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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: raab c. J Med Chem. 2009 Jun 11;52(11):3449-52. doi: 10.1021/jm900257b. J Med Chem. 2009. PMID: 19441819
A small molecule alpha4beta1/alpha4beta7 antagonist differentiates between the low-affinity states of alpha4beta1 and alpha4beta7: characterization of divalent cation dependence.
Egger LA, Cao J, McCallum C, Kidambi U, Van Riper G, McCauley E, Mumford RA, Lanza TJ, Lin LS, de Laszlo SE, Young DN, Yang G, Dean DC, Raab CE, Wallace MA, Jones AN, Hagmann WK, Schmidt JA, Pepinsky RB, Scott DM, Lee WC, Cornebise MA, Detmers PA. Egger LA, et al. Among authors: raab ce. J Pharmacol Exp Ther. 2003 Sep;306(3):903-13. doi: 10.1124/jpet.102.047704. Epub 2003 May 23. J Pharmacol Exp Ther. 2003. PMID: 12766251
Synthesis of the first sulfur-35-labeled hERG radioligand.
Raab CE, Butcher JW, Connolly TM, Karczewski J, Yu NX, Staskiewicz SJ, Liverton N, Dean DC, Melillo DG. Raab CE, et al. Bioorg Med Chem Lett. 2006 Mar 15;16(6):1692-5. doi: 10.1016/j.bmcl.2005.12.021. Epub 2006 Jan 11. Bioorg Med Chem Lett. 2006. PMID: 16377185
Identification of metabolites of a substance P (neurokinin 1 receptor) antagonist in rat hepatocytes and rat plasma.
Hop CE, Wang Y, Kumar S, Elipe MV, Raab CE, Dean DC, Poon GK, Keohane CA, Strauss J, Chiu SH, Curtis N, Elliott J, Gerhard U, Locker K, Morrison D, Mortishire-Smith R, Thomas S, Watt AP, Evans DC. Hop CE, et al. Among authors: raab ce. Drug Metab Dispos. 2002 Aug;30(8):937-43. doi: 10.1124/dmd.30.8.937. Drug Metab Dispos. 2002. PMID: 12124313
140 results