Biological evaluation and docking studies of natural isocoumarins as inhibitors for human kallikrein 5 and 7

Teixeira, Thiago Salem Pançonato; Freitas, Renato Ferreira de; Abrahão, Odonı́rio; Devienne, Karina F.; Souza, Lucas R. de; Blaber, Sachico I.; Blaber, Michael; Kondo, Márcia Y.; Juliano, María A.; Juliano, Luiz; Puzer, Luciano

doi:10.1016/j.bmcl.2011.08.044

Cited by 47 publications

(24 citation statements)

References 23 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Increases in KLK1 secretion and activity that are associated with the development of airway hyperresponsiveness are also dependent on the activation of resident and recruited inflammatory cells, including alveolar macrophages and neutrophils 130 . 185,186 . Using high-yield chemical synthesis, lactam-based enantiomers (for example, compound 3 in TABLE 2) have been generated that display potent covalent KLK3 inhibition 187 .…”

Section: Small-molecule Klk Inhibitorsmentioning

confidence: 97%

Unleashing the therapeutic potential of human kallikrein-related serine proteases

Prassas

Eissa

Poda

et al. 2015

Nat Rev Drug Discov

205

183

View full text Add to dashboard Cite

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.

show abstract

Section: Small-molecule Klk Inhibitorsmentioning

confidence: 97%

Unleashing the therapeutic potential of human kallikrein-related serine proteases

Prassas

Eissa

Poda

et al. 2015

Nat Rev Drug Discov

205

183

View full text Add to dashboard Cite

show abstract

“…Recently, three isocoumarin small compound inhibitors for hK7 and hK5 have been reported [56]. However, natural and synthetic isocoumarin compounds have been reported to be rather broad serine protease inhibitors [57].…”

Section: Discussionmentioning

confidence: 99%

Vaspin inhibits kallikrein 7 by serpin mechanism

Heiker

Klöting

Kovacs

et al. 2013

Cell. Mol. Life Sci.

134

144

View full text Add to dashboard Cite

not related to vaspin-mediated changes in insulin sensitivity as determined by euglycemic-hyperinsulinemic clamp studies. Improved glucose metabolism could be mediated by increased insulin plasma concentrations 150 min after a glucose challenge in db/db mice, supporting the hypothesis that vaspin may inhibit insulin degradation by hK7 in the circulation. In conclusion, we demonstrate the inhibitory serpin nature and the first protease target of the adipose tissue-derived serpin vaspin, and our findings suggest hK7 inhibition by vaspin as an underlying physiological mechanism for its compensatory actions on obesity-induced insulin resistance.

show abstract

“…Amongst the currently known inhibitors of kallikreins [41][42][43] , the naturally occurring cyclic peptide 539 SFTI has been extensively investigated due to it being amenable to chemical manipulation which 540 M A N U S C R I P T…”

mentioning

confidence: 99%

Persistent kallikrein 5 activation induces atopic dermatitis-like skin architecture independent of PAR2 activity

Zhu¹,

Underwood²,

Macmillan³

et al. 2017

Journal of Allergy and Clinical Immunology

View full text Add to dashboard Cite

show abstract

Biological evaluation and docking studies of natural isocoumarins as inhibitors for human kallikrein 5 and 7

Cited by 47 publications

References 23 publications

Unleashing the therapeutic potential of human kallikrein-related serine proteases

Unleashing the therapeutic potential of human kallikrein-related serine proteases

Vaspin inhibits kallikrein 7 by serpin mechanism

Persistent kallikrein 5 activation induces atopic dermatitis-like skin architecture independent of PAR2 activity

Contact Info

Product

Resources

About