mTORC1 and the regulation of skeletal muscle anabolism and mass
... activity and nutrition are the 2 most important environmental factors that can affect muscle health. At the molecular level, the mammalian target of rapamycin complex 1 (mTORC1) is a critical signalling complex that regulates muscle mass. In response to nutrition and resistance exercise, increased m ...
... activity and nutrition are the 2 most important environmental factors that can affect muscle health. At the molecular level, the mammalian target of rapamycin complex 1 (mTORC1) is a critical signalling complex that regulates muscle mass. In response to nutrition and resistance exercise, increased m ...
Nutrients and growth factors in mTORC1 activation
... Alejo Efeyan and David M. Sabatini1 Whitehead Institute for Biomedical Research, 9 Cambridge Center, Cambridge, MA 02142, U.S.A., Broad Institute of Harvard and MIT, 7 Cambridge Center, Cambridge, MA 02142, U.S.A., Department of Biology, Massachusetts Institute of Technology (MIT), Cambridge, MA 021 ...
... Alejo Efeyan and David M. Sabatini1 Whitehead Institute for Biomedical Research, 9 Cambridge Center, Cambridge, MA 02142, U.S.A., Broad Institute of Harvard and MIT, 7 Cambridge Center, Cambridge, MA 02142, U.S.A., Department of Biology, Massachusetts Institute of Technology (MIT), Cambridge, MA 021 ...
Cellular Pathophysiology of Insulin Resistance
... Poretsky LO, ed. New York, Springer,2009, p. 75-87. ...
... Poretsky LO, ed. New York, Springer,2009, p. 75-87. ...
EGFR TYROSINE KINASE TARGETED COMPOUNDS: IN VITRO
... aimed at further exploration of the SAR of this novel template, led to the discovery of highly selective compounds that target EGFR. Benzothiazoles act via competing with ATP for binding at the catalytic domain of EGFR-TK (Noolvi et al., 2012). The characteristic features of ATP binding site are; ad ...
... aimed at further exploration of the SAR of this novel template, led to the discovery of highly selective compounds that target EGFR. Benzothiazoles act via competing with ATP for binding at the catalytic domain of EGFR-TK (Noolvi et al., 2012). The characteristic features of ATP binding site are; ad ...
Document
... GAT1, RTG13, and MSN24 inactive. • GLN3 is an activator of genes involved in ammonium assimilation. ...
... GAT1, RTG13, and MSN24 inactive. • GLN3 is an activator of genes involved in ammonium assimilation. ...
NOVEL FAK-SELECTIVE INHIBITORS
... FAK is a non-receptor tyrosine kinase which is overexpressed (through either gene amplification or increased levels of protein expression), or over-activated in many human cancers (including solid tumours and acute myelogenous leukaemia (AML)). Increased levels of FAK and/or phosphorylated FAK are o ...
... FAK is a non-receptor tyrosine kinase which is overexpressed (through either gene amplification or increased levels of protein expression), or over-activated in many human cancers (including solid tumours and acute myelogenous leukaemia (AML)). Increased levels of FAK and/or phosphorylated FAK are o ...
Alex A. Adjei, Roswell Park Cancer Institute, Buffalo, NY
... –Specification about time interval between prior therapy and initiation of study treatment ...
... –Specification about time interval between prior therapy and initiation of study treatment ...
Cylene Builds on Success, Presents Second CK2 Inhibitor at AACR
... an oral inhibitor is safe and effective, resulting in inhibition of CK2 and CK2-driven pathways, inhibition of tumor-based markers and reductions in tumor size. “We are delighted to showcase the promising preclinical profile of our second generation inhibitor, CX-8184, demonstrating our commitment t ...
... an oral inhibitor is safe and effective, resulting in inhibition of CK2 and CK2-driven pathways, inhibition of tumor-based markers and reductions in tumor size. “We are delighted to showcase the promising preclinical profile of our second generation inhibitor, CX-8184, demonstrating our commitment t ...
3rd year antidepressant part 22011-09
... Metabolism: P450 through glucuronide or sulfate conjugation They are enzyme inhibitor Weak inhibitors < Sertraline, Citalopram interaction Strong inhibitors > Fluoxetine, Paroxetine metabolism of TCA, neuroleptic, some antiarrhythmic, β-blockers. Primarily excreted through kidney; not paro ...
