cover_article_1135_en_US
... In the present study, we reported a novel AKT1 inhibitor DC120 and its antitumor mechanism and clarified resistant mechanism of the ATP-competitive AKT inhibitors. Unexpectedly, AKT inhibitors both DC120 and GDC0068 induced hyperphosphorylation of AKT, which might be common characters of the ATP-com ...
... In the present study, we reported a novel AKT1 inhibitor DC120 and its antitumor mechanism and clarified resistant mechanism of the ATP-competitive AKT inhibitors. Unexpectedly, AKT inhibitors both DC120 and GDC0068 induced hyperphosphorylation of AKT, which might be common characters of the ATP-com ...
Role of TMEM127 in the endomembrane system and mTOR
... restraining mTOR. mTOR is an enzyme that controls many important functions of the cell, including growth, survival, protein production, response to nutrients and various stresses. Many cancers have abnormally increased mTOR function. Thus, understanding the function of genes and proteins that contro ...
... restraining mTOR. mTOR is an enzyme that controls many important functions of the cell, including growth, survival, protein production, response to nutrients and various stresses. Many cancers have abnormally increased mTOR function. Thus, understanding the function of genes and proteins that contro ...
P023 Brk and mTOR signalling: potential involvement in Taxol
... is due to the development of distal metastases and the acquisition of resistance to chemotherapeutic agents. There is a scientific and clinical need to understand the alterations in cellular signalling pathways that could contribute to chemotherapeutic resistance in breast cancer. One such potential ...
... is due to the development of distal metastases and the acquisition of resistance to chemotherapeutic agents. There is a scientific and clinical need to understand the alterations in cellular signalling pathways that could contribute to chemotherapeutic resistance in breast cancer. One such potential ...
Targeting protein synthesis in cancer cells (PDF Available)
... mRNA translation into protein. Ribosome recruitment at the mRNA 5’ end is actually controlled by the mRNA 5’ cap binding protein eIF4E (eukaryotic translation initiation factor 4E) whose activity is inhibited by the hypophosphorylated forms of 4E-BPs (eIF4E-binding proteins 1 and 2) [1]. Upon mitoge ...
... mRNA translation into protein. Ribosome recruitment at the mRNA 5’ end is actually controlled by the mRNA 5’ cap binding protein eIF4E (eukaryotic translation initiation factor 4E) whose activity is inhibited by the hypophosphorylated forms of 4E-BPs (eIF4E-binding proteins 1 and 2) [1]. Upon mitoge ...
THE MAMMALIAN TARGET OF RAPAMYCIN (MTOR) AS A
... characterization of these compounds suggest they partially inhibit mTOR through modulation of an Akt regulated target TSC2. Taken together, these data suggest that persistent activation of Akt confers sensitivity to mTOR inhibitors. The effect of mTOR inhibition on protein expression is not restrict ...
... characterization of these compounds suggest they partially inhibit mTOR through modulation of an Akt regulated target TSC2. Taken together, these data suggest that persistent activation of Akt confers sensitivity to mTOR inhibitors. The effect of mTOR inhibition on protein expression is not restrict ...
Dissecting the mechanisms of mTOR activation. Supervisor: Dr. Zita
... Alzheimer's disease is the most common form of dementia in old age. Amyloid Precursor Protein (APP) plays a key role in Alzheimer's disease (AD). Mutations in APP gene cause an early onset or familial form of AD. The aberrant processing of APP by secretases is thought to be a key driver in AD as fam ...
... Alzheimer's disease is the most common form of dementia in old age. Amyloid Precursor Protein (APP) plays a key role in Alzheimer's disease (AD). Mutations in APP gene cause an early onset or familial form of AD. The aberrant processing of APP by secretases is thought to be a key driver in AD as fam ...
Phospho-MTOR(T1870) Blocking Peptide
... growth and survival in response to hormones, growth factors, nutrients, energy and stress signals. MTOR directly or indirectly regulates the phosphorylation of at least 800 proteins. Functions as part of 2 structurally and functionally distinct signaling complexes mTORC1 and mTORC2 (mTOR complex 1 ...
... growth and survival in response to hormones, growth factors, nutrients, energy and stress signals. MTOR directly or indirectly regulates the phosphorylation of at least 800 proteins. Functions as part of 2 structurally and functionally distinct signaling complexes mTORC1 and mTORC2 (mTOR complex 1 ...
