Small molecule probes for targeting autophagy

Phenotyping reveals the targets of a pseudo-natural product autophagy inhibitor

(2020) Herbert Waldmann et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

(2020) George M. Burslem et al.   CELL

Phase separation organizes the site of autophagosome formation

(2020) Yuko Fujioka et al.   NATURE

Temporal inhibition of autophagy reveals segmental reversal of ageing with increased cancer risk

(2020) Liam D. Cassidy et al.   Nature Communications

Beclin 1–ATG14L Protein–Protein Interaction Inhibitor Selectively Inhibits Autophagy through Disruption of VPS34 Complex I

(2020) Ivan Pavlinov et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Autophagy promotes immune evasion of pancreatic cancer by degrading MHC-I

(2020) Keisuke Yamamoto et al.   NATURE

Inhibition of Vps34 reprograms cold into hot inflamed tumors and improves anti–PD-1/PD-L1 immunotherapy

(2020) Muhammad Zaeem Noman et al.   Science Advances

Lysosome-targeting chimaeras for degradation of extracellular proteins

(2020) Steven M. Banik et al.   NATURE

Autophagy regulates fatty acid availability for oxidative phosphorylation through mitochondria-endoplasmic reticulum contact sites

(2020) Claudie Bosc et al.   Nature Communications

USP30 sets a trigger threshold for PINK1–PARKIN amplification of mitochondrial ubiquitylation

(2020) Emma V Rusilowicz-Jones et al.   Life Science Alliance

Discovery and optimization of pyrazolopyrimidine sulfamates as ATG7 inhibitors

(2020) Shih-Chung Huang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Autophagy Assays for Biological Discovery and Therapeutic Development

(2020) Noboru Mizushima et al.   TRENDS IN BIOCHEMICAL SCIENCES

Biological Functions of Autophagy Genes: A Disease Perspective

(2019) Beth Levine et al.   CELL

Virus-specific memory T cells populate tumors and can be repurposed for tumor immunotherapy

(2019) Pamela C. Rosato et al.   Nature Communications

AutophagySMDB: a curated database of small molecules that modulate protein targets regulating autophagy

(2019) Ravikanth Nanduri et al.   Autophagy

Autophagy-Independent Functions of the Autophagy Machinery

(2019) Lorenzo Galluzzi et al.   CELL

The cholesterol transfer protein GRAMD1A regulates autophagosome biogenesis

(2019) Luca Laraia et al.   Nature Chemical Biology

Covalent targeting of the vacuolar H+-ATPase activates autophagy via mTORC1 inhibition

(2019) Clive Yik-Sham Chung et al.   Nature Chemical Biology

Felodipine induces autophagy in mouse brains with pharmacokinetics amenable to repurposing

(2019) Farah H. Siddiqi et al.   Nature Communications

ER–lysosome contacts enable cholesterol sensing by mTORC1 and drive aberrant growth signalling in Niemann–Pick type C

(2019) Chun-Yan Lim et al.   NATURE CELL BIOLOGY

Lysosomes as a therapeutic target

(2019) Srinivasa Reddy Bonam et al.   NATURE REVIEWS DRUG DISCOVERY

Image-based morphological profiling identifies a lysosomotropic, iron-sequestering autophagy inhibitor

(2019) Herbert Waldmann et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Mode of action of quinoline antimalarial drugs in red blood cells infected by Plasmodium falciparum revealed in vivo

(2019) Sergey Kapishnikov et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Cellular quality control by the ubiquitin-proteasome system and autophagy

(2019) Christian Pohl et al.   SCIENCE

Autophagy modulator scoring system: a user-friendly tool for quantitative analysis of methodological integrity of chemical autophagy modulator studies

(2019) Yu Dong et al.   Autophagy

AUTACs: Cargo-Specific Degraders Using Selective Autophagy

(2019) Daiki Takahashi et al.   MOLECULAR CELL

High-Throughput Screens To Identify Autophagy Inducers That Function by Disrupting Beclin 1/Bcl-2 Binding

