567902ebf249c5e53a93de2d0
https://doi.org/10.1016/j.bmcl.2006.10.060

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Novel, Orally Bioavailable γ-Aminoamide CC Chemokine Receptor 2 (CCR2) Antagonists

Autor: Alexander Pasternak, Pasquale P. Vicario, Margaret A. Cascierri, Sander G. Mills, Julia M. Ayala, Dominick Marino, Malcolm MacCoss, Lihu Yang, William H. Parsons

Publikováno v: Journal of Medicinal Chemistry. 49:4801-4804

Through modification of a screening hit we have discovered a structurally distinct new lead, (2S)-N-[3,5-bis(trifluoromethyl)benzyl]-2-(4-fluorophenyl)-4-(4-phenylpiperidin-1-yl)butanamide (11), which has subsequently served as the departure point fo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::69162166c1bb2771b74c24bf80ad8fe4
https://doi.org/10.1021/jm060439n

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Leukotriene B4Strongly Increases Monocyte Chemoattractant Protein-1 in Human Monocytes

Autor: Samuel D. Wright, Frederick Wong, Julia M. Ayala, Jilly F. Evans, Annie Zhao, Feroze Ujjainwalla, Marty S. Springer, Li Huang, Mary Struthers, Jisong Cui

Publikováno v: Arteriosclerosis, Thrombosis, and Vascular Biology. 24:1783-1788

Objective—Leukotriene B4(LTB4), a product of the 5-lipoxygenase (5-LO) pathway of arachidonic acid metabolism, has been implicated in atherosclerosis. However, the molecular mechanisms for the atherogenic effect of LTB4are not well understood. This

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b47bf5d874fd97343f1f436f5e7ff558
https://doi.org/10.1161/01.atv.0000140063.06341.09

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Serum-induced monocyte differentiation and monocyte chemotaxis are regulated by the p38 MAP kinase signal transduction pathway

Autor: Dave A. Claremon, William A. Hanlon, Nigel J. Liverton, Stephen J. O'Keefe, Shefali Goyal, Julia M. Ayala

Publikováno v: Journal of Leukocyte Biology. 67:869-875

Regulation by the p38 mitogen-acti- vated protein (MAP) kinase signaling pathway of monocytic inflammatory functions was evaluated using L-790,070, a potent and selective inhibitor of p38 MAP kinase. Three major functions of monocytes were investigat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9492db8ab1d2f5ece40d81bb01e88bc6
https://doi.org/10.1002/jlb.67.6.869

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Immunohistochemical localization of types 1 and 2 5α-reductase in human scalp

Autor: B. Azzolina, Julia M. Ayala, B. Chang, M. Einstein, Diane Thiboutot, Richard A. Mumford, John G. Flanagan, Georgianna Harris, Irwin I. Singer, Ellen K. Bayne, David A. Whiting

Publikováno v: British Journal of Dermatology. 141:481-491

The predominant form of 5alpha-reductase (5aR) in human scalp is 5aR1. None the less, clinical studies have shown that finasteride, a selective inhibitor of 5aR2, decreases scalp dihydrotestosterone and promotes hair growth in men with androgenetic a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b3e124a32c3a3e63e0f0f5ab5c2604c7
https://doi.org/10.1046/j.1365-2133.1999.03042.x

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Activation of the Native 45-kDa Precursor Form of Interleukin-1-converting Enzyme

Autor: Julia M. Ayala, Ting-Ting Yamin, Douglas K. Miller

Publikováno v: Journal of Biological Chemistry. 271:13273-13282

Active interleukin-1beta-converting enzyme (ICE) is composed of 20- and 10-kDa polypeptides (p20 and p10) derived from the processing of a cytosolic 45-kDa precursor protein (p45). The cleavage and activation of the native p45 ICE precursor have been

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a75847d8440c0e30c8563ccb1c58e494
https://doi.org/10.1074/jbc.271.22.13273

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VDIPEN, a metalloproteinase-generated neoepitope, is induced and immunolocalized in articular cartilage during inflammatory arthritis

Autor: Susan Donatelli, Douglas W. Kawka, Richard A. Mumford, Hollis R. Williams, Jeffrey R. Weidner, Michael W. Lark, Julia M. Ayala, Irwin I. Singer, Ellen K. Bayne, Tibor T. Glant

Publikováno v: Journal of Clinical Investigation. 95:2178-2186

The destruction of articular cartilage in immune inflammatory arthritic disease involves the proteolytic degradation of its extracellular matrix. The role of activated matrix metalloproteinases (MMPs) in the chondrodestructive process was studied by

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7c0b58e7525aefa6ad2bc68aa1097220
https://doi.org/10.1172/jci117907

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Cell-mediated Catabolism of Aggrecan

Autor: Michael W. Lark, Hollis R. Williams, John T. Gordy, Steven S. Carlson, Carl R. Flannery, Jeffrey R. Weidner, James H. Kimura, Richard A. Mumford, John D. Sandy, Julia M. Ayala, Mineo Iwata

Publikováno v: Journal of Biological Chemistry. 270:2550-2556

A rat chondrosarcoma cell line and primary bovine chondrocytes have been used to study cell-mediated aggrecan catabolism. Addition of 1 microM retinoic acid to chondrosarcoma cultures resulted in aggrecan proteolysis with the release of greater than

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9dbd0d5ceffd1e1f506a965aa2fb50c4
https://doi.org/10.1074/jbc.270.6.2550

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