The Engineered Serine Protease Inhibitor MDPK67b for the Treatment of Diseases Involving Hyperactivi

来源 :中国上海第七届国际新药发明科技年会 | 被引量 : 0次 | 上传用户:xieqi509
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  Human kallikrein-related peptidase2 (KLK2) is a trypsin-like serine protease specifically expressed in the prostate gland and are suggested to be involved in prostate cancer development where its expression correlates with prostate cancer aggressiveness.The closely related kallikreins KLK4 and KLK14 are also predominantly expressed in the prostate and are suspected to participate in the biology of prostate cancer.MDPK67b is a potent and selective prostatic kallikrein inhibitor intended for use in treatment of prostate cancer.MDPK67b is a genetically engineered serine protease inhibitor which was developed to inhibit human kallikrein 2 (KLK2).MDPK67b is based on the human serpin alphal-Antichymotrypsin (ACT),in which the protease cleavage site within the reactive center loop was replaced with a KLK2-specific pentapeptide selected by phage display.
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