(2018) Wei-Chung Chiang et al.   ACS Chemical Biology

Chloroquine inhibits autophagic flux by decreasing autophagosome-lysosome fusion

(2018) Mario Mauthe et al.   Autophagy

Metformin induces autophagy and G0/G1 phase cell cycle arrest in myeloma by targeting the AMPK/mTORC1 and mTORC2 pathways

(2018) Yan Wang et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

The coming of age of chaperone-mediated autophagy

(2018) Susmita Kaushik et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Mechanism and medical implications of mammalian autophagy

(2018) Ivan Dikic et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Discovery of the novel autophagy inhibitor aumitin that targets mitochondrial complex I

(2018) Lucas Robke et al.   Chemical Science

Disruption of the beclin 1–BCL2 autophagy regulatory complex promotes longevity in mice

(2018) Álvaro F. Fernández et al.   NATURE

A new quinoline-based chemical probe inhibits the autophagy-related cysteine protease ATG4B

(2018) D. Bosc et al.   Scientific Reports

Trehalose induces autophagy via lysosomal-mediated TFEB activation in models of motoneuron degeneration

(2018) Paola Rusmini et al.   Autophagy

HIP1R targets PD-L1 to lysosomal degradation to alter T cell–mediated cytotoxicity

(2018) Huanbin Wang et al.   Nature Chemical Biology

The pharmacological regulation of cellular mitophagy

(2017) Nikolaos D Georgakopoulos et al.   Nature Chemical Biology

Pharmacological modulation of autophagy: therapeutic potential and persisting obstacles

(2017) Lorenzo Galluzzi et al.   NATURE REVIEWS DRUG DISCOVERY

Guidelines for the use and interpretation of assays for monitoring autophagy (3rd edition)

(2016) Daniel J Klionsky et al.   Autophagy

Caloric Restriction Mimetics Enhance Anticancer Immunosurveillance

(2016) Federico Pietrocola et al.   CANCER CELL

An Autophagic Flux Probe that Releases an Internal Control

(2016) Takeshi Kaizuka et al.   MOLECULAR CELL

Trehalose inhibits solute carrier 2A (SLC2A) proteins to induce autophagy and prevent hepatic steatosis

(2016) Brian J. DeBosch et al.   Science Signaling

Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors

(2016) Zongxing Qiu et al.   ACS Medicinal Chemistry Letters

Cholesterol and ORP1L-mediated ER contact sites control autophagosome transport and fusion with the endocytic pathway

(2016) Ruud H. Wijdeven et al.   Nature Communications

Trehalose inhibits solute carrier 2A (SLC2A) proteins to induce autophagy and prevent hepatic steatosis

(2016) Brian J. DeBosch et al.   Science Signaling

Overcoming Chemical, Biological, and Computational Challenges in the Development of Inhibitors Targeting Protein-Protein Interactions

(2015) Luca Laraia et al.   CHEMISTRY & BIOLOGY

Pharmacological Inhibition of ULK1 Kinase Blocks Mammalian Target of Rapamycin (mTOR)-dependent Autophagy

(2015) Katy J. Petherick et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of a Small-Molecule Probe for V-ATPase Function

(2015) Leslie N. Aldrich et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates

(2015) Daniel F. Egan et al.   MOLECULAR CELL

Transcriptional control of autophagy–lysosome function drives pancreatic cancer metabolism

(2015) Rushika M. Perera et al.   NATURE

Lysosomal calcium signalling regulates autophagy through calcineurin and TFEB

(2015) Diego L. Medina et al.   NATURE CELL BIOLOGY

Small-molecule enhancers of autophagy modulate cellular disease phenotypes suggested by human genetics

(2015) Szu-Yu Kuo et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Characterization of VPS34-IN1, a selective inhibitor of Vps34, reveals that the phosphatidylinositol 3-phosphate-binding SGK3 protein kinase is a downstream target of class III phosphoinositide 3-kinase

