Výsledky vyhledávání - "D I, Stirling"

Apremilast, a cAMP phosphodiesterase-4 inhibitor, demonstrates anti-inflammatory activity in vitro and in a model of psoriasis

Autor: Lori Capone, Loveland Ma, Cheung Yf, Lei Wu, Anita Gandhi, Peter H. Schafer, Justin B. Bartlett, Amos Gilhar, Mary Adams, George S. Baillie, D. I. Stirling, G. W. Muller, Anastasia Parton, Houslay, Man Hw

Publikováno v: British Journal of Pharmacology. 159:842-855

Background and purpose: Apremilast is an orally administered phosphodiesterase-4 inhibitor, currently in phase 2 clinical studies of psoriasis and other chronic inflammatory diseases. The inhibitory effects of apremilast on pro-inflammatory responses

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b99b2bd538e86f4b148f758f94ec804b
https://doi.org/10.1111/j.1476-5381.2009.00559.x

Zobrazit plný text záznamu

Discovery of (S)-N-{2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl}acetamide (Apremilast), a Potent and Orally Active Phosphodiesterase 4 and Tumor Necrosis Factor-α Inhibitor

Autor: Peter H. Schafer, Rebecca T. Patterson, D. I. Stirling, Michael A. Shirley, Kate Blease, Lu Min Wong, George W. Muller, Laura G. Corral, Heather Raymon, Darius Babusis, Hon-Wah Man, Yang Tang, Roger Shen-Chu Chen, Jim Leisten

Publikováno v: Journal of Medicinal Chemistry. 52:1522-1524

In this communication, we report the discovery of 1S (apremilast), a novel potent and orally active phosphodiesterase 4 (PDE4) and tumor necrosis factor-alpha inhibitor. The optimization of previously reported 3-(1,3-dioxo-1,3-dihydroisoindol-2-yl)-3

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d4d477da9bf927b28bf8be6aacbf81a7
https://doi.org/10.1021/jm900210d

Zobrazit plný text záznamu

Apremilast, a cAMP phosphodiesterase-4 inhibitor, demonstrates anti-inflammatory activity in vitro and in a model of psoriasis

Autor: P H, Schafer, A, Parton, A K, Gandhi, L, Capone, M, Adams, L, Wu, J B, Bartlett, M A, Loveland, A, Gilhar, Y-F, Cheung, G S, Baillie, M D, Houslay, H-W, Man, G W, Muller, D I, Stirling

Publikováno v: British journal of pharmacology. 159(4)

Apremilast is an orally administered phosphodiesterase-4 inhibitor, currently in phase 2 clinical studies of psoriasis and other chronic inflammatory diseases. The inhibitory effects of apremilast on pro-inflammatory responses of human primary periph

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::3341fc207e2b60462624c8e47b819406
https://pubmed.ncbi.nlm.nih.gov/20050849

Zobrazit plný text záznamu

Potent inhibition of cytokine production from intestinal lamina propria T cells by phosphodiesterase-4 inhibitory thalidomide analogues

Autor: J L, Prehn, C, Landers, G W, Muller, H W, Man, D I, Stirling, S R, Targan

Publikováno v: Journal of clinical immunology. 21(5)

In Crohn's disease, intestinal lamina propria (LP) T cells overproduce TNF-alpha and IFN-gamma, and clinical and animal studies indicate that this is pathogenic. Thalidomide influences cytokine production by leukocytes, inhibiting macrophage TNF-alph

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::b4d05491754bc0678f01d6b7f984683b
https://pubmed.ncbi.nlm.nih.gov/11720008

Zobrazit plný text záznamu

Thalidomide is distributed into human semen after oral dosing

Autor: S K, Teo, J L, Harden, A B, Burke, F H, Noormohamed, M, Youle, M A, Johnson, B S, Peters, D I, Stirling, S D, Thomas

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 29(10)

As part of a double-blind placebo-controlled study of the effect of thalidomide on body weight and the viral load of human immunodeficiency virus-seropositive patients, plasma and semen samples were analyzed for the presence of thalidomide. Patients

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::2983c5d0d1bf3000500077141b7aaeb2
https://pubmed.ncbi.nlm.nih.gov/11560881

Zobrazit plný text záznamu

Effect of a high-fat meal on thalidomide pharmacokinetics and the relative bioavailability of oral formulations in healthy men and women

Autor: S K, Teo, M R, Scheffler, K A, Kook, W G, Tracewell, W A, Colburn, D I, Stirling, S D, Thomas

Publikováno v: Biopharmaceuticsdrug disposition. 21(1)

The effect of food on the oral pharmacokinetics of thalidomide and the relative bioavailability of two oral thalidomide formulations were determined in an open label, single dose, randomized, three-way crossover study. Five male and eight female heal

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::5cf5b8eca4dd1b1652e079c5bb7f5093
https://pubmed.ncbi.nlm.nih.gov/11038436

Zobrazit plný text záznamu

Differential cytokine modulation and T cell activation by two distinct classes of thalidomide analogues that are potent inhibitors of TNF-alpha

Autor: L G, Corral, P A, Haslett, G W, Muller, R, Chen, L M, Wong, C J, Ocampo, R T, Patterson, D I, Stirling, G, Kaplan

Publikováno v: Journal of immunology (Baltimore, Md. : 1950). 163(1)

TNF-alpha mediates both protective and detrimental manifestations of the host immune response. Our previous work has shown thalidomide to be a relatively selective inhibitor of TNF-alpha production in vivo and in vitro. Additionally, we have recently

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::afd9e3ea7dd1afa4a1296907a85ba78a
https://pubmed.ncbi.nlm.nih.gov/10384139

Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání