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Potent cyclic peptide inhibitors of VLA-4 (alpha4beta1 integrin)-mediated cell adhesion. Discovery of compounds like cyclo(MePhe-Leu-Asp-Val-D-Arg-D-Arg) (ZD7349) compatible with depot formulation.
Dutta AS, Gormley JJ, Coath M, Hassall L, Hayward CF, Gellert PR, Kittlety RS, Alcock PJ, Ferguson R, Halterman T, Jamieson A, Moors JA, Moores JM, Rees A, Wood LJ, Reilly CF, Haworth D. Dutta AS, et al. Among authors: rees a. J Pept Sci. 2000 Aug;6(8):398-412. doi: 10.1002/1099-1387(200008)6:8<398::AID-PSC270>3.0.CO;2-1. J Pept Sci. 2000. PMID: 10969869
Potent cyclic monomeric and dimeric peptide inhibitors of VLA-4 (alpha4beta1 integrin)-mediated cell adhesion based on the Ile-Leu-Asp-Val tetrapeptide.
Dutta AS, Crowther M, Gormley JJ, Hassall L, Hayward CF, Gellert PR, Kittlety RS, Alcock PJ, Jamieson A, Moores JM, Rees A, Wood LJ, Reilly CF, Haworth D. Dutta AS, et al. Among authors: rees a. J Pept Sci. 2000 Jul;6(7):321-41. doi: 10.1002/1099-1387(200007)6:7<321::AID-PSC259>3.0.CO;2-A. J Pept Sci. 2000. PMID: 10946997
Structure-based design of protein tyrosine phosphatase-1B inhibitors.
Black E, Breed J, Breeze AL, Embrey K, Garcia R, Gero TW, Godfrey L, Kenny PW, Morley AD, Minshull CA, Pannifer AD, Read J, Rees A, Russell DJ, Toader D, Tucker J. Black E, et al. Among authors: rees a. Bioorg Med Chem Lett. 2005 May 16;15(10):2503-7. doi: 10.1016/j.bmcl.2005.03.068. Bioorg Med Chem Lett. 2005. PMID: 15863305
Novel acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with reduced acyl glucuronide liability: the discovery of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid (AZD8329).
Scott JS, deSchoolmeester J, Kilgour E, Mayers RM, Packer MJ, Hargreaves D, Gerhardt S, Ogg DJ, Rees A, Selmi N, Stocker A, Swales JG, Whittamore PR. Scott JS, et al. Among authors: rees a. J Med Chem. 2012 Nov 26;55(22):10136-47. doi: 10.1021/jm301252n. Epub 2012 Nov 7. J Med Chem. 2012. PMID: 23088558
Discovery of a potent, selective, and orally bioavailable acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor: discovery of 2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid (AZD4017).
Scott JS, Bowker SS, Deschoolmeester J, Gerhardt S, Hargreaves D, Kilgour E, Lloyd A, Mayers RM, McCoull W, Newcombe NJ, Ogg D, Packer MJ, Rees A, Revill J, Schofield P, Selmi N, Swales JG, Whittamore PR. Scott JS, et al. Among authors: rees a. J Med Chem. 2012 Jun 28;55(12):5951-64. doi: 10.1021/jm300592r. Epub 2012 Jun 19. J Med Chem. 2012. PMID: 22691057
946 results