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Design, synthesis, and analysis of a polyethelene glycol-modified (PEGylated) small molecule inhibitor of integrin {alpha}4{beta}1 with improved pharmaceutical properties.
Pepinsky RB, Lee WC, Cornebise M, Gill A, Wortham K, Chen LL, Leone DR, Giza K, Dolinski BM, Perper S, Nickerson-Nutter C, Lepage D, Chakraborty A, Whalley ET, Petter RC, Adams SP, Lobb RR, Scott DM. Pepinsky RB, et al. Among authors: scott dm. J Pharmacol Exp Ther. 2005 Feb;312(2):742-50. doi: 10.1124/jpet.104.075648. Epub 2004 Oct 14. J Pharmacol Exp Ther. 2005. PMID: 15485895
An assessment of the mechanistic differences between two integrin alpha 4 beta 1 inhibitors, the monoclonal antibody TA-2 and the small molecule BIO5192, in rat experimental autoimmune encephalomyelitis.
Leone DR, Giza K, Gill A, Dolinski BM, Yang W, Perper S, Scott DM, Lee WC, Cornebise M, Wortham K, Nickerson-Nutter C, Chen LL, LePage D, Spell JC, Whalley ET, Petter RC, Adams SP, Lobb RR, Pepinsky RB. Leone DR, et al. Among authors: scott dm. J Pharmacol Exp Ther. 2003 Jun;305(3):1150-62. doi: 10.1124/jpet.102.047332. Epub 2003 Mar 6. J Pharmacol Exp Ther. 2003. PMID: 12626659
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: scott dm. 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
Utilizing structure based drug design and metabolic soft spot identification to optimize the in vitro potency and in vivo pharmacokinetic properties leading to the discovery of novel reversible Bruton's tyrosine kinase inhibitors.
Hopkins BT, Bame E, Bell N, Bohnert T, Bowden-Verhoek JK, Bui M, Cancilla MT, Conlon P, Cullen P, Erlanson DA, Fan J, Fuchs-Knotts T, Hansen S, Heumann S, Jenkins TJ, Gua C, Liu Y, Liu Y, Lulla M, Marcotte D, Marx I, McDowell B, Mertsching E, Negrou E, Romanowski MJ, Scott D, Silvian L, Yang W, Zhong M. Hopkins BT, et al. Bioorg Med Chem. 2021 Aug 15;44:116275. doi: 10.1016/j.bmc.2021.116275. Epub 2021 Jun 15. Bioorg Med Chem. 2021. PMID: 34314938
MS-325: a small-molecule vascular imaging agent for magnetic resonance imaging.
Lauffer RB, Parmelee DJ, Ouellet HS, Dolan RP, Sajiki H, Scott DM, Bernard PJ, Buchanan EM, Ong KY, Tyeklár Z, Midelfort KS, McMurry TJ, Walovitch RC. Lauffer RB, et al. Among authors: scott dm. Acad Radiol. 1996 Aug;3 Suppl 2:S356-8. doi: 10.1016/s1076-6332(96)80583-6. Acad Radiol. 1996. PMID: 8796603 No abstract available.
209 results