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Long-chain acyl-CoA esters inhibit phosphorylation of AMP-activated protein kinase at threonine-172 by LKB1/STRAD/MO25.
TLDR
The results demonstrate that the AMPKK activity of LKB1/STRAD/MO25 is substrate specific and distinct from the kinase activity of SOTA, and demonstrate that long-chain acyl-CoA esters inhibited phosphorylation of AMPK by the recombinant AMPK kinase (AMPKK) L KB1/ STRAD/ MO25 in a concentration-dependent manner. Expand
Endurance training increases skeletal muscle LKB1 and PGC-1alpha protein abundance: effects of time and intensity.
TLDR
It is demonstrated that LKB1 and PGC-1alpha protein abundances increase with endurance and interval training similarly to citrate synthase, which may function to maintain the training-induced increases in mitochondrial mass. Expand
Evidence against regulation of AMP-activated protein kinase and LKB1/STRAD/MO25 activity by creatine phosphate.
TLDR
It is found that creatine phosphate did not inhibit phosphorylation of either recombinant or purified rat liver AMPK by LKB1, and Creatine phosphate may indirectly modulate AMPK activity by replenishing ATP at the onset of muscle contraction. Expand
AMP-activated protein kinase kinase activity and phosphorylation of AMP-activated protein kinase in contracting muscle of sedentary and endurance-trained rats.
TLDR
The results suggest that AMPKK is activated during electrical stimulation of both trained and nontrained muscle by mechanisms other than covalent modification. Expand
Endurance training increases LKB1 and MO25 protein but not AMP-activated protein kinase kinase activity in skeletal muscle.
TLDR
In conclusion, endurance training markedly increased skeletal muscle L KB1 and MO25 protein without increasing AMPKK activity, suggesting LKB1 may be playing multiple roles in skeletal muscle adaptation to endurance training. Expand
A small molecule inhibitor of Pim-1 kinase with activity in both hematological and solid tumor malignancies
TLDR
The details of the biochemical and cell-based assay results as well as the activity in tumor xenograft models of the Pim-1 kinase inhibitors are presented. Expand
Abstract #2013: Discovery of SGI-1776, a potent and selective Pim-1 kinase inhibitor
TLDR
It is suggested that Pim-1 may be a promising drug target for development of anticancer agents after large-scale virtual screening and initial SAR studies revealed that the introduction of hydrophobic moiety at R1 and small ring substituent groups with 1 or 2 -CH2 spacer at the 6-amine position are vital for the PIM-1 kinase inhibition. Expand
MP470 suppresses repair of double-strand breaks following treatment with DNA-damaging agents.
TLDR
It is shown that MP470 inhibits the repair of DNA double strand breaks in cells following treatment with DNA damaging agents, such as etoposide, a topoisomerase II inhibitor, which strengthens the rationale for combining MP470 with DNA damaged agents. Expand
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