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Publication DateJournal of Cellular Biochemistry, ISSN 0730-2312, 06/2015, Volume 116, Issue 6, pp. 1019 - 1027
ABSTRACT Lung adenocarcinoma cells harboring epidermal growth factor receptor (EGFR) mutations are sensitive to EGFR tyrosine kinase inhibitor (TKI). Acquired...
DRUG RESISTANCE | GEFITINIB | γ SECRETASE INHIBITOR | LUNG CANCER | CELLS | gamma SECRETASE INHIBITOR | BIOCHEMISTRY & MOLECULAR BIOLOGY | TARGETING NOTCH | ACQUIRED-RESISTANCE | DRUG-RESISTANCE | CELL BIOLOGY | TYROSINE KINASE INHIBITORS | GROWTH-FACTOR RECEPTOR | THERAPY | NOTCH SIGNALING PATHWAY | ACTIVATING MUTATIONS | Immunohistochemistry | Cell Survival - drug effects | Lung Neoplasms - drug therapy | Apoptosis - drug effects | Lung Neoplasms - metabolism | Phosphatidylinositol 3-Kinases - metabolism | Oxadiazoles - therapeutic use | Animals | Sulfonamides - therapeutic use | Quinazolines - therapeutic use | Cell Line, Tumor | Receptor, Epidermal Growth Factor - antagonists & inhibitors | Female | Mice | Mice, Inbred BALB C | Amyloid Precursor Protein Secretases - antagonists & inhibitors | Proto-Oncogene Proteins c-akt - metabolism
DRUG RESISTANCE | GEFITINIB | γ SECRETASE INHIBITOR | LUNG CANCER | CELLS | gamma SECRETASE INHIBITOR | BIOCHEMISTRY & MOLECULAR BIOLOGY | TARGETING NOTCH | ACQUIRED-RESISTANCE | DRUG-RESISTANCE | CELL BIOLOGY | TYROSINE KINASE INHIBITORS | GROWTH-FACTOR RECEPTOR | THERAPY | NOTCH SIGNALING PATHWAY | ACTIVATING MUTATIONS | Immunohistochemistry | Cell Survival - drug effects | Lung Neoplasms - drug therapy | Apoptosis - drug effects | Lung Neoplasms - metabolism | Phosphatidylinositol 3-Kinases - metabolism | Oxadiazoles - therapeutic use | Animals | Sulfonamides - therapeutic use | Quinazolines - therapeutic use | Cell Line, Tumor | Receptor, Epidermal Growth Factor - antagonists & inhibitors | Female | Mice | Mice, Inbred BALB C | Amyloid Precursor Protein Secretases - antagonists & inhibitors | Proto-Oncogene Proteins c-akt - metabolism
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Loading RightsBBA - Biomembranes, ISSN 0005-2736, 12/2013, Volume 1828, Issue 12, pp. 2898 - 2907
γ-Secretase is a fascinating, multi-subunit, intramembrane cleaving protease that is now being considered as a therapeutic target for a number of diseases....