(2014) Ruzica Bago et al.   BIOCHEMICAL JOURNAL

Molecular Mechanism of Autophagic Membrane-Scaffold Assembly and Disassembly

(2014) Anna Kaufmann et al.   CELL

A highly potent and selective Vps34 inhibitor alters vesicle trafficking and autophagy

(2014) Baptiste Ronan et al.   Nature Chemical Biology

Rapid and reversible knockdown of endogenous proteins by peptide-directed lysosomal degradation

(2014) Xuelai Fan et al.   NATURE NEUROSCIENCE

A TRP Channel in the Lysosome Regulates Large Particle Phagocytosis via Focal Exocytosis

(2013) Mohammad Samie et al.   DEVELOPMENTAL CELL

Endogenous Nitrated Nucleotide Is a Key Mediator of Autophagy and Innate Defense against Bacteria

(2013) Chiaki Ito et al.   MOLECULAR CELL

Identification of a candidate therapeutic autophagy-inducing peptide

(2013) Sanae Shoji-Kawata et al.   NATURE

Cardiolipin externalization to the outer mitochondrial membrane acts as an elimination signal for mitophagy in neuronal cells

(2013) Charleen T. Chu et al.   NATURE CELL BIOLOGY

Chemical modulation of chaperone-mediated autophagy by retinoic acid derivatives

(2013) Jaime Anguiano et al.   Nature Chemical Biology

The role of autophagy in neurodegenerative disease

(2013) Ralph A Nixon   NATURE MEDICINE

The Contribution of Lysosomotropism to Autophagy Perturbation

(2013) Roshan Ashoor et al.   PLoS One

The autophagic inhibitor 3-methyladenine potently stimulates PKA-dependent lipolysis in adipocytes

(2012) Bradlee L Heckmann et al.   BRITISH JOURNAL OF PHARMACOLOGY

The Hairpin-type Tail-Anchored SNARE Syntaxin 17 Targets to Autophagosomes for Fusion with Endosomes/Lysosomes

(2012) Eisuke Itakura et al.   CELL

Evidence for risk of cardiomyopathy with hydroxychloroquine

(2012) MD Sumpter et al.   LUPUS

Molecular determinants of selective clearance of protein inclusions by autophagy

(2012) Esther Wong et al.   Nature Communications

Microautophagy: lesser-known self-eating

(2011) Wen-wen Li et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Natural products reveal cancer cell dependence on oxysterol-binding proteins

(2011) Anthony W G Burgett et al.   Nature Chemical Biology

Probing the Probes: Fitness Factors For Small Molecule Tools

(2010) Paul Workman et al.   CHEMISTRY & BIOLOGY

Discovery of 1-(4-(4-Propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a Highly Potent, Selective Mammalian Target of Rapamycin (mTOR) Inhibitor for the Treatment of Cancer

(2010) Qingsong Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Harnessing chaperone-mediated autophagy for the selective degradation of mutant huntingtin protein

(2010) Peter O Bauer et al.   NATURE BIOTECHNOLOGY

AZD8055 Is a Potent, Selective, and Orally Bioavailable ATP-Competitive Mammalian Target of Rapamycin Kinase Inhibitor with In vitro and In vivo Antitumor Activity

(2009) C. M. Chresta et al.   CANCER RESEARCH

Nutrient-dependent mTORC1 Association with the ULK1–Atg13–FIP200 Complex Required for Autophagy

(2009) Nao Hosokawa et al.   MOLECULAR BIOLOGY OF THE CELL

ULK-Atg13-FIP200 Complexes Mediate mTOR Signaling to the Autophagy Machinery

(2009) Chang Hwa Jung et al.   MOLECULAR BIOLOGY OF THE CELL

AMPK Phosphorylation of Raptor Mediates a Metabolic Checkpoint

(2008) Dana M. Gwinn et al.   MOLECULAR CELL

Identification of New Functional Inhibitors of Acid Sphingomyelinase Using a Structure−Property−Activity Relation Model

(2007) Johannes Kornhuber et al.   JOURNAL OF MEDICINAL CHEMISTRY