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Structure of the catalytic domain of fibroblast collagenase complexed with an inhibitor.
The detailed description of protein-inhibitor interactions present in the structure will aid in the design of compounds that selectively inhibit individual members of the MMP family.
Potent and selective nonpeptidic inhibitors of procollagen C-proteinase.
Sulfonamide 56 (UK-421,045) was selected as a candidate for further preclinical evaluation as a topically applied, dermal anti-scarring agent and demonstrates excellent selectivity over MMPs involved in wound healing (>10 000-fold).
Highly potent and selective heptapeptide antagonists of the neurokinin NK-2 receptor.
Replacement of D-Trp9 by D-Pro9 in the nonselective neurokinin antagonist SP(5-11) gave a partial agonist withNK-2 receptor selectivity, which produced a potent inhibition of NK-2 agonist-induced bronchoconstriction in the anaesthetized guinea-pig.
Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents.
GR159897 and related analogues as highly potent, orally active non-peptide neurokinin NK2 receptor antagonists.
Characterisation, CNS distribution and function of NK2 receptors studied using potent NK2 receptor antagonists
Low molecular weight neurokinin NK2 antagonists
Discovery of potent & selective inhibitors of activated thrombin-activatable fibrinolysis inhibitor for the treatment of thrombosis.
Data indicate 21 (UK-396,082) has potential as a novel TAFIa inhibitor for the treatment of thrombosis and other fibrin-dependent diseases in humans.
NK2 antagonists and the role of NK2 receptors
Conformationally constrained tachykinin analogues: potent and highly selective neurokinin NK-2 receptor agonists.
The design and synthesis of potent and selective neurokinin NK-2 receptor agonists 12 (GR64349) and 31 are described, together with structure-activity relationships for related analogues. Compound 12…