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Page 1
Discovery of N-{N-[(3-cyanophenyl)sulfonyl]-4(R)-cyclobutylamino-(L)-prolyl}-4-[(3',5'-dichloroisonicotinoyl) amino]-(L)-phenylalanine (MK-0668), an extremely potent and orally active antagonist of very late antigen-4.
Lin LS, Lanza T, Jewell JP, Liu P, Jones C, Kieczykowski GR, Treonze K, Si Q, Manior S, Koo G, Tong X, Wang J, Schuelke A, Pivnichny J, Wang R, Raab C, Vincent S, Davies P, Maccoss M, Mumford RA, Hagmann WK. Lin LS, et al. Among authors: koo g. J Med Chem. 2009 Jun 11;52(11):3449-52. doi: 10.1021/jm900257b. J Med Chem. 2009. PMID: 19441819
Discovery of 4-heteroarylbicyclo[2.2.2]octyltriazoles as potent and selective inhibitors of 11beta-HSD1: novel therapeutic agents for the treatment of metabolic syndrome.
Gu X, Dragovic J, Koo GC, Koprak SL, LeGrand C, Mundt SS, Shah K, Springer MS, Tan EY, Thieringer R, Hermanowski-Vosatka A, Zokian HJ, Balkovec JM, Waddell ST. Gu X, et al. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5266-9. doi: 10.1016/j.bmcl.2005.08.052. Epub 2005 Sep 26. Bioorg Med Chem Lett. 2005. PMID: 16185866
Correolide and derivatives are novel immunosuppressants blocking the lymphocyte Kv1.3 potassium channels.
Koo GC, Blake JT, Shah K, Staruch MJ, Dumont F, Wunderler D, Sanchez M, McManus OB, Sirotina-Meisher A, Fischer P, Boltz RC, Goetz MA, Baker R, Bao J, Kayser F, Rupprecht KM, Parsons WH, Tong XC, Ita IE, Pivnichny J, Vincent S, Cunningham P, Hora D Jr, Feeney W, Kaczorowski G, et al. Koo GC, et al. Cell Immunol. 1999 Nov 1;197(2):99-107. doi: 10.1006/cimm.1999.1569. Cell Immunol. 1999. PMID: 10607427
Potent Kv1.3 inhibitors from correolide-modification of the C18 position.
Bao J, Miao S, Kayser F, Kotliar AJ, Baker RK, Doss GA, Felix JP, Bugianesi RM, Slaughter RS, Kaczorowski GJ, Garcia ML, Ha SN, Castonguay L, Koo GC, Shah K, Springer MS, Staruch MJ, Parsons WH, Rupprecht KM. Bao J, et al. Bioorg Med Chem Lett. 2005 Jan 17;15(2):447-51. doi: 10.1016/j.bmcl.2004.10.058. Bioorg Med Chem Lett. 2005. PMID: 15603971
A tacrolimus-related immunosuppressant with reduced toxicity.
Dumont FJ, Koprak S, Staruch MJ, Talento A, Koo G, DaSilva C, Sinclair PJ, Wong F, Woods J, Barker J, Pivnichny J, Singer I, Sigal NH, Williamson AR, Parsons WH, Wyvratt M. Dumont FJ, et al. Among authors: koo g. Transplantation. 1998 Jan 15;65(1):18-26. doi: 10.1097/00007890-199801150-00005. Transplantation. 1998. PMID: 9448138
Benzamide derivatives as blockers of Kv1.3 ion channel.
Miao S, Bao J, Garcia ML, Goulet JL, Hong XJ, Kaczorowski GJ, Kayser F, Koo GC, Kotliar A, Schmalhofer WA, Shah K, Sinclair PJ, Slaughter RS, Springer MS, Staruch MJ, Tsou NN, Wong F, Parsons WH, Rupprecht KM. Miao S, et al. Bioorg Med Chem Lett. 2003 Mar 24;13(6):1161-4. doi: 10.1016/s0960-894x(03)00014-3. Bioorg Med Chem Lett. 2003. PMID: 12643934
Identification of a new class of inhibitors of the voltage-gated potassium channel, Kv1.3, with immunosuppressant properties.
Schmalhofer WA, Bao J, McManus OB, Green B, Matyskiela M, Wunderler D, Bugianesi RM, Felix JP, Hanner M, Linde-Arias AR, Ponte CG, Velasco L, Koo G, Staruch MJ, Miao S, Parsons WH, Rupprecht K, Slaughter RS, Kaczorowski GJ, Garcia ML. Schmalhofer WA, et al. Among authors: koo g. Biochemistry. 2002 Jun 18;41(24):7781-94. doi: 10.1021/bi025722c. Biochemistry. 2002. PMID: 12056910
208 results