γ-Secretase inhibitor | Alzheimer's disease | γ-Secretase modulator | Cancer | SIGNAL PEPTIDE PEPTIDASE | BIOCHEMISTRY & MOLECULAR BIOLOGY | TRANSMEMBRANE DOMAIN | AMYLOID PRECURSOR PROTEIN | A-BETA PEPTIDES | BIOPHYSICS | NONSTEROIDAL ANTIINFLAMMATORY DRUGS | INTRAMEMBRANE CLEAVAGE | ACUTE LYMPHOBLASTIC-LEUKEMIA | IN-VIVO | gamma-Secretase modulator | TRANSGENIC MOUSE MODEL | gamma-Secretase inhibitor | FAMILIAL ALZHEIMER-DISEASE | Amyloid beta-Protein Precursor - chemistry | Humans | Substrate Specificity | Structure-Activity Relationship | Protein Subunits - metabolism | Alzheimer Disease - pathology | Protease Inhibitors - pharmacology | Proteolysis | Amyloid beta-Protein Precursor - metabolism | Drug Design | Binding Sites | Signal Transduction | Alzheimer Disease - drug therapy | Neoplasms - enzymology | Protease Inhibitors - chemistry | Clinical Trials as Topic | Alzheimer Disease - enzymology | Amyloid Precursor Protein Secretases - chemistry | Neoplasms - drug therapy | Amyloid Precursor Protein Secretases - metabolism | Protein Binding | Protein Subunits - antagonists & inhibitors | Protein Subunits - chemistry | Amyloid Precursor Protein Secretases - antagonists & inhibitors | Neoplasms - pathology | Index Medicus
γ-Secretase inhibitor | Alzheimer's disease | γ-Secretase modulator | Cancer | SIGNAL PEPTIDE PEPTIDASE | BIOCHEMISTRY & MOLECULAR BIOLOGY | TRANSMEMBRANE DOMAIN | AMYLOID PRECURSOR PROTEIN | A-BETA PEPTIDES | BIOPHYSICS | NONSTEROIDAL ANTIINFLAMMATORY DRUGS | INTRAMEMBRANE CLEAVAGE | ACUTE LYMPHOBLASTIC-LEUKEMIA | IN-VIVO | gamma-Secretase modulator | TRANSGENIC MOUSE MODEL | gamma-Secretase inhibitor | FAMILIAL ALZHEIMER-DISEASE | Amyloid beta-Protein Precursor - chemistry | Humans | Substrate Specificity | Structure-Activity Relationship | Protein Subunits - metabolism | Alzheimer Disease - pathology | Protease Inhibitors - pharmacology | Proteolysis | Amyloid beta-Protein Precursor - metabolism | Drug Design | Binding Sites | Signal Transduction | Alzheimer Disease - drug therapy | Neoplasms - enzymology | Protease Inhibitors - chemistry | Clinical Trials as Topic | Alzheimer Disease - enzymology | Amyloid Precursor Protein Secretases - chemistry | Neoplasms - drug therapy | Amyloid Precursor Protein Secretases - metabolism | Protein Binding | Protein Subunits - antagonists & inhibitors | Protein Subunits - chemistry | Amyloid Precursor Protein Secretases - antagonists & inhibitors | Neoplasms - pathology | Index Medicus
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Loading RightsCellular Signalling, ISSN 0898-6568, 01/2014, Volume 26, Issue 1, pp. 149 - 161
T-cell acute lymphoblastic leukemia (T-ALL) is characterized as a high-risk stratified disease associated with frequent relapse, chemotherapy resistance, and a...
mTOR | AKT | γ-Secretase inhibitor resistance | Notch1 | Leukemia | Protein phosphatase 2A | MTOR | MAMMALIAN TARGET | PHOSPHATIDYLINOSITOL 3-KINASE/AKT | TRANSCRIPTIONAL ACTIVITY | C-MYC | ACUTE MYELOID-LEUKEMIA | OF-FUNCTION MUTATIONS | CELL BIOLOGY | SCFFBW7 UBIQUITIN LIGASE | gamma-Secretase inhibitor resistance | TUMOR-SUPPRESSOR | PROGNOSTIC-SIGNIFICANCE | Precursor Cell Lymphoblastic Leukemia-Lymphoma - drug therapy | Amyloid Precursor Protein Secretases - metabolism | Animals | Signal Transduction - drug effects | Receptors, Notch - metabolism | Humans | Enzyme Inhibitors - pharmacology | Precursor Cell Lymphoblastic Leukemia-Lymphoma - enzymology | Amyloid Precursor Protein Secretases - antagonists & inhibitors | Precursor Cell Lymphoblastic Leukemia-Lymphoma - pathology | Enzyme Inhibitors - therapeutic use | Drug Resistance, Neoplasm - drug effects | Mutations | Therapy | Cellular | Control | Inhibitors | Activation | Inactivation | Leukemias
mTOR | AKT | γ-Secretase inhibitor resistance | Notch1 | Leukemia | Protein phosphatase 2A | MTOR | MAMMALIAN TARGET | PHOSPHATIDYLINOSITOL 3-KINASE/AKT | TRANSCRIPTIONAL ACTIVITY | C-MYC | ACUTE MYELOID-LEUKEMIA | OF-FUNCTION MUTATIONS | CELL BIOLOGY | SCFFBW7 UBIQUITIN LIGASE | gamma-Secretase inhibitor resistance | TUMOR-SUPPRESSOR | PROGNOSTIC-SIGNIFICANCE | Precursor Cell Lymphoblastic Leukemia-Lymphoma - drug therapy | Amyloid Precursor Protein Secretases - metabolism | Animals | Signal Transduction - drug effects | Receptors, Notch - metabolism | Humans | Enzyme Inhibitors - pharmacology | Precursor Cell Lymphoblastic Leukemia-Lymphoma - enzymology | Amyloid Precursor Protein Secretases - antagonists & inhibitors | Precursor Cell Lymphoblastic Leukemia-Lymphoma - pathology | Enzyme Inhibitors - therapeutic use | Drug Resistance, Neoplasm - drug effects | Mutations | Therapy | Cellular | Control | Inhibitors | Activation | Inactivation | Leukemias
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Loading RightsPharmacology and Therapeutics, ISSN 0163-7258, 08/2013, Volume 139, Issue 2, pp. 95 - 110
Notch signaling is an evolutionarily conserved cell signaling pathway involved in cell fate during development, stem cell renewal and differentiation in...
