Xiao B, Sanders MJ, Carmena D, Bright NJ, Haire LF, Underwood E, Patel BR, Heath RB, Walker PA, Hallen S et al. (2013) Structural basis of AMPK regulation by small molecule activators.According to the most recent scientific findings, many physicians think that activating AMPK is the key to living a longer and healthier life. Walter C, Clemens LE, Müller AJ, Fallier-Becker P, Proikas-Cezanne T, Riess O, Metzger S, Nguyen HP. (2016) Activation of AMPK-induced autophagy ameliorates Huntington disease pathology in vitro.ġ1. Sarkar S, Krishna G, Imarisio S, Saiki S, O'Kane CJ, Rubinsztein DC. (2008) A rational mechanism for combination treatment of Huntington's disease using lithium and rapamycin.ġ0. Ravikumar B, Vacher C, Berger Z, Davies JE, Luo S, Oroz LG, Scaravilli F, Easton DF, Duden R, O'Kane CJ et al. (2004) Inhibition of mTOR induces autophagy and reduces toxicity of polyglutamine expansions in fly and mouse models of Huntington disease.ĩ. Rajamohan F, Harris MS, Frisbie RK, Hoth LR, Geoghegan KF, Valentine JJ, Reyes AR, Landro JA, Qiu X, Kurumbail RG. (2010) Escherichia coli expression, purification and characterization of functional full-length recombinant alpha2beta2gamma3 heterotrimeric complex of human AMP-activated protein kinase.Ĩ. Machrouhi F, Ouhamou N, Laderoute K, Calaoagan J, Bukhtiyarova M, Ehrlich PJ, Klon AE. (2010) The rational design of a novel potent analogue of the 5'-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity.ħ. Göransson O, McBride A, Hawley SA, Ross FA, Shpiro N, Foretz M, Viollet B, Hardie DG, Sakamoto K. (2007) Mechanism of action of A-769662, a valuable tool for activation of AMP-activated protein kinase.Ħ. Engers DW, Frist AY, Lindsley CW, Hong CC, Hopkins CR. (2013) Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolopyrimidine scaffold of dorsomorphin: the discovery of M元47 as an ALK2 versus ALK3 selective MLPCN probe.ĥ.
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A specific method for activating AMP-activated protein kinase in intact cells?.Ĥ. Corton JM, Gillespie JG, Hawley SA, Hardie DG. (1995) 5-aminoimidazole-4-carboxamide ribonucleoside.
Ampk metabolic activator Activator#
Cool B, Zinker B, Chiou W, Kifle L, Cao N, Perham M, Dickinson R, Adler A, Gagne G, Iyengar R et al. (2006) Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome.ģ. Coffey G, Betz A, DeGuzman F, Pak Y, Inagaki M, Baker DC, Hollenbach SJ, Pandey A, Sinha U. (2014) The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer.Ģ. Thus, drug-like AMPK activators are being investigated as a mechanism to elevate autophagy-driven clearance of the protein aggregates associated with neurodegenerative diseases, as an alternative mechanism to mTOR inhibition. In neurodegenerative conditions that are characterised by the formation of protein aggregates (tauopathies, Huntington disease, Alzheimer's), autophagic function is considered to be key for effective depletion of the aberrant proteins whose accumulation proves to be toxic to cells. Dysregulated/ineffective autophagy is recognised as being associated with a variety of diseases including cancer, viral and bacterial infections, and neurodegeneration. The autophagic system degrades unwanted or damaging cellular contents including long-lived proteins, protein complexes, damaged organelles and invading pathogens.
Ampk metabolic activator driver#
For example, AMPK is now considered as a driver of autophagy, a process that is very important for maintaining proper cell function. It has subsequently been ascribed roles in additional biological processes. ĪMPK was originally recognised as a regulator of energy and metabolic balance and was proposed as a promising target for drugs aimed at treatment of type 2 diabetes and the metabolic syndrome.
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Characterization of functional, full-length, muscle-specific α2β2γ3 AMPK produced in E. AMP binds to "Bateman domains" on the γ subunit and this promotes activation via increased phosphorylation of Thr172 on the activation loop of AMPK's α subunit. AMPK is a regulator of energy balance at the cellular and whole body levels.
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Description: Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunitsĪMP-activated protein kinase (AMPK) is a heterotrimeric protein kinase, made up of one catalytic α subunit, one β and one γ subunit, both of which are regulatory in function.