Relevant to neuronal activity, AMPKmediated changes in long-term potentiation are mTOR-dependent. Differences in acute seizure test profiles between three different treatments that affect AMPK activity support the hypothesis that downstream effects of neuronal mTOR inhibition likely depend on additional factors specific to each intervention. Rapamycin is known to bind FKBP12 to specifically inhibit mTORC1activity. Evidence… Continue reading It appears that rapamycin is more effective in seizure models where mTOR activity is significantly increased at baseline
Category: Bioactive Compound Library
M2 protein inhibitors and demonstrated for the two new scaffolds thus these are considered novel findings
On the basis of their selectivity for PKCs and CAMKs, we chose to primarily focus on the 4-azaindole series of inhibitors, since they clearly displayed greater selectivity for PKD1 than the quinolinylmethylenethiazolinone derivative. 4-Azaindoles have previously been developed and characterized as inhibitors of p38a/b by Trejo et al.. Compounds 140 and 139 have been designed… Continue reading M2 protein inhibitors and demonstrated for the two new scaffolds thus these are considered novel findings
Despite substantial progress in ligand docking one of the major limitations remains the inaccuracy of the scoring functions used
Recently, selective inhibitors for CDK4 have gained substantial interest. For example the orally active small molecule PD0332991, which induces G1 arrest in primary myeloma cells, prevents tumor growth by specific inhibition of CDK4/6 and is now in Phase 2 clinical trials. The natural compound fascaplysin, originally isolated from the sponge Fascaplysinopsis Bergquist, is a kinase… Continue reading Despite substantial progress in ligand docking one of the major limitations remains the inaccuracy of the scoring functions used
Autophagic suppression is not the main cause of the CE increase induced by CHX with a phospholipid monolayer
In white adipocytes, the lipid ester core consists almost exclusively of triglycerides, whereas in many non-adipocytes LDs contain both TG and cholesterol esters in various ratios. TG synthesis is facilitated in the presence of excess fatty acids. In many non-adipocytes in culture, only a small number of LDs exist under normal conditions, but the addition… Continue reading Autophagic suppression is not the main cause of the CE increase induced by CHX with a phospholipid monolayer
Confirmed persistent target inhibition after HD-TKI pulseexposure with no evidence of BCR-ABL or STAT5 rephosphorylation
RAMs might determine a phenotypic drug-resistance without altering the secondary RNA-structure stability. Chronic myeloid leukemia is characterized by the constitutively activated tyrosine kinase BCR-ABL. Treatment of CML with the small molecule tyrosine kinase inhibitor imatinib stands as a paradigm for clinical efficacy of targeted small molecule therapy in malignant disease. Imatinib inhibits BCRABL tyrosine kinase… Continue reading Confirmed persistent target inhibition after HD-TKI pulseexposure with no evidence of BCR-ABL or STAT5 rephosphorylation