of calcium by a mechanism that depends upon activation of protein kinase A.
Increased intracellular calcium reinforce some cyclic AMP mediated actions of glucagon, particularly on glycogenolysis.
Ketogenesis
Ketogenesis is the process by which ketone bodies are produced as a result of fatty acid breakdown.
Glucagon control the ketogenesis
The same reaction that inhibits fatty acid synth
of cigarette smoke-induced proinflammatory mediator release via sirtuin-NF-κB RelA/p65 interaction. Cigarette smoke decreased sirtuin levels and caused posttranslational modification by reactive aldehydes/reactive oxygen species/RNS, thereby disrupting SIRT1-RelA/p65 complex via phosphorylation (P) and acetylation (Ac) of RelA/p65. This leads to increased release of pro-inflammatory mediators.
of pure natural peptide must reproduce the effect on target organ
③ Synthetic peptide should reproduce the effect found with natural peptide
④ Circulating concentration of peptide that cause stimulation oftarget organ should be the same
⑤ The assay must not measure biologically inactive degradation product
⑥ It should be possible to prevent the physiologic response by removing the pe
In 2006 to 2007, Hayakawa
Micromolar 수준의 potency로 PI3K 억제효과를 가지는 생리활성물질(Hit compound) 발견
->한자리수의 nanomolar lead(선도물질) 개발
Broad spectrum PI3K inhibitor 로서 쓰임.
PI 103은 세포투과적.
ATP 와 경쟁하는 경쟁적 kinase inhibitor 이다. 일반적으로 100nM에 효과나타남
PI103은 Class Ia PI 30kinase isoform,