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Apremilast, a cAMP phosphodiesterase-4 inhibitor, demonstrates anti-inflammatory activity in vitro and in a model of psoriasis.
Schafer PH, Parton A, Gandhi AK, Capone L, Adams M, Wu L, Bartlett JB, Loveland MA, Gilhar A, Cheung YF, Baillie GS, Houslay MD, Man HW, Muller GW, Stirling DI. Schafer PH, et al. Among authors: muller gw. Br J Pharmacol. 2010 Feb;159(4):842-55. doi: 10.1111/j.1476-5381.2009.00559.x. Epub 2009 Dec 24. Br J Pharmacol. 2010. PMID: 20050849 Free PMC article.
Immunomodulatory drugs (IMiDs) increase the production of IL-2 from stimulated T cells by increasing PKC-theta activation and enhancing the DNA-binding activity of AP-1 but not NF-kappaB, OCT-1, or NF-AT.
Payvandi F, Wu L, Naziruddin SD, Haley M, Parton A, Schafer PH, Chen RS, Muller GW, Hughes CC, Stirling DI. Payvandi F, et al. Among authors: muller gw. J Interferon Cytokine Res. 2005 Oct;25(10):604-16. doi: 10.1089/jir.2005.25.604. J Interferon Cytokine Res. 2005. PMID: 16241859
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-alpha inhibitor.
Man HW, Schafer P, Wong LM, Patterson RT, Corral LG, Raymon H, Blease K, Leisten J, Shirley MA, Tang Y, Babusis DM, Chen R, Stirling D, Muller GW. Man HW, et al. Among authors: muller gw. J Med Chem. 2009 Mar 26;52(6):1522-4. doi: 10.1021/jm900210d. J Med Chem. 2009. PMID: 19256507
Thalidomide analogs and PDE4 inhibition.
Muller GW, Shire MG, Wong LM, Corral LG, Patterson RT, Chen Y, Stirling DI. Muller GW, et al. Bioorg Med Chem Lett. 1998 Oct 6;8(19):2669-74. doi: 10.1016/s0960-894x(98)00475-2. Bioorg Med Chem Lett. 1998. PMID: 9873600
Alpha-fluoro-substituted thalidomide analogues.
Man HW, Corral LG, Stirling DI, Muller GW. Man HW, et al. Among authors: muller gw. Bioorg Med Chem Lett. 2003 Oct 20;13(20):3415-7. doi: 10.1016/s0960-894x(03)00778-9. Bioorg Med Chem Lett. 2003. PMID: 14505639
103 results