Harnessing the power of structure-based design: A new lease on life for cardiovascular drug development with apelin receptormodulators

References

[1] Zhang M, Chen T, Lu X, Lan X, Chen Z, Lu S. G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery. Signal Transduct Target Ther. 2024; 9: 88.

[2] Liu S, Anderson PJ, Rajagopal S, Lefkowitz RJ, Rockman HA. G protein-coupled receptors: a century of research and discovery. Circ Res. 2024; 135: 174-197.

[3] Duan J, He XH, Li SJ, Xu HE. Cryo-electron microscopy for GPCR research and drug discovery in endocrinology and metabolism. Nat Rev Endocrinol. 2024; 20: 349-365.

[4] Inoue A, Raimondi F, Kadji FMN, et al. Illuminating G-protein-coupling selectivity of GPCRs. Cell. 2019; 177: 1933-1947. e25.

[5] Li B, Yang MY, Kim SK. The G protein-first mechanism for activation of the class B glucagon-like peptide 1 receptor coupled to N-terminal domain-mediated conformational progression. J Am Chem Soc. 2024; 146: 26251-26260.

[6] Estruch R, Ruilope LM, Cosentino F. The year in cardiovascular medicine 2020: epidemiology and prevention. Eur Heart J. 2021; 42: 813-821.

[7] Mullard A. 2019 FDA drug approvals. Nat Rev Drug Discovery. 2020; 19: 79-84.

[8] Chapman FA, Maguire JJ, Newby DE, Davenport AP, Dhaun N. Targeting the apelin system for the treatment of cardiovascular diseases. Cardiovasc Res. 2023; 119: 2683-2696.

[9] Japp AG, Newby DE. Unlocking the therapeutic potential of apelin. Hypertension. 2016; 68: 307-309.

[10] Scimia MC, Hurtado C, Ray S, et al. APJ acts as a dual receptor in cardiac hypertrophy. Nature. 2012; 488: 394-398.

[11] Coquerel D, Delile E, Dumont L, et al. Gαi-biased apelin analog protects against isoproterenol-induced myocardial dysfunction in rats. Am J Physiol Heart Circ Physiol. 2021; 320: H1646-h1656.

[12] Read C, Nyimanu D, Yang P, et al. The G protein biased small molecule apelin agonist CMF-019 is disease modifying in endothelial cell apoptosis in vitro and induces vasodilatation without desensitisation in vivo. Front Pharmacol. 2020; 11: 588669.

[13] Yang P, Read C, Kuc RE, et al. A novel cyclic biased agonist of the apelin receptor, MM07, is disease modifying in the rat monocrotaline model of pulmonary arterial hypertension. Br J Pharmacol. 2019; 176: 1206-1221.

[14] Wang WW, Ji SY, Zhang W, et al. Structure-based design of non-hypertrophic apelin receptor modulator. Cell. 2024; 187: 1460-1475. e20.

[15] André F, Rassy E, Marabelle A, Michiels S, Besse B. Forget lung, breast or prostate cancer: why tumour naming needs to change. Nature. 2024; 626: 26-29.

[16] Figtree GA, Broadfoot K, Casadei B, et al. A call to action for new global approaches to cardiovascular disease drug solutions. Circulation. 2021; 144: 159-169.

[17] Abdelsayed M, Kort EJ, Jovinge S, Mercola M. Repurposing drugs to treat cardiovascular disease in the era of precision medicine. Nat Rev Cardiol. 2022; 19: 751-764.

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2024 The Author(s). Clinical and Translational Medicine published by John Wiley & Sons Australia, Ltd on behalf of Shanghai Institute of Clinical Bioinformatics.