4.7 Article

Indoles and 1-(3-(benzyloxy)benzyl)piperazines: Reversible and selective monoamine oxidase B inhibitors identified by screening an in-house compound library

相关参考文献

注意:仅列出部分参考文献,下载原文获取全部文献信息。
Article Biochemistry & Molecular Biology

The Determining Role of Mitochondrial Reactive Oxygen Species Generation and Monoamine Oxidase Activity in Doxorubicin-Induced Cardiotoxicity

Salvatore Antonucci et al.

Summary: The study demonstrates the crucial role of monoamine oxidases (MAOs) in oxidative stress and mitochondrial dysfunction in doxorubicin cardiomyopathy. Pharmacological inhibition of MAOs can alleviate the dysfunctions leading to cell death.

ANTIOXIDANTS & REDOX SIGNALING (2021)

Article Biochemistry & Molecular Biology

Biphenylpiperazine Based MAO Inhibitors: Synthesis, Biological Evaluation, Reversibility and Molecular Modeling Studies

Lamiaa O. El-Halaby et al.

Summary: This study involved the design and synthesis of 21 new 1,4-biphenylpiperazine derivatives, with compound 20 showing the best activity and selectivity towards hMAO-B. The compounds demonstrated potential as promising leads for the development of more potent and safer MAO inhibitors for the treatment of various neurological disorders.

BIOORGANIC CHEMISTRY (2021)

Review Pharmacology & Pharmacy

Evaluating and evolving a screening library in academia: the St Jude approach

Gisele Nishiguchi et al.

Summary: The quality of lead compounds is crucial for the success of chemical probe and drug discovery programs, especially with high-throughput screening being a dominant lead generation paradigm. This article discusses a strategy implemented a decade ago to build one of the largest compound collections in academia, and a recent multidisciplinary effort aimed at enhancing and expanding the collection.

DRUG DISCOVERY TODAY (2021)

Article Biochemistry & Molecular Biology

Cardiomyocytes-specific deletion of monoamine oxidase B reduces irreversible myocardial ischemia/reperfusion injury

Jacqueline Heger et al.

Summary: The creation of MAO-B knockout mice demonstrates that the lack of cardiomyocyte MAO-B can protect the heart from I/R injury and reduce infarct size.

FREE RADICAL BIOLOGY AND MEDICINE (2021)

Article Chemistry, Multidisciplinary

Targeting the Main Protease of SARS-CoV-2: From the Establishment of High Throughput Screening to the Design of Tailored Inhibitors

Julian Breidenbach et al.

Summary: Two classes of protease inhibitors, azanitriles and pyridyl esters, were identified and optimized for potential use against COVID-19. Tailored peptides with unique azanitrile warheads showed promising results in inhibiting M-pro and cathepsin L. Through a focused approach, two irreversible inhibitors, azanitrile 8 and pyridyl ester 17, have been discovered as potential drug candidates for further development.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2021)

Review Pharmacology & Pharmacy

Gains from no real PAINS: Where 'Fair Trial Strategy' stands in the development of multi-target ligands

Jianbo Sun et al.

Summary: The development of compounds with selectivity for multiple targets is hindered by the presence of PAINS suspects, which can result in false positive data. Extensive offline experiments are necessary to distinguish between harmful and beneficial compounds after online filtering.

ACTA PHARMACEUTICA SINICA B (2021)

Article Chemistry, Medicinal

Small-Molecule Inhibitors of Reactive Oxygen Species Production

Elisa Sassetti et al.

Summary: Reactive oxygen species (ROS) play vital roles in physiological cellular processes, and maintaining appropriate levels of cellular ROS is important for redox homeostasis. Directly targeting the sources of ROS production has become a key focus in research due to the potential link between high ROS concentrations and severe diseases.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Immunology

Targeting monoamine oxidase A for T cell-based cancer immunotherapy

Xi Wang et al.

Summary: The enzyme MAO-A has been found to play a critical role in anti-tumor immunity, with its inhibition enhancing anti-tumor T cell responses and suppressing tumor growth. Treatment with MAO inhibitors (MAOIs) significantly inhibits tumor growth, and combining MAOI with anti-PD-1 therapy produces synergistic effects in tumor suppression.

SCIENCE IMMUNOLOGY (2021)

Review Biochemistry & Molecular Biology

Nuisance compounds in cellular assays

Jayme L. Dahlin et al.

Summary: Nuisance compounds, which can waste resources and erode scientific trust, are a major obstacle in realizing the full potential of chemical biology. Understanding and addressing these compounds in complex cell-based assays is essential for efficient drug discovery and research.

CELL CHEMICAL BIOLOGY (2021)

Review Chemistry, Medicinal

Propargylamine-derived multi-target directed ligands for Alzheimer's disease therapy

Maria do Carmo Carreiras et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2020)

Editorial Material Cell Biology

Cardiac monoamine oxidases: at the heart of mitochondrial dysfunction

Jeanne Mialet-Perez et al.

