Recombinant human H2 relaxin (serelaxin) as a cardiovascular drug: aiming at the right target

被引：22

作者：

Bani, Daniele ^{[1
]}

机构：

[1] Univ Florence, Res Unit Histol & Embryol, Dept Expt & Clin Med, Florence, Italy

来源：

DRUG DISCOVERY TODAY | 2020年 / 25卷 / 07期

关键词：

ENDOTHELIAL GROWTH-FACTOR; MYOCARDIAL-INFARCTION; CARDIAC FIBROSIS; DOUBLE-BLIND; REPERFUSION; HORMONE; INJURY; RECEPTOR; INVOLVEMENT; INHIBITION;

D O I：

10.1016/j.drudis.2020.04.014

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Serelaxin (recombinant human relaxin-2 hormone; RLX-2) had raised expectations as a new medication for cardiovascular diseases. Evidence from preclinical studies indicated that serelaxin has chronotropic, inotropic, and anti-arrhythmic actions on the myocardium and cardioprotective effects mediated by vasodilation, angiogenesis, and inhibition of inflammation and fibrosis. However, clinical trials with serelaxin in patients with acute heart failure (AHF) gave inconclusive results. A critical reappraisal of the comprehensive cardiovascular actions of serelaxin clearly delineates acute myocardial infarction (AMI) as a feasible therapeutic target. Serelaxin acts at multiple levels on the pathogenic mechanisms of AMI and previous in vivo studies suggest that its administration at reperfusion affords myocardial salvage. Thus, serelaxin could be an effective adjunctive medical therapy to coronary angioplasty.

引用

页码：1239 / 1244

页数：6

共 62 条

[1] Synthetic non-peptide low molecular weight agonists of the relaxin receptor 1 [J].

Agoulnik, Alexander I. ;

Agoulnik, Irina U. ;

Hu, Xin ;

Marugan, Juan .

BRITISH JOURNAL OF PHARMACOLOGY, 2017, 174 (10) :977-989

[2] Relaxin activates AMPK-AKT signaling and increases glucose uptake by cultured cardiomyocytes [J].

Aragon-Herrera, A. ;

Feijoo-Bandin, S. ;

Rodriguez-Penas, D. ;

Rosello-Lleti, E. ;

Portoles, M. ;

Rivera, M. ;

Bigazzi, M. ;

Bani, D. ;

Gualillo, O. ;

Gonzalez-Juanatey, J. R. ;

Lago, F. .

ENDOCRINE, 2018, 60 (01) :103-111

[3] Relaxin: A pleiotropic hormone [J].

Bani, D .

GENERAL PHARMACOLOGY-THE VASCULAR SYSTEM, 1997, 28 (01) :13-22

[4]

Bani D, 1998, AM J PATHOL, V152, P1367

[5] A novel, simple bioactivity assay for relaxin based on inhibition of platelet aggregation [J].

Bani, Daniele ;

Nistri, Silvia ;

Cinci, Lorenzo ;

Giannini, Lucia ;

Princivalle, Marc ;

Elliott, Lucy ;

Bigazzi, Mario ;

Masini, Emanuela .

REGULATORY PEPTIDES, 2007, 144 (1-3) :10-16

[6] Relaxin as a natural agent for vascular health [J].

Bani, Daniele .

VASCULAR HEALTH AND RISK MANAGEMENT, 2008, 4 (03) :515-524

[7]

BANI G, 1988, HISTOL HISTOPATHOL, V3, P337

[8] RELAXIN-INDUCED INCREASED CORONARY FLOW-THROUGH STIMULATION OF NITRIC-OXIDE PRODUCTION [J].

BANISACCHI, T ;

BIGAZZI, M ;

BANI, D ;

MANNAIONI, PF ;

MASINI, E .

BRITISH JOURNAL OF PHARMACOLOGY, 1995, 116 (01) :1589-1594

[9] The relaxin receptor as a therapeutic target - perspectives from evolution Cheek for updates and drug targeting [J].

Bathgate, Ross A. D. ;

Kocan, Martina ;

Scott, Daniel J. ;

Hossain, M. Akhter ;

Good, Sara V. ;

Yegorov, Sergey ;

Bogerd, Jan ;

Gooley, Paul R. .

PHARMACOLOGY & THERAPEUTICS, 2018, 187 :114-132

[10]

BELL RJ, 1987, OBSTET GYNECOL, V69, P585

← 1 2 3 4 5 6 7 →