Summary
August 2004, Vol. 14, No. 8, Pages 1185-1197 , DOI 10.1517/13543776.14.8.1185

Inhibition of procollagen C-proteinase: fibrosis and beyond

Eric D Turtle, Wen-Bin Ho
FibroGen, Inc., Department of Medicinal Chemistry, 225 Gateway Blvd. South San Francisco, CA 94080, USA. eturtle@fibrogen.com



Procollagen C-proteinase (PCP) plays a key role in fibrosis. The activity of PCP is necessary to convert soluble procollagens into fully formed collagen fibrils. Fibrosis is a pathological condition in which the normal wound healing process goes awry, culminating in the excessive production and deposition of collagen, a major component of scar tissue. The persistent formation of scar tissue hinders proper tissue function and can lead to organ failure in a wide range of fibrotic diseases. PCP is recognised as an attractive target for antifibrotic therapies. This review provides a discussion of the therapeutic potential of PCP inhibition and an examination of relevant patent literature, primarily focused on the identification of small molecule inhibitors of PCP for the prevention of dermal scarring and fibrotic disease. The emerging roles of PCP in biological processes other than collagen biosynthesis are also discussed.

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Authors:
Eric D Turtle
Wen-Bin Ho
Keywords:
bone morphogenetic protein-1
fibrosis
mammalian tolloid
procollagen C-proteinase
tolloid-like protein