Notch inhibitors | Cancer stem cells | Notch signaling | Cancer | GAMMA-SECRETASE INHIBITOR | HUMAN BREAST-CANCER | PRIMARY MELANOMA PROGRESSION | TUMOR-INITIATING CELLS | RESVERATROL-INDUCED APOPTOSIS | STEM-LIKE CELLS | MAMMARY-GLAND DEVELOPMENT | ACUTE LYMPHOBLASTIC-LEUKEMIA | SQUAMOUS-CELL CARCINOMA | PHARMACOLOGY & PHARMACY | NF-KAPPA-B | Neoplasms - metabolism | Receptors, Notch - antagonists & inhibitors | Animals | Signal Transduction | Receptors, Notch - metabolism | Humans | Antineoplastic Agents - therapeutic use | Neoplasms - drug therapy | Care and treatment | Index Medicus | cancer | cancer stem cells
Notch inhibitors | Cancer stem cells | Notch signaling | Cancer | GAMMA-SECRETASE INHIBITOR | HUMAN BREAST-CANCER | PRIMARY MELANOMA PROGRESSION | TUMOR-INITIATING CELLS | RESVERATROL-INDUCED APOPTOSIS | STEM-LIKE CELLS | MAMMARY-GLAND DEVELOPMENT | ACUTE LYMPHOBLASTIC-LEUKEMIA | SQUAMOUS-CELL CARCINOMA | PHARMACOLOGY & PHARMACY | NF-KAPPA-B | Neoplasms - metabolism | Receptors, Notch - antagonists & inhibitors | Animals | Signal Transduction | Receptors, Notch - metabolism | Humans | Antineoplastic Agents - therapeutic use | Neoplasms - drug therapy | Care and treatment | Index Medicus | cancer | cancer stem cells
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Loading RightsJournal of Medicinal Chemistry, ISSN 0022-2623, 04/2015, Volume 58, Issue 7, pp. 2895 - 2940
The carbamate group is a key structural motif in many approved drugs and prodrugs. There is an increasing use of carbamates in medicinal chemistry and many...
