title: Unleashing the therapeutic potential of human kallikrein-related serine proteases.
abstract: Tissue kallikreins are a family of fifteen secreted serine proteases encoded by the largest protease gene cluster in the human genome. In the past decade, substantial progress has been made in characterizing the natural substrates, endogenous inhibitors and in vivo functions of kallikreins, and studies have delineated important pathophysiological roles for these proteases in a variety of tissues. Thus, kallikreins are now considered attractive targets for the development of novel therapeutics for airway, cardiovascular, tooth, brain, skin and neoplastic diseases. In this Review, we discuss recent advances in our understanding of the physiological functions and pathological implications of kallikrein proteases, and highlight progress in the identification of kallikrein inhibitors, which together are bringing us closer to therapeutically targeting kallikreins in selected disease settings.
authors.affiliation: 1] Department of Pathology and Laboratory Medicine, Mount Sinai Hospital, Toronto, M5G 1X5, Canada. [2] Department of Clinical Biochemistry, University Health Network, Toronto, M5G 2C4, Canada. [3].
authors.forename: Ioannis
authors.initials: I
authors.lastname: Prassas
authors.affiliation: 1] Department of Pathology and Laboratory Medicine, Mount Sinai Hospital, Toronto, M5G 1X5, Canada. [2] Department of Clinical Biochemistry, University Health Network, Toronto, M5G 2C4, Canada. [3].
authors.forename: Azza
authors.initials: A
authors.lastname: Eissa
authors.affiliation: 1] Drug Discovery Program, Ontario Institute for Cancer Research, Toronto, M5G 0A3, Canada. [2] Leslie Dan Faculty of Pharmacy, University of Toronto, Toronto, M5S 3M2, Canada.
authors.forename: Gennadiy
authors.initials: G
authors.lastname: Poda
authors.affiliation: 1] Department of Pathology and Laboratory Medicine, Mount Sinai Hospital, Toronto, M5G 1X5, Canada. [2] Department of Clinical Biochemistry, University Health Network, Toronto, M5G 2C4, Canada.
authors.forename: Eleftherios P
authors.initials: EP
authors.lastname: Diamandis
mesh_terms: D000818:Animals; D006801:Humans; D008958:Models, Molecular; D057057:Serine Proteases / Q000235:genetics / Q000502:physiology; D015842:Serine Proteinase Inhibitors / Q000627:therapeutic use*; D020840:Tissue Kallikreins / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000502:physiology
chemical_list: D015842:Serine Proteinase Inhibitors; D057057:Serine Proteases; D020840:Tissue Kallikreins