Biological Activity
uk 383367 is a novel procollagen c-protein (pcp) inhibitor being investigated for the treatment of post-surgical dermal scarring, which potently inhibits the activity of pcp with the value of 50% inhibition concentration ic50 of 44 nm, as well as a selective inhibitor of matrix metalloproteinases (mmps) with values of ic50 >60,000 nm for mmp-2 and >10,000 nm for mmp-1, mmp-3, mmp-9 and mmp-4. although the mechanism is not clear yet, uk 383367 also exhibits weak inhibitory effects against phosphodiesterase-4 (pde-4) enzyme, including pde-4a, pde-4b, pde-4c and pde-4d, with values of ic50 of 1.8 μm, 1.5 μm, 2.4 μm and 0.9 μm respectively.g. a. allan, j. i. gedge, a. n. r. nedderman, s. j. roffey, h. f. small and r. webster. pharmacokinetics and metabolism of uk-383,367 in rats and dogs: a rationale for long-lived plasma radioactivity. xenobiotica 2006; 36(5): 399-418bailey s, fish pv, billotte s, bordner j, greiling d, james k, mcelroy a, mills je, reed c, webster r.ff. succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen c-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents. bioorg med chem lett. 2008;18(24):6562-6567