ENZYME PRODRUG THERAPY | NS3 SERINE-PROTEASE | HIV-1 PROTEASE INHIBITORS | CHEMISTRY, MEDICINAL | ACID AMIDE HYDROLASE | SOLID-PHASE SYNTHESIS | 2 BETA-SECRETASE | HEPATITIS-C-VIRUS | HUMAN-LEUKOCYTE ELASTASE | GAMMA-SECRETASE INHIBITORS | ACUTE RESPIRATORY SYNDROME | Antiviral Agents - pharmacology | Chemistry Techniques, Synthetic | Chemistry, Pharmaceutical - methods | Hepatitis C - drug therapy | Drug Stability | Humans | HIV Protease | HIV Protease Inhibitors - chemistry | Carbamates - chemistry | HIV Protease Inhibitors - pharmacology | Carbamates - chemical synthesis | Serine Proteinase Inhibitors - chemistry | Antiviral Agents - chemistry | Cysteine Proteinase Inhibitors - pharmacology | Drug Design | Prodrugs - chemical synthesis | Cysteine Proteinase Inhibitors - chemistry | Amyloid Precursor Protein Secretases - antagonists & inhibitors | Viral Nonstructural Proteins - antagonists & inhibitors | Serine Proteinase Inhibitors - pharmacology | Carbamates - pharmacology
ENZYME PRODRUG THERAPY | NS3 SERINE-PROTEASE | HIV-1 PROTEASE INHIBITORS | CHEMISTRY, MEDICINAL | ACID AMIDE HYDROLASE | SOLID-PHASE SYNTHESIS | 2 BETA-SECRETASE | HEPATITIS-C-VIRUS | HUMAN-LEUKOCYTE ELASTASE | GAMMA-SECRETASE INHIBITORS | ACUTE RESPIRATORY SYNDROME | Antiviral Agents - pharmacology | Chemistry Techniques, Synthetic | Chemistry, Pharmaceutical - methods | Hepatitis C - drug therapy | Drug Stability | Humans | HIV Protease | HIV Protease Inhibitors - chemistry | Carbamates - chemistry | HIV Protease Inhibitors - pharmacology | Carbamates - chemical synthesis | Serine Proteinase Inhibitors - chemistry | Antiviral Agents - chemistry | Cysteine Proteinase Inhibitors - pharmacology | Drug Design | Prodrugs - chemical synthesis | Cysteine Proteinase Inhibitors - chemistry | Amyloid Precursor Protein Secretases - antagonists & inhibitors | Viral Nonstructural Proteins - antagonists & inhibitors | Serine Proteinase Inhibitors - pharmacology | Carbamates - pharmacology
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Loading RightsProceedings of the National Academy of Sciences of the United States of America, ISSN 0027-8424, 01/2019, Volume 116, Issue 1, pp. 141 - 147
Presenilin is the catalytic subunit of gamma-secretase, a four-component intramembrane protease responsible for the generation of (beta-amyloid (A beta)...
Presenilin | Bax inhibitor 1 | Alzheimer’s disease | γ-secretase | β-amyloid | APOPTOSIS | SUPPRESSOR | ACTIVATION | MULTIDISCIPLINARY SCIENCES | gamma-secretase | CALCIUM LEAK | IMPAIRMENT | beta-amyloid | presenilin | HYPOTHESIS | PLANTS | MUTANT PRESENILIN-1 | MUTATIONS | Alzheimer's disease | FAMILIAL ALZHEIMER-DISEASE | Peptides | Bax protein | Substrates | Proteins | Inhibitors | Presenilin 2 | Proteases | Presenilin 1 | Proteolysis | β-Amyloid | Mutation | Catalysis | Alzheimers disease | Secretase | Biological Sciences | PNAS Plus
Presenilin | Bax inhibitor 1 | Alzheimer’s disease | γ-secretase | β-amyloid | APOPTOSIS | SUPPRESSOR | ACTIVATION | MULTIDISCIPLINARY SCIENCES | gamma-secretase | CALCIUM LEAK | IMPAIRMENT | beta-amyloid | presenilin | HYPOTHESIS | PLANTS | MUTANT PRESENILIN-1 | MUTATIONS | Alzheimer's disease | FAMILIAL ALZHEIMER-DISEASE | Peptides | Bax protein | Substrates | Proteins | Inhibitors | Presenilin 2 | Proteases | Presenilin 1 | Proteolysis | β-Amyloid | Mutation | Catalysis | Alzheimers disease | Secretase | Biological Sciences | PNAS Plus
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Loading RightsMedicinal Research Reviews, ISSN 0198-6325, 11/2006, Volume 26, Issue 6, pp. 767 - 792
Sulfamide, a quite simple molecule incorporating the sulfonamide functionality, widely used by medicinal chemists for the design of a host of biologically...
