An overview of glutaminyl cyclase inhibitors for Alzheimer’s disease

A critical appraisal of amyloid-β-targeting therapies for Alzheimer disease

(2019) Francesco Panza et al.   Nature Reviews Neurology

Potent human glutaminyl cyclase inhibitors as potential anti-Alzheimer’s agents: Structure-activity relationship study of Arg-mimetic region

(2018) Van T.H. Ngo et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Structure-activity relationship investigation of Phe-Arg mimetic region of human glutaminyl cyclase inhibitors

(2018) Van T.H. Ngo et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Immunohistochemical Evidence from APP-Transgenic Mice for Glutaminyl Cyclase as Drug Target to Diminish pE-Abeta Formation

(2018) Maike Hartlage-Rübsamen et al.   MOLECULES

Concerted action of dipeptidyl peptidase IV and glutaminyl cyclase results in formation of pyroglutamate-modified amyloid peptides in vitro

(2018) Alvard Antonyan et al.   NEUROCHEMISTRY INTERNATIONAL

Highlights in BACE1 Inhibitors for Alzheimer's Disease Treatment

(2018) Judite R. M. Coimbra et al.   Frontiers in Chemistry

Pyroglutamate and Isoaspartate modified Amyloid-Beta in ageing and Alzheimer’s disease

(2018) Maria Luisa Moro et al.   Acta Neuropathologica Communications

Identifying hQC Inhibitors of Alzheimer’s Disease by Effective Customized Pharmacophore-Based Virtual Screening, Molecular Dynamic Simulation, and Binding Free Energy Analysis

(2018) Weicong Lin et al.   APPLIED BIOCHEMISTRY AND BIOTECHNOLOGY

Glutaminyl Cyclase in Human Cortex: Correlation with (pGlu)-Amyloid-β Load and Cognitive Decline in Alzheimer's Disease

(2018) Markus Morawski et al.   JOURNAL OF ALZHEIMERS DISEASE

Comprehensive review of mechanisms of pathogenesis involved in Alzheimer’s disease and potential therapeutic strategies

(2018) Piyoosh Sharma et al.   PROGRESS IN NEUROBIOLOGY

Safety, tolerability and efficacy of the glutaminyl cyclase inhibitor PQ912 in Alzheimer’s disease: results of a randomized, double-blind, placebo-controlled phase 2a study

(2018) Philip Scheltens et al.   Alzheimers Research & Therapy

Can small molecule inhibitors of glutaminyl cyclase be used as a therapeutic for Alzheimer's disease?

(2017) Haiqiang Wu   Future Medicinal Chemistry

Synthesis and Evaluation of Diphenyl Conjugated Imidazole Derivatives as Potential Glutaminyl Cyclase Inhibitors for Treatment of Alzheimer’s Disease

(2017) Manman Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Potent Human Glutaminyl Cyclase Inhibitors as Anti-Alzheimer’s Agents Based on Rational Design

(2017) Van-Hai Hoang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Glutaminyl Cyclase Inhibitor PQ912 Improves Cognition in Mouse Models of Alzheimer’s Disease—Studies on Relation to Effective Target Occupancy

(2017) Torsten Hoffmann et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Identification of potential glutaminyl cyclase inhibitors from lead-like libraries by in silico and in vitro fragment-based screening

(2017) Mária Szaszkó et al.   MOLECULAR DIVERSITY

Glutaminyl cyclase activity correlates with levels of Aβ peptides and mediators of angiogenesis in cerebrospinal fluid of Alzheimer’s disease patients

(2017) Claire Bridel et al.   Alzheimers Research & Therapy

Inhibitory effect of flavonoids on human glutaminyl cyclase

(2016) Manman Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Natural Products from Microalgae with Potential against Alzheimer’s Disease: Sulfolipids Are Potent Glutaminyl Cyclase Inhibitors

(2016) Stephanie Hielscher-Michael et al.   Marine Drugs

siRNA screen identifies QPCT as a druggable target for Huntington's disease

(2015) Maria Jimenez-Sanchez et al.   Nature Chemical Biology

Cortical pyroglutamate amyloid-β levels and cognitive decline in Alzheimer's disease

(2015) Violetta N. Pivtoraiko et al.   NEUROBIOLOGY OF AGING

Oleuropein aglycone protects against pyroglutamylated-3 amyloid-ß toxicity: biochemical, epigenetic and functional correlates

(2015) Ilaria Luccarini et al.   NEUROBIOLOGY OF AGING

Neuropathology and biochemistry of Aβ and its aggregates in Alzheimer’s disease

(2014) Dietmar Rudolf Thal et al.   ACTA NEUROPATHOLOGICA

Pyroglutamylated amyloid-β is associated with hyperphosphorylated tau and severity of Alzheimer’s disease

(2014) Markus Mandler et al.   ACTA NEUROPATHOLOGICA

Increased glutaminyl cyclase expression in peripheral blood of Alzheimer's disease patients

(2014) Silvia Bolognin et al.   Alzheimers & Dementia

Biochemical stages of amyloid-β peptide aggregation and accumulation in the human brain and their association with symptomatic and pathologically preclinical Alzheimer’s disease

(2014) Ajeet Rijal Upadhaya et al.   BRAIN

Pyroglutamate-3 Amyloid-β Deposition in the Brains of Humans, Non-Human Primates, Canines, and Alzheimer Disease–Like Transgenic Mouse Models

(2013) Jeffrey L. Frost et al.   AMERICAN JOURNAL OF PATHOLOGY

Structure–activity relationship of human glutaminyl cyclase inhibitors having an N-(5-methyl-1H-imidazol-1-yl)propyl thiourea template

(2013) Phuong-Thao Tran et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Structure–Activity Relationships of Benzimidazole-Based Glutaminyl Cyclase Inhibitors Featuring a Heteroaryl Scaffold

(2013) Daniel Ramsbeck et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Polyphenol Oleuropein Aglycone Protects TgCRND8 Mice against Aß Plaque Pathology

(2013) Cristina Grossi et al.   PLoS One

CP-MLR/PLS directed QSAR study on the glutaminyl cyclase inhibitory activity of imidazoles: rationales to advance the understanding of activity profile

(2012) Viney Kumar et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

The isoenzyme of glutaminyl cyclase is an important regulator of monocyte infiltration under inflammatory conditions

(2011) Holger Cynis et al.   EMBO Molecular Medicine

Selective Hippocampal Neurodegeneration in Transgenic Mice Expressing Small Amounts of Truncated A  Is Induced by Pyroglutamate-A  Formation

(2011) A. Alexandru et al.   JOURNAL OF NEUROSCIENCE

Pyroglutamate Formation Influences Solubility and Amyloidogenicity of Amyloid Peptides

(2009) Dagmar Schlenzig et al.   BIOCHEMISTRY

Inhibitors for Human Glutaminyl Cyclase by Structure Based Design and Bioisosteric Replacement

(2009) Mirko Buchholz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Systemic inflammation and disease progression in Alzheimer disease

(2009) C. Holmes et al.   NEUROLOGY

A conserved hydrogen-bond network in the catalytic centre of animal glutaminyl cyclases is critical for catalysis

(2008) Kai-Fa Huang et al.   BIOCHEMICAL JOURNAL

Inhibition of glutaminyl cyclase prevents pGlu-A formation after intracorticalhippocampal microinjectionin vivoin situ

(2008) Stephan Schilling et al.   JOURNAL OF NEUROCHEMISTRY

Glutaminyl cyclase inhibition attenuates pyroglutamate Aβ and Alzheimer's disease–like pathology

(2008) Stephan Schilling et al.   NATURE MEDICINE