标题
Structural and Chemical Biology of Presenilin Complexes
作者
关键词
-
出版物
Cold Spring Harbor Perspectives in Medicine
Volume 7, Issue 12, Pages a024067
出版商
Cold Spring Harbor Laboratory
发表日期
2017-03-21
DOI
10.1101/cshperspect.a024067
参考文献
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注意:仅列出部分参考文献,下载原文获取全部文献信息。- Acute Effect on the Aβ Isoform Pattern in CSF in Response to γ-Secretase Modulator and Inhibitor Treatment in Dogs
- (2017) Erik Portelius et al. JOURNAL OF ALZHEIMERS DISEASE
- Restricted Location of PSEN2/γ-Secretase Determines Substrate Specificity and Generates an Intracellular Aβ Pool
- (2016) Ragna Sannerud et al. CELL
- Minimization of drug–drug interaction risk and candidate selection in a natural product-based class of gamma-secretase modulators
- (2015) Jed L. Hubbs et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- The topology of pen-2, a γ-secretase subunit, revisited: evidence for a reentrant loop and a single pass transmembrane domain
- (2015) Xulun Zhang et al. Molecular Neurodegeneration
- Amyloid-PET predicts inhibition of de novo plaque formation upon chronic γ-secretase modulator treatment
- (2015) M Brendel et al. MOLECULAR PSYCHIATRY
- An atomic structure of human γ-secretase
- (2015) Xiao-chen Bai et al. NATURE
- Presenilin-1 Knockin Mice Reveal Loss-of-Function Mechanism for Familial Alzheimer’s Disease
- (2015) Dan Xia et al. NEURON
- Design of Pyridopyrazine-1,6-dione γ-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability
- (2015) Martin Pettersson et al. ACS Medicinal Chemistry Letters
- Sampling the conformational space of the catalytic subunit of human γ-secretase
- (2015) Xiao-chen Bai et al. eLife
- Pen-2 Is Essential for γ-Secretase Complex Stability and Trafficking but Partially Dispensable for Endoproteolysis
- (2014) Oliver Holmes et al. BIOCHEMISTRY
- Lessons from a Failed γ-Secretase Alzheimer Trial
- (2014) Bart De Strooper CELL
- The dynamic conformational landscape of -secretase
- (2014) N. Elad et al. JOURNAL OF CELL SCIENCE
- Design, Synthesis, and Pharmacological Evaluation of a Novel Series of Pyridopyrazine-1,6-dione γ-Secretase Modulators
- (2014) Martin Pettersson et al. JOURNAL OF MEDICINAL CHEMISTRY
- Three-dimensional structure of human γ-secretase
- (2014) Peilong Lu et al. NATURE
- Therapeutic modulation of Notch signalling — are we there yet?
- (2014) Emma R. Andersson et al. NATURE REVIEWS DRUG DISCOVERY
- Allosteric regulation of -secretase activity by a phenylimidazole-type -secretase modulator
- (2014) K. Takeo et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Crystal structure of the γ-secretase component nicastrin
- (2014) Tian Xie et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Nontranscriptional Role of Hif-1α in Activation of γ-Secretase and Notch Signaling in Breast Cancer
- (2014) Jennifer C. Villa et al. Cell Reports
- Development and Mechanism of γ-Secretase Modulators for Alzheimer’s Disease
- (2013) Christina J. Crump et al. BIOCHEMISTRY
- Toward the structure of presenilin/γ-secretase and presenilin homologs
- (2013) Michael S. Wolfe BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES
- Design and synthesis of bicyclic heterocycles as potent γ-secretase modulators
- (2013) Daniel Oehlrich et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Novel γ-secretase modulators for the treatment of Alzheimer's disease: a review focusing on patents from 2010 to 2012
- (2013) Martin Pettersson et al. EXPERT OPINION ON THERAPEUTIC PATENTS
- γ-Secretase Modulator (GSM) Photoaffinity Probes Reveal Distinct Allosteric Binding Sites on Presenilin
- (2013) Nikolay Pozdnyakov et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Safety, tolerability, pharmacokinetics, and pharmacodynamics of the novel γ-secretase modulator, E2212, in healthy human subjects
- (2013) Yanke Yu et al. JOURNAL OF CLINICAL PHARMACOLOGY
- A Phase 3 Trial of Semagacestat for Treatment of Alzheimer's Disease
- (2013) Rachelle S. Doody et al. NEW ENGLAND JOURNAL OF MEDICINE
- Synthesis of Pyridopyrazine-1,6-diones from 6-Hydroxypicolinic Acids via a One-Pot Coupling/Cyclization Reaction
- (2013) Tuan P. Tran et al. ORGANIC LETTERS