... Metabolism: P450 through glucuronide or sulfate conjugation They are enzyme inhibitor Weak inhibitors < Sertraline, Citalopram interaction Strong inhibitors > Fluoxetine, Paroxetine metabolism of TCA, neuroleptic, some antiarrhythmic, β-blockers. Primarily excreted through kidney; not paro ...
Peptide microarrays for detailed, high-throughput
... was used for real-time detection of protein kinase A (PKA) for substrate identification and kinetic characterization of PKA (figure 1). Figure 2 shows a time course of peptide phosphorylation over 50 minutes. In this assay the IC50 of three PKA inhibitors, AMP–PNP, staurosporin, and PKA inhibitor pe ...
... was used for real-time detection of protein kinase A (PKA) for substrate identification and kinetic characterization of PKA (figure 1). Figure 2 shows a time course of peptide phosphorylation over 50 minutes. In this assay the IC50 of three PKA inhibitors, AMP–PNP, staurosporin, and PKA inhibitor pe ...
Materials and Methods S1
... inhibitor. < 1 when binding of one supported the other, > 1 when binding of one impedes the other and when = 1, binding of one has no effect on the other. For a mixed-type noncompetitive inhibitor, is either < 1 or > 1. For classical noncompetitive inhibitors, α = 1, thus, Ki’ = Ki ...
... inhibitor. < 1 when binding of one supported the other, > 1 when binding of one impedes the other and when = 1, binding of one has no effect on the other. For a mixed-type noncompetitive inhibitor, is either < 1 or > 1. For classical noncompetitive inhibitors, α = 1, thus, Ki’ = Ki ...
Chapter 16 Cholinesterase Inhibitors
... • Likely to elicit substantial muscarinic responses • May need to administer atropine (muscarinic antagonist) ...
... • Likely to elicit substantial muscarinic responses • May need to administer atropine (muscarinic antagonist) ...
Anticoagulants
... predictable; subcutaneous injection twice daily; use preferred over unfractionated heparin ...
... predictable; subcutaneous injection twice daily; use preferred over unfractionated heparin ...
TyrPhos12
... Src homology (SH)2 and SH3 domains • Tyr phosphorylation allows recruitment of proteins that possess domains that bind to specific peptide sequences that encompass a phosphorylated tyr and which activating a variety of signalling pathways. • Such domains include SH2 and SH3 and P-tyr ...
... Src homology (SH)2 and SH3 domains • Tyr phosphorylation allows recruitment of proteins that possess domains that bind to specific peptide sequences that encompass a phosphorylated tyr and which activating a variety of signalling pathways. • Such domains include SH2 and SH3 and P-tyr ...
Cardiac Energy Dependence on Glucose Increases
... Methods and Results-—Metabolomics analysis identified 60 metabolites altered in Acsl1H/ hearts, including 6 related to glucose metabolism and 11 to cysteine and glutathione pathways. Concurrently, global cardiac transcriptional analysis revealed differential expression of 568 genes in Acsl1H/ hea ...
... Methods and Results-—Metabolomics analysis identified 60 metabolites altered in Acsl1H/ hearts, including 6 related to glucose metabolism and 11 to cysteine and glutathione pathways. Concurrently, global cardiac transcriptional analysis revealed differential expression of 568 genes in Acsl1H/ hea ...
article in press - Biochemistry
... arresting nonessential ATP-utilizing functions and stimulating available ATP-generating pathways. The fact that the ADP/ATP ratio in many cell types is maintained within a narrow range regardless of nutrient availability, hypoxia or cellular activity indicates the existence of a very effective and r ...
... arresting nonessential ATP-utilizing functions and stimulating available ATP-generating pathways. The fact that the ADP/ATP ratio in many cell types is maintained within a narrow range regardless of nutrient availability, hypoxia or cellular activity indicates the existence of a very effective and r ...
Implications for Cancer Biology
... Thomas, 2001). The role for PI3K in mediating signals from insulin to these effectors became evident from a combination of biochemical and chemical genetic experiments. Engagement of insulin receptor by insulin normally leads to recruitment of the IRS-1 protein, which subsequently recruits PI3K (Fig ...
