Targeting allosteric regulation of cancer metabolism

MAT2A inhibition blocks the growth of MTAP-deleted cancer cells by reducing PRMT5-dependent mRNA splicing and inducing DNA damage

(2021) Peter Kalev et al.   CANCER CELL

Serine synthesis pathway inhibition cooperates with dietary serine and glycine limitation for cancer therapy

(2021) Mylène Tajan et al.   Nature Communications

Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion

(2021) Zenon Konteatis et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fragment-Based Design of a Potent MAT2a Inhibitor and in Vivo Evaluation in an MTAP Null Xenograft Model

(2021) Claudia De Fusco et al.   JOURNAL OF MEDICINAL CHEMISTRY

Biophysical and biochemical properties of PHGDH revealed by studies on PHGDH inhibitors

(2021) Yuping Tan et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Click Chemistry in Proteomic Investigations

(2020) Christopher G. Parker et al.   CELL

Integrated Computational Approaches and Tools for Allosteric Drug Discovery

(2020) Olivier Sheik Amamuddy et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

2-Sulfonylpyridines as Tunable, Cysteine-Reactive Electrophiles

(2020) Claudio Zambaldo et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Dietary modifications for enhanced cancer therapy

(2020) Naama Kanarek et al.   NATURE

A small molecule G6PD inhibitor reveals immune dependence on pentose phosphate pathway

(2020) Jonathan M. Ghergurovich et al.   Nature Chemical Biology

Combining Allosteric and Orthosteric Drugs to Overcome Drug Resistance

(2020) Duan Ni et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Protein topology and allostery

(2020) Juan Xie et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Limited Environmental Serine and Glycine Confer Brain Metastasis Sensitivity to PHGDH Inhibition

(2020) Bryan Ngo et al.   Cancer Discovery

A machine learning-based chemoproteomic approach to identify drug targets and binding sites in complex proteomes

(2020) Ilaria Piazza et al.   Nature Communications

Allosteric Feedback Inhibition Enables Robust Amino Acid Biosynthesis in E. coli by Enforcing Enzyme Overabundance

(2019) Timur Sander et al.   Cell Systems

Allostery in Its Many Disguises: From Theory to Applications

(2019) Shoshana J. Wodak et al.   STRUCTURE

Navigating metabolic pathways to enhance antitumour immunity and immunotherapy

(2019) Xiaoyun Li et al.   Nature Reviews Clinical Oncology

Allosteric Modulator Discovery: From Serendipity to Structure-Based Design

(2019) Shaoyong Lu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Serine Metabolism Supports Macrophage IL-1β Production

(2019) Arianne E. Rodriguez et al.   Cell Metabolism

An allosteric mechanism for potent inhibition of human ATP-citrate lyase

(2019) Jia Wei et al.   NATURE

Inhibition of 3-phosphoglycerate dehydrogenase (PHGDH) by indole amides abrogates de novo serine synthesis in cancer cells

(2019) Edouard Mullarky et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Intracellular Trapping of the Selective Phosphoglycerate Dehydrogenase (PHGDH) Inhibitor BI-4924 Disrupts Serine Biosynthesis

(2019) Harald Weinstabl et al.   JOURNAL OF MEDICINAL CHEMISTRY

Functional cross-talk between allosteric effects of activating and inhibiting ligands underlies PKM2 regulation

(2019) Jamie A Macpherson et al.   eLife

SuFEx-enabled, agnostic discovery of covalent inhibitors of human neutrophil elastase

(2019) Qinheng Zheng et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Global targeting of functional tyrosines using sulfur-triazole exchange chemistry

(2019) Heung Sik Hahm et al.   Nature Chemical Biology

Glutamine blockade induces divergent metabolic programs to overcome tumor immune evasion

(2019) Robert D. Leone et al.   SCIENCE

A Map of Protein-Metabolite Interactions Reveals Principles of Chemical Communication

(2018) Ilaria Piazza et al.   CELL

Characterization of the interactions of potent allosteric inhibitors with glutaminase C, a key enzyme in cancer cell glutamine metabolism

(2018) Qingqiu Huang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Menin regulates the serine biosynthetic pathway in Ewing sarcoma

(2018) Laurie K Svoboda et al.   JOURNAL OF PATHOLOGY

Reversal of indoleamine 2,3-dioxygenase–mediated cancer immune suppression by systemic kynurenine depletion with a therapeutic enzyme

(2018) Todd A Triplett et al.   NATURE BIOTECHNOLOGY

CavityPlus: a web server for protein cavity detection with pharmacophore modelling, allosteric site identification and covalent ligand binding ability prediction

(2018) Youjun Xu et al.   NUCLEIC ACIDS RESEARCH

AlloFinder: a strategy for allosteric modulator discovery and allosterome analyses

(2018) Min Huang et al.   NUCLEIC ACIDS RESEARCH

ATP citrate lyase (ACLY) inhibitors: An anti-cancer strategy at the crossroads of glucose and lipid metabolism