Thilo HAGEN
... Our laboratory is currently interested in a number of aspects related to cancer biology and human metabolism. These include understanding basic mechanisms that underlie cellular signaling and energy metabolism. Another emphasis in our lab is to identify new therapeutic strategies targeting the cellu ...
... Our laboratory is currently interested in a number of aspects related to cancer biology and human metabolism. These include understanding basic mechanisms that underlie cellular signaling and energy metabolism. Another emphasis in our lab is to identify new therapeutic strategies targeting the cellu ...
Immunosuppressive drugs: the first 50 years and a glance forward
... Cyclophosphamide metabolites alkylate DNA bases and preferentially suppress immune responses mediated by B-lymphocytes. Methotrexate and its polyglutamate derivatives suppress inflammatory responses through release of adenosine; they suppress immune responses by inducing the apoptosis of activated T ...
... Cyclophosphamide metabolites alkylate DNA bases and preferentially suppress immune responses mediated by B-lymphocytes. Methotrexate and its polyglutamate derivatives suppress inflammatory responses through release of adenosine; they suppress immune responses by inducing the apoptosis of activated T ...
Mapping Inhibitor Interactions and Conformational Space of the
... The problem addressed here is to find potent and cancer-selective inhibitors of prevalidated cancer drug targets. We have chosen to find inhibitors of the MAP3K TAO2 because its elimination in a NSCLC (non-small-cell lung carcinoma) cell line killed the cells. TAO2 has been shown to participate in t ...
... The problem addressed here is to find potent and cancer-selective inhibitors of prevalidated cancer drug targets. We have chosen to find inhibitors of the MAP3K TAO2 because its elimination in a NSCLC (non-small-cell lung carcinoma) cell line killed the cells. TAO2 has been shown to participate in t ...
Case Report - Thalidomide and hyperkalemia
... Current development of mTOR inhibitors Conclusion ...
... Current development of mTOR inhibitors Conclusion ...
Dr. Bryan Ballif identifies phosphorylation sites on key proteins regulating cell growth and proliferation.
... However, determining precisely where a protein is phosphorylated, and understanding the effect of phosphorylation at a given amino acid requires exacting instrumentation and skilled analysis. Dr. Ballif, working with a colleague, Dr. Diane Fingar, from the University of Mich ...
... However, determining precisely where a protein is phosphorylated, and understanding the effect of phosphorylation at a given amino acid requires exacting instrumentation and skilled analysis. Dr. Ballif, working with a colleague, Dr. Diane Fingar, from the University of Mich ...
Roles of the mammalian target of rapamycin
... mTOR-KIs inhibit their synthesis more strongly than does rapamycin, in line with the effects of these compounds on overall protein synthesis rates. For proteins known to be encoded by 5 -TOP mRNAs, such as ribosomal proteins, rapamycin inhibited synthesis quite strongly (typically by 20–50%), which ...
... mTOR-KIs inhibit their synthesis more strongly than does rapamycin, in line with the effects of these compounds on overall protein synthesis rates. For proteins known to be encoded by 5 -TOP mRNAs, such as ribosomal proteins, rapamycin inhibited synthesis quite strongly (typically by 20–50%), which ...
Inhibitors
... Complementary to ATG start, 5’UTR or splice junction Prevents translation or splicing ...
... Complementary to ATG start, 5’UTR or splice junction Prevents translation or splicing ...
DF-Bio714-2
... mTOR (Mammalian Target of Rapamycin) •Regulator of cell proliferation and cell growth •Responds to nutrients (amino acids, glucose, lipids?) •Regulates initiation of protein synthesis - including Myc •Inhibited by rapamycin •There are two mTOR complexes - mTORC1 and mTORC2 •Phosphatidic acid (PA), ...
... mTOR (Mammalian Target of Rapamycin) •Regulator of cell proliferation and cell growth •Responds to nutrients (amino acids, glucose, lipids?) •Regulates initiation of protein synthesis - including Myc •Inhibited by rapamycin •There are two mTOR complexes - mTORC1 and mTORC2 •Phosphatidic acid (PA), ...
Interpretation of bafilomycin, pH neutralizing or protease inhibitor
... levels with experiments done without using these drugs.1 MTOR (mechanistic target of rapamycin) is a serine/threonine kinase that integrates multiple signals such as growth factor abundance with intracellular amino acid and ATP levels to coordinate cell growth and autophagy. MTOR promotes translatio ...