... Thomas, 2001). The role for PI3K in mediating signals from insulin to these effectors became evident from a combination of biochemical and chemical genetic experiments. Engagement of insulin receptor by insulin normally leads to recruitment of the IRS-1 protein, which subsequently recruits PI3K (Fig ...
mTORC1 Activates SREBP-1c and Uncouples Lipogenesis From Gluconeogenesis Please share
... the major driving forces leading to hyperglycemia. Paradoxically, high hepatic levels of SREBP-1c mRNA expression and nuclear accumulation have been observed in type 2 diabetic mouse models and are likely to contribute to the enhanced hepatic lipogenesis found in these animals (7). The molecular mec ...
... the major driving forces leading to hyperglycemia. Paradoxically, high hepatic levels of SREBP-1c mRNA expression and nuclear accumulation have been observed in type 2 diabetic mouse models and are likely to contribute to the enhanced hepatic lipogenesis found in these animals (7). The molecular mec ...
Amino acids and mTORC1: from lysosomes to disease
... RagA/BGTP–RagC/DGDP mutants display maximum binding to mTORC1; they also potently activate mTORC1 signaling and render it insensitive to amino acid starvation. Conversely, the ‘inactive’ RagA/BGDP–RagC/DGTP mutants are unable to bind to mTORC1 and potently suppress mTORC1 activity, even in the prese ...
... RagA/BGTP–RagC/DGDP mutants display maximum binding to mTORC1; they also potently activate mTORC1 signaling and render it insensitive to amino acid starvation. Conversely, the ‘inactive’ RagA/BGDP–RagC/DGTP mutants are unable to bind to mTORC1 and potently suppress mTORC1 activity, even in the prese ...
Regulation of T Lymphocyte Metabolism
... Rapamycin is also a potent T cell immunosuppressant, indicating the importance of mTOR function during T cell activation (33). mTOR regulates protein synthesis via multiple phosphorylation targets, including p70S6 kinase, a regulator of ribosome function, and 4E-BP1, an inhibitor of translation (32) ...
... Rapamycin is also a potent T cell immunosuppressant, indicating the importance of mTOR function during T cell activation (33). mTOR regulates protein synthesis via multiple phosphorylation targets, including p70S6 kinase, a regulator of ribosome function, and 4E-BP1, an inhibitor of translation (32) ...
a proprietary enzyme blend designed
... the individual amino acids themselves, which are then absorbed into the body for use in a variety of functions, including building hormones and neurotransmitters, and also promoting immune function plus tissue repair.10-13 Some of the most important amino acids for skeletal muscle growth, and thus s ...
... the individual amino acids themselves, which are then absorbed into the body for use in a variety of functions, including building hormones and neurotransmitters, and also promoting immune function plus tissue repair.10-13 Some of the most important amino acids for skeletal muscle growth, and thus s ...
Molecular Pathways: Fatty Acid Synthase
... following binding to its cognate receptor. FASN inhibition not only can reduce this important posttranslation modification of these proteins, but also may have more specific effects on the activation of b-catenin alone. By disrupting the classical Wnt/ b-catenin pathway, expression of important tumor ...
... following binding to its cognate receptor. FASN inhibition not only can reduce this important posttranslation modification of these proteins, but also may have more specific effects on the activation of b-catenin alone. By disrupting the classical Wnt/ b-catenin pathway, expression of important tumor ...
Epidermal Growth Factor Receptor Inhibitors in Clinical Trials
... hindering autophosphorylation, and induce tumor stasis and even tumor regression in some tumor xenograft models. In addition to their shared mechanism of action, these agents are also administered orally on chronic schedules and have a similar spectrum of toxicity, with diarrhea and skin rash being ...
... hindering autophosphorylation, and induce tumor stasis and even tumor regression in some tumor xenograft models. In addition to their shared mechanism of action, these agents are also administered orally on chronic schedules and have a similar spectrum of toxicity, with diarrhea and skin rash being ...
COX 2 Inhibitor Interactions - Center for Selective C–H
... Other References Selective COX-2 inhibitors by Knaus et al. and COX inhibitory effects by Amini et al. ...
... Other References Selective COX-2 inhibitors by Knaus et al. and COX inhibitory effects by Amini et al. ...