Coactivators

Mediating the functional connection between transcription factors and the general transcription apparatus are the coactivators. Coactivator refers to a protein or protein complex that increases the rate of transcription by interacting with transcription factors but does not itself bind to DNA in a sequence-specific manner. Peroxisome proliferator–activated receptor-γ coactivator-1 (PGC-1s) are proteins that enhance the transcriptional activity of transcription factors through direct protein-protein interactions. PGC-1α serves as an inducible coregulator in the control of energy homeostasis, and its expression is induced rapidly by physiological conditions known to increase the demand for mitochondrial ATP production such as cold exposure, exercise, and fasting. It has been shown to regulate adaptive thermogenesis, mitochondrial biogenesis, glucose and fatty acid metabolism, the peripheral circadian clock, fiber-type switching in skeletal muscle, and heart development.[1][2][3]


[1] L.N. Zhang et al. Novel small-molecule PGC-1α transcriptional regulator with beneficial effects on diabetic db/db mice. Diabetes. 2013, 62, 1297-1307.
[2] P. Puigserver et al. Peroxisome proliferator-activated receptor-gamma coactivator 1 alpha (PGC-1 alpha): transcriptional coactivator and metabolic regulator. Endocr. Rev. 2003, 24, 78-90.
[3] B.N. Finck et al. Peroxisome proliferator-activated receptor gamma coactivator-1 (PGC-1) regulatory cascade in cardiac physiology and disease. Circulation. 2007, 115, 2540-2548.

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Axon ID Name Description From price
4267 FX-909 Peroxisome proliferator-activated receptor gamma (PPARG) inverse agonist  Recently added Inquire
4102 GA-017 Potent LATS1/2 inhibitor  Recently added €140.00
3480 PY-60 Specific YAP activator targeting ANXA2 €150.00
3824 TEAD inhibitor TM2 Potent reversible pan-TEAD inhibitor €130.00
3276 TRULI LATS1/2 inhibitor €120.00
3354 Verteporfin Inhibitor of TEAD-YAP association; Photosensitizer €90.00
2379 ZLN 005 Selective transcriptional regulator of peroxisome PPAR-γ coactivator-1α (PGC-1α). €50.00

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