γ‐secretase | sulfamide | thrombin | protein tyrosine phosphatase | chymase | HIV protease | enzyme‐inhibitor adduct | steroid sulfatase inhibitors | elastase | carbonic anhydrase inhibitors | carboxypeptidase A | protease inhibitors | matrix metalloproteinase | tryptase | HUMAN-LEUKOCYTE ELASTASE | RAY CRYSTAL-STRUCTURE | PHARMACOLOGY & PHARMACY | ISOZYME-II | CHEMISTRY, MEDICINAL | STATE ANALOG INHIBITORS | gamma-secretase | GAMMA-SECRETASE INHIBITORS | OF-THE-ART | enzyme-inhibitor adduct | TYROSINE-PHOSPHATASE 1B | 1,2,5-THIADIAZOLIDIN-3-ONE 1,1 DIOXIDE | CARBONIC-ANHYDRASE INHIBITORS | Protease Inhibitors - pharmacology | Sulfonamides - chemistry | Enzyme Inhibitors - chemistry | Humans | Enzyme Inhibitors - pharmacology | Carbonic Anhydrase Inhibitors - pharmacology | Sulfonamides - pharmacology | Enzyme Inhibitors - therapeutic use | Organic chemistry | Chemical Sciences
γ‐secretase | sulfamide | thrombin | protein tyrosine phosphatase | chymase | HIV protease | enzyme‐inhibitor adduct | steroid sulfatase inhibitors | elastase | carbonic anhydrase inhibitors | carboxypeptidase A | protease inhibitors | matrix metalloproteinase | tryptase | HUMAN-LEUKOCYTE ELASTASE | RAY CRYSTAL-STRUCTURE | PHARMACOLOGY & PHARMACY | ISOZYME-II | CHEMISTRY, MEDICINAL | STATE ANALOG INHIBITORS | gamma-secretase | GAMMA-SECRETASE INHIBITORS | OF-THE-ART | enzyme-inhibitor adduct | TYROSINE-PHOSPHATASE 1B | 1,2,5-THIADIAZOLIDIN-3-ONE 1,1 DIOXIDE | CARBONIC-ANHYDRASE INHIBITORS | Protease Inhibitors - pharmacology | Sulfonamides - chemistry | Enzyme Inhibitors - chemistry | Humans | Enzyme Inhibitors - pharmacology | Carbonic Anhydrase Inhibitors - pharmacology | Sulfonamides - pharmacology | Enzyme Inhibitors - therapeutic use | Organic chemistry | Chemical Sciences
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Loading RightsNeurobiology of Aging, ISSN 0197-4580, 2013, Volume 34, Issue 1, pp. 275 - 285
Abstract Deposition of β-amyloid (Aβ) as senile plaques and disrupted glucose metabolism are two main characteristics of Alzheimer's disease (AD). It is...
Neurology | Internal Medicine | Alzheimer's disease (AD) | O-GlcNAcylation | Nicastrin | NButGT | 5XFAD transgenic mouse | β-Amyloid (Aβ) | 3T3-L1 ADIPOCYTES | GAMMA-SECRETASE COMPLEX | ALZHEIMERS-DISEASE | GLYCOSYLATION | NEUROSCIENCES | GERIATRICS & GERONTOLOGY | beta-Amyloid (A beta) | GLCNACASE INHIBITOR | INSULIN-RESISTANCE | IN-VIVO | PRECURSOR PROTEIN | TRANSGENIC MICE | Gene Expression Regulation, Enzymologic - drug effects | Alzheimer Disease - complications | Humans | Fear - drug effects | Dose-Response Relationship, Drug | Transfection | Bridged Bicyclo Compounds, Heterocyclic - therapeutic use | Amyloid beta-Peptides - metabolism | HEK293 Cells | Disease Models, Animal | Memory Disorders - enzymology | Peptide Fragments - metabolism | Enzyme-Linked Immunosorbent Assay | Conditioning (Psychology) - drug effects | beta-N-Acetylhexosaminidases - metabolism | Alzheimer Disease - drug therapy | Presenilin-1 - genetics | Mice, Transgenic | Maze Learning - drug effects | Mutation - genetics | Enzyme Inhibitors - therapeutic use | Plaque, Amyloid - drug therapy | Amyloid Precursor Protein Secretases - metabolism | Amyloid beta-Protein Precursor - genetics | Animals | Memory Disorders - drug therapy | Memory Disorders - etiology | Analysis of Variance | Presenilin-2 - genetics | Mice | Alzheimer Disease - genetics
