Inhibition of matrix metalloproteinases: An examination of the S1' pocket

Bioorganic and Medicinal Chemistry Letters

Volumn 7, Issue 2, 1997, Pages 193-198

  Miller, Andrew ^a   Askew, Marion ^a   Beckett, R Paul ^a   Bellamy, Claire L ^a   Bone, Elisabeth A ^a   Coates, Rachael E ^a   Davidson, Alan H ^a   Drummond, Alan H ^a   Huxley, Philip ^a   Martin, Fionna M ^a   Saroglou, Lydia ^a   Thompson, Alison J ^a   Van Dijk, Sonja E ^a   Whittaker, Mark ^a  

^a British Biotech Pharmaceuticals Ltd   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

MATRIX METALLOPROTEINASE; MATRIX METALLOPROTEINASE INHIBITOR;

ARTICLE; CHIRALITY; DRUG SYNTHESIS; ENZYME SPECIFICITY; REACTION ANALYSIS;

EID: 0031024461     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(96)00602-6     Document Type: Article

References (27)

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23. The following literature procedures were adapted to determine the potency of compounds against recombinant enzyme. HFC, Sawston, T. E.; Barrett, A. J. Anal. Biochem. 1979, 99, 340-345; Cawston, T. E.; Murphy, G. In Methods in Enzymology, ed Lorand, L. (Academic Press, New York), 1981, Vol. 80, pp. 711-722. HFS, GelA, Sellars, A.; Reynolds, J. J.; Meikle, M. C. Biochem. J. 1979, 171, 493-496.
24. The following literature procedures were adapted to determine the potency of compounds against recombinant enzyme. HFC, Sawston, T. E.; Barrett, A. J. Anal. Biochem. 1979, 99, 340-345; Cawston, T. E.; Murphy, G. In Methods in Enzymology, ed Lorand, L. (Academic Press, New York), 1981, Vol. 80, pp. 711-722. HFS, GelA, Sellars, A.; Reynolds, J. J.; Meikle, M. C. Biochem. J. 1979, 171, 493-496.
25. 50 18 nM).
26. 50 HFS, 14 nM
27. Male rats (n=12) were dosed orally with compound 7e (10 mg/kg), serial blood samples were removed and MMPI activity extracted and assayed against GelA. Concentrations were calculated against a standard curve. The mean blood levels were in excess of 100 ng/ml at 2h post dosing. Bone, E. A.; Askew, M.; Laber, D.; unpublished results.