Discovery of a potent HMG-CoA reductase degrader that eliminates statin …
2018年12月3日 · Accumulated HMG-CoA reductase (HMGCR) limits the cholesterol-lowering effect of statins via a feedback loop.
Statin therapy inhibits fatty acid synthase via dynamic protein ...
2022年5月10日 · Statins inhibit HMG-CoA reductase (HMGCR), which converts the metabolite HMG-CoA into mevalonate.
Discovery of a potent HMG-CoA reductase degrader that eliminates statin …
2018年12月3日 · Accumulated HMG-CoA reductase (HMGCR) limits the cholesterol-lowering effect of statins via a feedback loop. Here the authors developed a compound that degrades HMGCR, thus decreasing cholesterol levels and reducing atherosclerotic plaques.
Regulated degradation of HMG CoA reductase requires ... - Nature
2020年5月18日 · Competitive inhibitors of HMGCR called statins are prescribed to lower circulating levels of low density lipoprotein (LDL)-cholesterol and reduce the incidence of atherosclerotic cardiovascular...
Structural Mechanism for Statin Inhibition of HMG-CoA Reductase
Although the statins that are currently available or in late-stage development excel in curtailing the biosynthesis of mevalonate, the precursor of cholesterol, it is possible that the visualization of statin bound to HMGR will assist in the development of even better inhibitors.
Statin-induced anti-HMGCR myopathy: successful therapeutic …
2020年1月8日 · This case series provides an overview of the disease spectrum of statin-induced anti-HMGCR myopathy, ranging from presentation as an acute IMNM to persistent hyperCKemia despite statin discontinuation.
Inhibition of human 3-hydroxy-3-methylglutaryl CoA reductase by ...
2019年6月6日 · Currently, statins are the most extensively used drugs for lowering cholesterol. The statins reduce the regulatory pool of intracellular cholesterol by competitively inhibiting HMGCR. The cholesterol-lowering action of statins has shown to affect fewer cardiovascular events consistently [14, 15].
Statin-Induced Low-Density Lipoprotein Cholesterol Lowering …
To evaluate possible associations between statin treatment and noncardiovascular effects (ie, pleiotropy), we used a previously reported genetic instrument for HMGCR. 16 Specifically, we constructed a weighted GRS of HMGCR using 6 genetic variants within the HMGCR region that have been independently associated with LDL-C levels (eTable 1 in the ...
HMG-CoA reductase degrader, SR-12813, counteracts statin …
2023年10月15日 · Dual targeting of HMGCR using statins and SR-12813 (or similar TPD drugs targeting the HMGCR protein) may represent an improved anticancer therapeutic approach compared with statin monotherapy. Several efforts have been made to counteract statin-induced activation of SREBP2 transcription.
Limb girdle muscular disease caused by HMGCR mutation and statin …
Keywords: HMGCR, statins, limb girdle muscular dystrophy, mutation. Abstract. Myopathy is the main adverse effect of the widely prescribed statin drug class. Statins exert their beneficial effect by inhibiting HMG CoA-reductase, the rate-controlling enzyme of the mevalonate pathway. The mechanism of statin myopathy is yet to be resolved, and ...