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Page 1
The discovery of sulfonylated dipeptides as potent VLA-4 antagonists.
Hagmann WK, Durette PL, Lanza T, Kevin NJ, de Laszlo SE, Kopka IE, Young D, Magriotis PA, Li B, Lin LS, Yang G, Kamenecka T, Chang LL, Wilson J, MacCoss M, Mills SG, Van Riper G, McCauley E, Egger LA, Kidambi U, Lyons K, Vincent S, Stearns R, Colletti A, Teffera J, Tong S, Fenyk-Melody J, Owens K, Levorse D, Kim P, Schmidt JA, Mumford RA. Hagmann WK, et al. Bioorg Med Chem Lett. 2001 Oct 22;11(20):2709-13. doi: 10.1016/s0960-894x(01)00544-3. Bioorg Med Chem Lett. 2001. PMID: 11591507
The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists.
Lin LS, Kopka IE, Mumford RA, Magriotis PA, Lanza T Jr, Durette PL, Kamenecka T, Young DN, de Laszlo SE, McCauley E, Riper GV, Kidambi U, Egger LA, Tong X, Lyons K, Vincent S, Stearns R, Colletti A, Teffera Y, Fenyk-Melody J, Schmidt JA, MacCoss M, Hagmann WK. Lin LS, et al. Bioorg Med Chem Lett. 2002 Feb 25;12(4):611-4. doi: 10.1016/s0960-894x(01)00818-6. Bioorg Med Chem Lett. 2002. PMID: 11844683
N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists.
Li B, de Laszlo SE, Kamenecka TM, Kopka IE, Durette PL, Lanza T Jr, MacCoss M, Tong S, Mumford RA, McCauley ED, Van Riper G, Schmidt JA, Hagmann WK. Li B, et al. Bioorg Med Chem Lett. 2002 Aug 19;12(16):2141-4. doi: 10.1016/s0960-894x(02)00366-9. Bioorg Med Chem Lett. 2002. PMID: 12127523
Substituted 3-amino biaryl propionic acids as potent VLA-4 antagonists.
Kopka IE, Lin LS, Mumford RA, Lanza T Jr, Magriotis PA, Young D, DeLaszlo SE, MacCoss M, Mills SG, Van Riper G, McCauley E, Lyons K, Vincent S, Egger LA, Kidambi U, Stearns R, Colletti A, Teffera Y, Tong S, Owens K, Levorse D, Schmidt JA, Hagmann WK. Kopka IE, et al. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2415-8. doi: 10.1016/s0960-894x(02)00460-2. Bioorg Med Chem Lett. 2002. PMID: 12161146
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. J Med Chem. 2009 Jun 11;52(11):3449-52. doi: 10.1021/jm900257b. J Med Chem. 2009. PMID: 19441819
Effects of VLA-4 antagonists in rat whole embryo culture.
Spence S, Vetter C, Hagmann WK, Van Riper G, Williams H, Mumford RA, Lanza TJ, Lin LS, Schmidt JA. Spence S, et al. Among authors: lanza tj. Teratology. 2002 Jan;65(1):26-37. doi: 10.1002/tera.1095. Teratology. 2002. PMID: 11835229
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: lanza tj. 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
31 results