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Artepillin C (CREB-CRTC2 inhibitor APC) is an inhibitor of CREB/CRTC2 interaction (IC50=24.5 uM), dissociates the CREB/CRTC2 complex, directly binds to CREB with Kd of 3.2 uM.CREB-CRTC2 inhibitor APC inhibits CRTC2 interacting with CREB-ZIP and reduces acetyltransferase activity of CBP by binding with CREB protein directly.Artepillin C attenuated gluconeogenesis in primary hepatocytes, reduced glucose output from primary hepatocytes induced by glucagon, remarkably decreased the mRNA accumulation of G6pc, Pck1, and Pgc-1α induced by glucagon in primary hepatocytes.|Artepillin C could ameliorate hyperlipidemia in obese mice.
ATF3W-aeg peptide is a selective, peptide inhibitor of activating transcription factor 3 (ATF3) with high affinity (Kd=151 nM), increases CCL4 expression levels in human macrophages.
Artepillin C (CREB-CRTC2 inhibitor APC) is an inhibitor of CREB/CRTC2 interaction (IC50=24.5 uM), dissociates the CREB/CRTC2 complex, directly binds to CREB with Kd of 3.2 uM.CREB-CRTC2 inhibitor APC inhibits CRTC2 interacting with CREB-ZIP and reduces acetyltransferase activity of CBP by binding with CREB protein directly.Artepillin C attenuated gluconeogenesis in primary hepatocytes, reduced glucose output from primary hepatocytes induced by glucagon, remarkably decreased the mRNA accumulation of G6pc, Pck1, and Pgc-1α induced by glucagon in primary hepatocytes.|Artepillin C could ameliorate hyperlipidemia in obese mice.
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