Compound C/dorsomorphin: its use and misuse as an AMPK inhibitor
B Dasgupta, W Seibel - AMPK: methods and protocols, 2018 - Springer
AMPK: methods and protocols, 2018•Springer
The evolutionary conserved energy sensor AMPK plays crucial roles in many biological
processes—both during normal development and pathology. Loss-of-function genetic
studies in mice as well as in lower organisms underscore its importance in embryonic
development, stress physiology in the adult, and in key metabolic disorders including
cardiovascular disease, diabetes, cancer, and metabolic syndrome. In contrast to several
other kinases important in human health and medicine where specific/selective inhibitors …
processes—both during normal development and pathology. Loss-of-function genetic
studies in mice as well as in lower organisms underscore its importance in embryonic
development, stress physiology in the adult, and in key metabolic disorders including
cardiovascular disease, diabetes, cancer, and metabolic syndrome. In contrast to several
other kinases important in human health and medicine where specific/selective inhibitors …
Abstract
The evolutionary conserved energy sensor AMPK plays crucial roles in many biological processes—both during normal development and pathology. Loss-of-function genetic studies in mice as well as in lower organisms underscore its importance in embryonic development, stress physiology in the adult, and in key metabolic disorders including cardiovascular disease, diabetes, cancer, and metabolic syndrome. In contrast to several other kinases important in human health and medicine where specific/selective inhibitors are available, no AMPK-specific inhibitors are available. The only reagent called dorsomorphin or compound C that is occasionally used as an AMPK inhibitor unfortunately inhibits several other kinases much more potently than AMPK and is therefore highly non-specific. In this chapter, we discuss the pros and cons of using this reagent to study AMPK functions.
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