Neurology | Internal Medicine | Alzheimer's disease (AD) | O-GlcNAcylation | Nicastrin | NButGT | 5XFAD transgenic mouse | β-Amyloid (Aβ) | 3T3-L1 ADIPOCYTES | GAMMA-SECRETASE COMPLEX | ALZHEIMERS-DISEASE | GLYCOSYLATION | NEUROSCIENCES | GERIATRICS & GERONTOLOGY | beta-Amyloid (A beta) | GLCNACASE INHIBITOR | INSULIN-RESISTANCE | IN-VIVO | PRECURSOR PROTEIN | TRANSGENIC MICE | Gene Expression Regulation, Enzymologic - drug effects | Alzheimer Disease - complications | Humans | Fear - drug effects | Dose-Response Relationship, Drug | Transfection | Bridged Bicyclo Compounds, Heterocyclic - therapeutic use | Amyloid beta-Peptides - metabolism | HEK293 Cells | Disease Models, Animal | Memory Disorders - enzymology | Peptide Fragments - metabolism | Enzyme-Linked Immunosorbent Assay | Conditioning (Psychology) - drug effects | beta-N-Acetylhexosaminidases - metabolism | Alzheimer Disease - drug therapy | Presenilin-1 - genetics | Mice, Transgenic | Maze Learning - drug effects | Mutation - genetics | Enzyme Inhibitors - therapeutic use | Plaque, Amyloid - drug therapy | Amyloid Precursor Protein Secretases - metabolism | Amyloid beta-Protein Precursor - genetics | Animals | Memory Disorders - drug therapy | Memory Disorders - etiology | Analysis of Variance | Presenilin-2 - genetics | Mice | Alzheimer Disease - genetics
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Loading RightsPharmacology and Therapeutics, ISSN 0163-7258, 04/2012, Volume 134, Issue 1, pp. 8 - 25
Alzheimer's disease (AD) is the most common cause of memory impairment and dementia in the elderly. AD is pathologically characterized by extracellular...
Pharmacotherapy | Alzheimer's disease | Cholinesterase inhibitors | Immunotherapy | Beta-amyloid | Dementia | TARGETING A-BETA | GAMMA-SECRETASE INHIBITOR | ELECTIVE STATIN USE | AMYLOID-PRECURSOR-PROTEIN | RANDOMIZED CONTROLLED-TRIAL | MILD COGNITIVE IMPAIRMENT | NONSTEROIDAL ANTIINFLAMMATORY DRUGS | MOUSE MODEL | DOUBLE-BLIND | PHARMACOLOGY & PHARMACY | PLACEBO-CONTROLLED TRIAL | Alzheimer Disease - drug therapy | Alzheimer Disease - epidemiology | Alzheimer Disease - physiopathology | Animals | Cholinesterase Inhibitors - therapeutic use | Humans | Methyl aspartate | Enzyme inhibitors | Amyloid beta-protein | Development and progression | Cognition disorders | Apolipoproteins | Drugs | Deposits | Neurodegenerative diseases | Glutamic acid receptors (ionotropic) | memantine | Memory | Cognitive ability | Clinical trials | N-Methyl-D-aspartic acid receptors | beta -Amyloid | Glutamic acid receptors | Acetylcholinesterase | galantamine | Neurotransmitters | Tau protein | Aging | Dementia disorders | Geriatrics
Pharmacotherapy | Alzheimer's disease | Cholinesterase inhibitors | Immunotherapy | Beta-amyloid | Dementia | TARGETING A-BETA | GAMMA-SECRETASE INHIBITOR | ELECTIVE STATIN USE | AMYLOID-PRECURSOR-PROTEIN | RANDOMIZED CONTROLLED-TRIAL | MILD COGNITIVE IMPAIRMENT | NONSTEROIDAL ANTIINFLAMMATORY DRUGS | MOUSE MODEL | DOUBLE-BLIND | PHARMACOLOGY & PHARMACY | PLACEBO-CONTROLLED TRIAL | Alzheimer Disease - drug therapy | Alzheimer Disease - epidemiology | Alzheimer Disease - physiopathology | Animals | Cholinesterase Inhibitors - therapeutic use | Humans | Methyl aspartate | Enzyme inhibitors | Amyloid beta-protein | Development and progression | Cognition disorders | Apolipoproteins | Drugs | Deposits | Neurodegenerative diseases | Glutamic acid receptors (ionotropic) | memantine | Memory | Cognitive ability | Clinical trials | N-Methyl-D-aspartic acid receptors | beta -Amyloid | Glutamic acid receptors | Acetylcholinesterase | galantamine | Neurotransmitters | Tau protein | Aging | Dementia disorders | Geriatrics
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