激肽释放酶蛋白酶激活受体（PAR）轴：一个有吸引力的药物开发靶点。 - Suppr

Kallikrein protease activated receptor (PAR) axis: an attractive target for drug development.

作者信息

Caliendo Giuseppe, Santagada Vincenzo, Perissutti Elisa, Severino Beatrice, Fiorino Ferdinando, Frecentese Francesco, Juliano Luiz

机构信息

Dipartimento di Chimica Farmaceutica e Tossicologica, Università degli Studi di Napoli Federico II, Via D. Montesano, 49, 80131, Napoli, Italy.

出版信息

J Med Chem. 2012 Aug 9;55(15):6669-86. doi: 10.1021/jm300407t. Epub 2012 Jun 12.

DOI:10.1021/jm300407t

PMID:22607152

Abstract

摘要

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Kallikrein protease activated receptor (PAR) axis: an attractive target for drug development.激肽释放酶蛋白酶激活受体（PAR）轴：一个有吸引力的药物开发靶点。

J Med Chem. 2012 Aug 9;55(15):6669-86. doi: 10.1021/jm300407t. Epub 2012 Jun 12.

Substrate-guided design of a potent and selective kallikrein-related peptidase inhibitor for kallikrein 4.基于底物导向设计的一种针对激肽释放酶4的强效且选择性激肽释放酶相关肽酶抑制剂。

Chem Biol. 2009 Jun 26;16(6):633-43. doi: 10.1016/j.chembiol.2009.05.008.

Kallikreins and proteinase-mediated signaling: proteinase-activated receptors (PARs) and the pathophysiology of inflammatory diseases and cancer.激肽释放酶与蛋白酶介导的信号传导：蛋白酶激活受体（PARs）以及炎症性疾病和癌症的病理生理学

Biol Chem. 2008 Jun;389(6):643-51. doi: 10.1515/BC.2008.077.

Biol Chem. 2010 Apr;391(4):299-310. doi: 10.1515/BC.2010.038.

Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.信号转导及转录激活因子3（Stat3）蛋白的小分子抑制剂

J Med Chem. 2012 Aug 9;55(15):6645-68. doi: 10.1021/jm300207s. Epub 2012 Jun 15.

Inhibiting aberrant Stat3 function with molecular therapeutics: a progress report.用分子疗法抑制异常 Stat3 功能：进展报告。

Anticancer Drugs. 2011 Feb;22(2):115-27. doi: 10.1097/CAD.0b013e328341185b.

Recent advances in synthesis of PAR ligands as therapeutic strategy for inflammatory diseases.

Mini Rev Med Chem. 2009 Jun;9(6):653-63. doi: 10.2174/138955709788452711.

Reddish, scaly, and itchy: how proteases and their inhibitors contribute to inflammatory skin diseases.发红、脱屑与瘙痒：蛋白酶及其抑制剂如何引发炎症性皮肤病

Arch Immunol Ther Exp (Warsz). 2009 Sep-Oct;57(5):345-54. doi: 10.1007/s00005-009-0045-6. Epub 2009 Aug 18.

Prostate-specific kallikreins-2 and -4 enhance the proliferation of DU-145 prostate cancer cells through protease-activated receptors-1 and -2.前列腺特异性激肽释放酶-2和-4通过蛋白酶激活受体-1和-2促进DU-145前列腺癌细胞的增殖。

Mol Cancer Res. 2008 Jun;6(6):1043-51. doi: 10.1158/1541-7786.MCR-08-0096.

Targeting proteinase-activated receptors: therapeutic potential and challenges.靶向蛋白酶激活受体：治疗潜力与挑战。

Nat Rev Drug Discov. 2012 Jan 3;11(1):69-86. doi: 10.1038/nrd3615.

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A Pair of Prognostic Biomarkers in Triple-Negative Breast Cancer: KLK10 and KLK11 mRNA Expression.三阴性乳腺癌中的一对预后生物标志物：激肽释放酶10（KLK10）和激肽释放酶11（KLK11）mRNA表达

Life (Basel). 2022 Sep 28;12(10):1517. doi: 10.3390/life12101517.

Remodelling of the tumour microenvironment by the kallikrein-related peptidases.激肽释放酶相关肽酶重塑肿瘤微环境。

Nat Rev Cancer. 2022 Apr;22(4):223-238. doi: 10.1038/s41568-021-00436-z. Epub 2022 Jan 31.

Topical Delivery of Rapamycin by Means of Microenvironment-Sensitive Core-Multi-Shell Nanocarriers: Assessment of Anti-Inflammatory Activity in an ex vivo Skin/T Cell Co-Culture Model.基于微环境敏感核-多壳纳米载体的雷帕霉素局部递送：在体外皮肤/ T 细胞共培养模型中评估抗炎活性。

Int J Nanomedicine. 2021 Oct 22;16:7137-7151. doi: 10.2147/IJN.S330716. eCollection 2021.

Biomarker implication of kallikrein-related peptidases as prognostic tissue substrates of poor survival in colorectal cancer.激肽释放酶相关肽酶作为结直肠癌患者预后不良的组织标志物的意义。

Cancer Cell Int. 2020 Jun 22;20:260. doi: 10.1186/s12935-020-01350-4. eCollection 2020.

Protease-activated receptors (PARs): mechanisms of action and potential therapeutic modulators in PAR-driven inflammatory diseases.蛋白酶激活受体（PARs）：PAR驱动的炎症性疾病中的作用机制及潜在治疗调节剂

Thromb J. 2019 Mar 29;17:4. doi: 10.1186/s12959-019-0194-8. eCollection 2019.

A potent, proteolysis-resistant inhibitor of kallikrein-related peptidase 6 (KLK6) for cancer therapy, developed by combinatorial engineering.通过组合工程开发的一种强力、抗蛋白水解的激肽释放酶相关肽酶 6（KLK6）抑制剂，用于癌症治疗。

J Biol Chem. 2018 Aug 17;293(33):12663-12680. doi: 10.1074/jbc.RA117.000871. Epub 2018 Jun 22.

Cathepsin K induces platelet dysfunction and affects cell signaling in breast cancer - molecularly distinct behavior of cathepsin K in breast cancer.组织蛋白酶K诱导血小板功能障碍并影响乳腺癌中的细胞信号传导——组织蛋白酶K在乳腺癌中的分子不同行为。

BMC Cancer. 2016 Mar 1;16:173. doi: 10.1186/s12885-016-2203-7.

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Kallikrein protease activated receptor (PAR) axis: an attractive target for drug development.

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