- Structural Interactions between Inhibitor and Substrate Docking Sites Give Insight into Mechanisms of Human PS1 Complexes
- (2013) Yi Li et al. STRUCTURE
- E2012-Induced Cataract and Its Predictive Biomarkers
- (2013) K. Nakano-Ito et al. TOXICOLOGICAL SCIENCES
- Investigating γ-secretase protein interactions in live cells using active site-directed clickable dual-photoaffinity probes
- (2013) T. Eric Ballard et al. MedChemComm
- Development of CBAP-BPyne, a probe for γ-secretase and presenilinase
- (2013) Natalya Gertsik et al. MedChemComm
- Efficacy of SPI-1865, a novel gamma-secretase modulator, in multiple rodent models
- (2013) Robyn M Loureiro et al. Alzheimers Research & Therapy
- Discovery of a Novel Pharmacological and Structural Class of Gamma Secretase Modulators Derived from the Extract of Actaea racemosa
- (2012) Mark A. Findeis et al. ACS Chemical Neuroscience
- Pharmacokinetics and Pharmacodynamics of CHF5074 After Short-term Administration in Healthy Subjects
- (2012) Bruno P. Imbimbo et al. ALZHEIMER DISEASE & ASSOCIATED DISORDERS
- Potential Use of γ-Secretase Modulators in the Treatment of Alzheimer Disease
- (2012) Steven L. Wagner et al. ARCHIVES OF NEUROLOGY
- Safety and Tolerability of the γ-Secretase Inhibitor Avagacestat in a Phase 2 Study of Mild to Moderate Alzheimer Disease
- (2012) Vladimir Coric et al. ARCHIVES OF NEUROLOGY
- BMS-708,163 Targets Presenilin and Lacks Notch-Sparing Activity
- (2012) Christina J. Crump et al. BIOCHEMISTRY
- Development of clickable active site-directed photoaffinity probes for γ-secretase
- (2012) Christina J. Crump et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- The mechanism of γ-Secretase dysfunction in familial Alzheimer disease
- (2012) Lucía Chávez-Gutiérrez et al. EMBO JOURNAL
- Familial Alzheimer Disease Presenilin-1 Mutations Alter the Active Site Conformation of γ-secretase
- (2012) De-Ming Chau et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- First and Second Generation γ-Secretase Modulators (GSMs) Modulate Amyloid-β (Aβ) Peptide Production through Different Mechanisms
- (2012) Tomas Borgegard et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Moving Forward One Notch at a Time
- (2012) Mrinal M. Gounder et al. JOURNAL OF CLINICAL ONCOLOGY
- Phase I Pharmacologic and Pharmacodynamic Study of the Gamma Secretase (Notch) Inhibitor MK-0752 in Adult Patients With Advanced Solid Tumors
- (2012) Ian Krop et al. JOURNAL OF CLINICAL ONCOLOGY
- Phase I Study of RO4929097, a Gamma Secretase Inhibitor of Notch Signaling, in Patients With Refractory Metastatic or Locally Advanced Solid Tumors
- (2012) Anthony W. Tolcher et al. JOURNAL OF CLINICAL ONCOLOGY
- Design and Synthesis of a Novel Series of Bicyclic Heterocycles As Potent γ-Secretase Modulators
- (2012) Francois Bischoff et al. JOURNAL OF MEDICINAL CHEMISTRY
- Optimization of a Natural Product-Based Class of γ-Secretase Modulators
- (2012) Jed L. Hubbs et al. JOURNAL OF MEDICINAL CHEMISTRY
- Pen-2 is dispensable for endoproteolysis of presenilin 1, and nicastrin-Aph subcomplex is important for both γ-secretase assembly and substrate recruitment
- (2012) Guozhang Mao et al. JOURNAL OF NEUROCHEMISTRY
- Differential Effects between -Secretase Inhibitors and Modulators on Cognitive Function in Amyloid Precursor Protein-Transgenic and Nontransgenic Mice
- (2012) Y. Mitani et al. JOURNAL OF NEUROSCIENCE
- Modulation of γ-secretase by EVP-0015962 reduces amyloid deposition and behavioral deficits in Tg2576 mice
- (2012) Kathryn Rogers et al. Molecular Neurodegeneration
- Structure of a presenilin family intramembrane aspartate protease
- (2012) Xiaochun Li et al. NATURE
- Vigilin interacts with signal peptide peptidase
- (2012) Stephen Hsueh-Jeng Lu et al. Proteome Science
- Synthesis and SAR Studies of Fused Oxadiazines as γ-Secretase Modulators for Treatment of Alzheimer's Disease
- (2012) Xianhai Huang et al. ACS Medicinal Chemistry Letters
- Piperidine Acetic Acid Based γ-Secretase Modulators Directly Bind to Presenilin-1
- (2011) Christina J. Crump et al. ACS Chemical Neuroscience
- Chronic treatment with a novel γ-secretase modulator, JNJ-40418677, inhibits amyloid plaque formation in a mouse model of Alzheimer's disease
