标题：Gelatinase inhibitors: a patent review (2011-2017)
作者机构：[Li, Xun] Shandong Univ, Sch Pharmaceut Sci, Minist Educ, Dept Med Chem,Key Lab Chem & Chem Biol, Jinan, Shandong, Peoples R China.
通讯作者地址：[Li, X]Shandong Univ, Sch Pharmaceut Sci, Minist Educ, Dept Med Chem,Key Lab Chem & Chem Biol, Jinan, Shandong, Peoples R China.
来源：EXPERT OPINION ON THERAPEUTIC PATENTS
关键词：MMP; gelatinase inhibitor; isoform selectivity; binding mode; drug; design strategy
摘要：Introduction: Gelatinase represents a promising biotarget in new drug development as it is closely related to various pathological events, including but not limited to neoplasm, aging, respiratory and neurological disorders. Gelatinase inhibitors are thereby designated as chemotherapeutics or as mechanistic probe to figure out the unrecognized functions of MMP members.; Areas covered: The focus of this article is to highlight recently issued patents concerning the naturally available or synthetic gelatinase inhibitors (2011-2017), where the chemical structures, SAR investigation, biological application. Besides, the binding modes of representative inhibitors with gelatinase are also briefly described.; Expert opinion: The access of crystallographic structure of inhibitor complexed with gelatinase, the availability of pharmacophoric features of gelatinase inhibitors, together with the proper use of drug design protocols, have paved the way for developing more selective and potent modulators. Moreover, considering typical bio-assessment was primarily concentrated on the antitumor effect, the other bioactivity outcomes should also be concerned to look for new application of gelatinase inhibitors.