... levels with experiments done without using these drugs.1 MTOR (mechanistic target of rapamycin) is a serine/threonine kinase that integrates multiple signals such as growth factor abundance with intracellular amino acid and ATP levels to coordinate cell growth and autophagy. MTOR promotes translatio ...
TGF-beta story - Department Of Biological Sciences Hunter
... cell cycle called START that is late in G1 where cells evaluate whether there is sufficient nutrition to complete cell division ...
... cell cycle called START that is late in G1 where cells evaluate whether there is sufficient nutrition to complete cell division ...
Cellular Metabolism Pathways
... PFK2. AMPK negatively regulates several proteins central to ATP consuming processes such as TORC2, glycogen synthase, SREBP-1 and TSC2, resulting in the downregulation or inhibition of gluconeogenesis, glycogen, lipid and protein synthesis. Due to its role as a central regulator of both lipid and gl ...
... PFK2. AMPK negatively regulates several proteins central to ATP consuming processes such as TORC2, glycogen synthase, SREBP-1 and TSC2, resulting in the downregulation or inhibition of gluconeogenesis, glycogen, lipid and protein synthesis. Due to its role as a central regulator of both lipid and gl ...
350-Cell Cycle-DF - Department Of Biological Sciences Hunter
... organisms determine whether it is appropriate for a cell to divide During G1-ps, cells that have been given the green light to divide, determine whether they have the means/raw materials to double the mass of a cell, Replicate its genome, and divide into two daughter cells The late G1 “Metabolic Che ...
... organisms determine whether it is appropriate for a cell to divide During G1-ps, cells that have been given the green light to divide, determine whether they have the means/raw materials to double the mass of a cell, Replicate its genome, and divide into two daughter cells The late G1 “Metabolic Che ...
The Expanding Role of the mammalian Target of Rapamycin
... the less enthusiastic and perhaps conflicting results of mTOR inhibition by rapamycin in clinical trials [27]. Recently, a newly developed class of mTOR inhibitors, termed the ATP-competitive mTOR kinase inhibitors, have been shown to inhibit both mTORC1 and mTORC2 complexes [28,29]. These mTOR kina ...
... the less enthusiastic and perhaps conflicting results of mTOR inhibition by rapamycin in clinical trials [27]. Recently, a newly developed class of mTOR inhibitors, termed the ATP-competitive mTOR kinase inhibitors, have been shown to inhibit both mTORC1 and mTORC2 complexes [28,29]. These mTOR kina ...
chang-hung-chou-china-medical-university-taiwan
... Lung cancer and Apoptosis Lung cancer is the second most frequent type of cancer Nonsmall-cell lung cancer (NSCLC) accounts for ∼80% of primary lung cancers Apoptosis, a major form of cell death, is regulated ...
... Lung cancer and Apoptosis Lung cancer is the second most frequent type of cancer Nonsmall-cell lung cancer (NSCLC) accounts for ∼80% of primary lung cancers Apoptosis, a major form of cell death, is regulated ...
Design and Synthesis of Small Molecule Inhibitors of
... Endothelial Lipase (EL) is a recently discovered member of the triglyceride lipase gene family whose activity is negatively correlated with levels of HDL-cholesterol in vivo. Disruption of EL activity, either through antibody directed inhibition, or gene knock-out, has been shown to increase levels ...
... Endothelial Lipase (EL) is a recently discovered member of the triglyceride lipase gene family whose activity is negatively correlated with levels of HDL-cholesterol in vivo. Disruption of EL activity, either through antibody directed inhibition, or gene knock-out, has been shown to increase levels ...
p38 MAP Kinase Inhibitor - Lilly Oncology Pipeline USA
... p38 mitogen-activated protein (MAP) kinase is activated in response to inflammatory stimuli (eg, tumor necrosis factor, interleukin-6), growth factors (eg, vascular endothelial growth factor, fibroblast growth factor, insulin-like growth factor), and cellular stress (eg, chemotherapeutic challenge). ...
... p38 mitogen-activated protein (MAP) kinase is activated in response to inflammatory stimuli (eg, tumor necrosis factor, interleukin-6), growth factors (eg, vascular endothelial growth factor, fibroblast growth factor, insulin-like growth factor), and cellular stress (eg, chemotherapeutic challenge). ...
... • The PI3K/Akt/mTOR pathway is an important signaling pathway for many cellular regulation functions such as cell proliferation, angiogenesis and vascular permeability – Significant therapeutic opportunities for pathway signaling – Agents in development affect different targets • PI3K inhibitors • A ...