Carbamate Insecticides Target Human Melatonin Receptors.

ABSTRACT: Carbaryl (1-naphthyl methylcarbamate) and carbofuran (2,3-dihydro-2,2-dimethyl-7-benzofuranyl methylcarbamate) are among the most toxic insecticides, implicated in a variety of diseases including diabetes and cancer among others. Using an integrated pharmacoinformatics based screening approach, we have identified these insecticides to be structural mimics of the neurohormone melatonin and were able to bind to the putative melatonin binding sites in MT₁ and MT₂ melatonin receptors in silico. Carbaryl and carbofuran then were tested for competition with 2-[¹²⁵I]-iodomelatonin (300 pM) binding to hMT₁ or hMT₂ receptors stably expressed in CHO cells. Carbaryl and carbofuran showed higher affinity for competition with 2-[¹²⁵I]-io

SUBMITTER: Popovska-Gorevski M 

PROVIDER: S-EPMC5318275 | biostudies-literature | 2017 Feb

REPOSITORIES: biostudies-literature