CELL DEATH & DISEASE (2020)

Article Biochemistry & Molecular Biology

Rational Redesign of Monoamine Oxidase A into a Dehydrogenase to Probe ROS in Cardiac Aging

Luca Giacinto Iacovino et al.

ACS CHEMICAL BIOLOGY (2020)

Article Chemistry, Medicinal

Evolution of Novartis' Small Molecule Screening Deck Design

Ansgar Schuffenhauer et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

Review Chemistry, Medicinal

A comprehensive review of monoamine oxidase inhibitors as Anti-Alzheimer's disease agents: A review

Shoaib Manzoor et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

Review Cell Biology

Highlights of ASS234: a novel and promising therapeutic agent for Alzheimer's disease therapy

Alejandro Romero et al.

NEURAL REGENERATION RESEARCH (2020)

Article Biochemistry & Molecular Biology

Accurate template-based modeling in CASP12 using the IntFOLD4-TS, ModFOLD6, and ReFOLD methods

Liam J. McGuffin et al.

PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS (2018)

Review Biochemistry & Molecular Biology

A review on the hybrids of hydroxycinnamic acid as multi-target-directed ligands against Alzheimer's disease

Xiao Zhang et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2018)

Review Pharmacology & Pharmacy

Safinamide: a new hope for Parkinson's disease?

Fabio G. Teixeira et al.

DRUG DISCOVERY TODAY (2018)

Review Chemistry, Medicinal

Privileged scaffolds as MAO inhibitors: Retrospect and prospects

Avinash C. Tripathi et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)

Article Chemistry, Medicinal

Where Do Recent Small Molecule Clinical Development Candidates Come From?

Dean G. Brown et al.

JOURNAL OF MEDICINAL CHEMISTRY (2018)

Review Clinical Neurology

Monoamine oxidase-B inhibitors in the treatment of Parkinson's disease: clinical-pharmacological aspects

Peter Riederer et al.

JOURNAL OF NEURAL TRANSMISSION (2018)

Review Medicine, Research & Experimental

Current Strategies for Brain Drug Delivery

Xiaowei Dong

THERANOSTICS (2018)

Review Clinical Neurology

Monoamine oxidase isoenzymes: genes, functions and targets for behavior and cancer therapy

Jean C. Shih

JOURNAL OF NEURAL TRANSMISSION (2018)

Review Clinical Neurology

Monoamine oxidase inhibitors, and iron chelators in depressive illness and neurodegenerative diseases

Moussa B. H. Youdim

JOURNAL OF NEURAL TRANSMISSION (2018)

Review Neurosciences

The SH-SY5Y cell line in Parkinson's disease research: a systematic review

Helena Xicoy et al.

MOLECULAR NEURODEGENERATION (2017)

Article Biochemistry & Molecular Biology

Focused screening to identify new adenosine kinase inhibitors

Meryem Koese et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2016)

Article Chemistry, Medicinal

The essential roles of chemistry in high-throughput screening triage

Jayme L. Dahlin et al.

FUTURE MEDICINAL CHEMISTRY (2014)

Article Biochemistry & Molecular Biology

GABA from reactive astrocytes impairs memory in mouse models of Alzheimer's disease

Seonmi Jo et al.

NATURE MEDICINE (2014)

Article Chemistry, Medicinal

Metal Impurities Cause False Positives in High-Throughput Screening Campaigns

Johannes C. Hermann et al.

ACS MEDICINAL CHEMISTRY LETTERS (2013)

Review Biotechnology & Applied Microbiology

Cell death assays for drug discovery

Oliver Kepp et al.

NATURE REVIEWS DRUG DISCOVERY (2011)

Article Chemistry, Multidisciplinary

Open Babel: An open chemical toolbox

Noel M. O'Boyle et al.

JOURNAL OF CHEMINFORMATICS (2011)

Article Chemistry, Medicinal

Inhibition of monoamine oxidase by indole and benzofuran derivatives

Louis H. A. Prins et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2010)

Article Biochemistry & Molecular Biology

Improving physical realism, stereochemistry, and side-chain accuracy in homology modeling: Four approaches that performed well in CASP8

Elmar Krieger et al.

PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS (2009)

Article Biochemistry & Molecular Biology

Synthesis, structure-activity relationships and molecular modeling studies of new indole inhibitors of monoamine oxidases A and B

Giuseppe La Regina et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2008)

Article Chemistry, Medicinal

Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues

F Hubálek et al.

JOURNAL OF MEDICINAL CHEMISTRY (2004)

Review Biochemistry & Molecular Biology

High-throughput characterization and quality control of small-molecule combinatorial libraries

JR Kenseth et al.

CURRENT OPINION IN CHEMICAL BIOLOGY (2004)