Target Validation Information
Target ID T94309
Target Name Triacylglycerol lipase, pancreatic
Target Type
Successful
Drug Potency against Target Dalbavancin Drug Info MIC50 = 0.06 ug/ml [552333]
Action against Disease Model Dalbavancin In a recent survey of more than 1100 MRSA clinical isolates, the MIC50 of dalbavancin was 0.06 mg/L, compared with 1 and 0.5 mg/L, respectively, for vancomycin and teicoplanin. [553099] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations Pancreatic acinar cells synthesize two pancreatic lipase-related proteins (PLRP1 and PLRP2), which have a high degree of sequence and structural homology with PTL. The lipase activity of PLRP2 has been confirmed, whereas no known triglyceride lipase activity has been detected with PLRP1 up to now. To explore the biological functions of PLRP1 in vivo, we generated Plrp1 knockout (KO) mice in our laboratory. Here we show that the Plrp1 KO mice displayed mature-onset obesity with increased fat mass, impaired glucose clearance and the resultant insulin resistance. When fed on high-fat (HF) diet, the Plrp1 KO mice exhibited an increased weight gain, fat mass and severe insulin resistance compared with wild-type mice. Pancreatic juice extracted from Plrp1 KO mice had greater ability to hydrolyze triglyceride than that from the wild-type littermates. We propose that PLRP1 may function as a metabolic inhibitor in vivo of PLT-colipase-mediated dietary triglyceride digestion and provides potential anti-obesity targets for developing new drugs [552333]
References
Ref 552333Novel antibacterial agents for the treatment of serious Gram-positive infections. Expert Opin Investig Drugs. 2003 Mar;12(3):379-99.
Ref 553099Effects of age on parathyroid hormone signaling in human marrow stromal cells. Aging Cell. 2011 Oct;10(5):780-8. doi: 10.1111/j.1474-9726.2011.00717.x. Epub 2011 May 25.

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