SR-4995 is a potent and selective ligand of α-β-hydrolase domain containing 5 (ABHD5) that activates adipose triglyceride lipase (ATGL) by dissociating ABHD5 from its inhibitory regulator, perilipin-1 (PLIN1) and PLIN5. SR-4995 directly binds to ABHD5 and prevents ABHD5 to PLIN1. SR-4995 induces lipolysis in adipocytes and muscle, avoiding PKA-dependent signaling.
potent and selective ligand of ABHD5 that activates ATGL by dissociating ABHD5 from PLIN1 and PLIN5
The Journal of pharmacology and experimental therapeutics, 363(3), 367-376 (2017-09-21)
Current knowledge regarding acute regulation of adipocyte lipolysis is largely based on receptor-mediated activation or inhibition of pathways that influence intracellular levels of cAMP, thereby affecting protein kinase A (PKA) activity. We recently identified synthetic ligands of α-β-hydrolase domain containing
Fat and muscle lipolysis involves functional interactions of adipose triglyceride lipase (ATGL), α-β hydrolase domain-containing protein 5 (ABHD5), and tissue-specific perilipins 1 and 5 (PLIN1 and PLIN5). ABHD5 potently activates ATGL, but this lipase-promoting activity is suppressed when ABHD5 is
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