- (2011) B Van Broeck et al. BRITISH JOURNAL OF PHARMACOLOGY
- Advances in the identification of γ-secretase inhibitors for the treatment of Alzheimer's disease
- (2011) Grazia D'Onofrio et al. Expert Opinion on Drug Discovery
- Novel γ-secretase modulators: a review of patents from 2008 to 2010
- (2011) Martin Pettersson et al. EXPERT OPINION ON THERAPEUTIC PATENTS
- Structure of γ-Secretase and Its Trimeric Pre-activation Intermediate by Single-particle Electron Microscopy
- (2011) Fabiana Renzi et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Novel γ-Secretase Enzyme Modulators Directly Target Presenilin Protein
- (2011) Amelie Ebke et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Cyclic Hydroxyamidines as Amide Isosteres: Discovery of Oxadiazolines and Oxadiazines as Potent and Highly Efficacious γ-Secretase Modulators in Vivo
- (2011) Zhong-Yue Sun et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of BIIB042, a Potent, Selective, and Orally Bioavailable γ-Secretase Modulator
- (2011) Hairuo Peng et al. ACS Medicinal Chemistry Letters
- E2012, a novel gamma-secretase modulator, decreases plasma amyloid-beta (Aβ) levels in humans
- (2010) Christa Nagy et al. Alzheimers & Dementia
- E2012: A novel gamma-secretase modulator-pharmacology part
- (2010) Toshihide Hashimoto et al. Alzheimers & Dementia
- Novel Research Horizons for Presenilins and γ-Secretases in Cell Biology and Disease
- (2010) Bart De Strooper et al. Annual Review of Cell and Developmental Biology
- β-Amyloid Precursor Protein Mutants Respond to γ-Secretase Modulators
- (2010) Richard M. Page et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Functional Analysis of the Transmembrane Domains of Presenilin 1
- (2010) Naoto Watanabe et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- -Secretase Composed of PS1/Pen2/Aph1a Can Cleave Notch and Amyloid Precursor Protein in the Absence of Nicastrin
- (2010) G. Zhao et al. JOURNAL OF NEUROSCIENCE
- An APP inhibitory domain containing the Flemish mutation residue modulates γ-secretase activity for Aβ production
- (2010) Yuan Tian et al. NATURE STRUCTURAL & MOLECULAR BIOLOGY
- Modulation of γ-Secretase Reduces β-Amyloid Deposition in a Transgenic Mouse Model of Alzheimer's Disease
- (2010) Maria Z. Kounnas et al. NEURON
- Structural investigation of the C-terminal catalytic fragment of presenilin 1
- (2010) S. Sobhanifar et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Activation and intrinsic -secretase activity of presenilin 1
- (2010) K. Ahn et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor
- (2010) Kevin W. Gillman et al. ACS Medicinal Chemistry Letters
- APH1 Polar Transmembrane Residues Regulate the Assembly and Activity of Presenilin Complexes
- (2009) Raphaëlle Pardossi-Piquard et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Intramembrane Proteolysis by Signal Peptide Peptidases: A Comparative Discussion of GXGD-type Aspartyl Proteases
- (2009) Regina Fluhrer et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Affinity pulldown of γ-secretase and associated proteins from human and rat brain
- (2009) Yasuhiro Teranishi et al. JOURNAL OF CELLULAR AND MOLECULAR MEDICINE
- Modulation of -secretase specificity using small molecule allosteric inhibitors
- (2009) C. C. Shelton et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- -Secretase Heterogeneity in the Aph1 Subunit: Relevance for Alzheimer's Disease
- (2009) L. Serneels et al. SCIENCE
- Stereo-controlled synthesis of novel photoreactive γ-secretase inhibitors
- (2008) Guangli Yang et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Pen2 and Presenilin-1 Modulate the Dynamic Equilibrium of Presenilin-1 and Presenilin-2 γ-Secretase Complexes
- (2008) Lisa Placanica et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Intramembrane Proteolysis by γ-Secretase
- (2008) Harald Steiner et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Cryoelectron Microscopy Structure of Purified γ-Secretase at 12 Å Resolution
- (2008) Pamela Osenkowski et al. JOURNAL OF MOLECULAR BIOLOGY
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