(2018) Carlotta Granchi   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A protein functionalization platform based on selective reactions at methionine residues

(2018) Michael T. Taylor et al.   NATURE

α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH)

(2017) Séverine Ravez et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting S-adenosylmethionine biosynthesis with a novel allosteric inhibitor of Mat2A

(2017) Casey L Quinlan et al.   Nature Chemical Biology

Global profiling of lysine reactivity and ligandability in the human proteome

(2017) Stephan M. Hacker et al.   Nature Chemistry

Redox-based reagents for chemoselective methionine bioconjugation

(2017) Shixian Lin et al.   SCIENCE

Compensatory metabolic networks in pancreatic cancers upon perturbation of glutamine metabolism

(2017) Douglas E. Biancur et al.   Nature Communications

The Emerging Hallmarks of Cancer Metabolism

(2016) Natalya N. Pavlova et al.   Cell Metabolism

Emerging Computational Methods for the Rational Discovery of Allosteric Drugs

(2016) Jeffrey R. Wagner et al.   CHEMICAL REVIEWS

Proteome-wide covalent ligand discovery in native biological systems

(2016) Keriann M. Backus et al.   NATURE

A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate

(2016) Michael E Pacold et al.   Nature Chemical Biology

Identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancers

(2016) Edouard Mullarky et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Disordered methionine metabolism in MTAP/CDKN2A-deleted cancers leads to dependence on PRMT5

(2016) Konstantinos J. Mavrakis et al.   SCIENCE

MTAPdeletion confers enhanced dependency on the PRMT5 arginine methyltransferase in cancer cells

(2016) Gregory V. Kryukov et al.   SCIENCE

Systems-level analysis of mechanisms regulating yeast metabolic flux

(2016) S. R. Hackett et al.   SCIENCE

MTAP Deletions in Cancer Create Vulnerability to Targeting of the MAT2A/PRMT5/RIOK1 Axis

(2016) Katya Marjon et al.   Cell Reports

A Global Map of Lipid-Binding Proteins and Their Ligandability in Cells

(2015) Micah J. Niphakis et al.   CELL

Action at a Distance: Allostery and the Development of Drugs to Target Cancer Cell Metabolism

(2014) Byron DeLaBarre et al.   CHEMISTRY & BIOLOGY

Selective Inhibition of Mutant Isocitrate Dehydrogenase 1 (IDH1) via Disruption of a Metal Binding Network by an Allosteric Small Molecule

(2014) Gejing Deng et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Mapping the Protein Interaction Landscape for Fully Functionalized Small-Molecule Probes in Human Cells

(2014) Tohru Kambe et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Quantitative flux analysis reveals folate-dependent NADPH production

(2014) Jing Fan et al.   NATURE

Unraveling structural mechanisms of allosteric drug action

(2014) Ruth Nussinov et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Structure and function study of the complex that synthesizesS-adenosylmethionine

(2014) Ben Murray et al.   IUCrJ

Allostery in Disease and in Drug Discovery

(2013) Ruth Nussinov et al.   CELL

Influence of Metabolism on Epigenetics and Disease

(2013) William G. Kaelin et al.   CELL

Understanding allosteric and cooperative interactions in enzymes

(2013) Athel Cornish-Bowden   FEBS Journal

Systematic identification of allosteric protein-metabolite interactions that control enzyme activity in vivo

(2013) Hannes Link et al.   NATURE BIOTECHNOLOGY

Proteome-wide mapping of cholesterol-interacting proteins in mammalian cells

(2013) Jonathan J Hulce et al.   NATURE METHODS

Modulation of oxidative stress as an anticancer strategy

(2013) Chiara Gorrini et al.   NATURE REVIEWS DRUG DISCOVERY

Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation

(2013) F. Wang et al.   SCIENCE

Phosphoglycerate Mutase 1 Coordinates Glycolysis and Biosynthesis to Promote Tumor Growth

(2012) Taro Hitosugi et al.   CANCER CELL

Small Molecule Activation of PKM2 in Cancer Cells Induces Serine Auxotrophy

(2012) Charles Kung et al.   CHEMISTRY & BIOLOGY

Serine is a natural ligand and allosteric activator of pyruvate kinase M2

(2012) Barbara Chaneton et al.   NATURE

Rational Engineering of Enzyme Allosteric Regulation through Sequence Evolution Analysis

(2012) Jae-Seong Yang et al.   PLoS Computational Biology

Hot Spots for Allosteric Regulation on Protein Surfaces

(2011) Kimberly A. Reynolds et al.   CELL

Turning a protein kinase on or off from a single allosteric site via disulfide trapping

(2011) J. D. Sadowsky et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Quantitative reactivity profiling predicts functional cysteines in proteomes

(2010) Eranthie Weerapana et al.   NATURE

Cancer-associated IDH1 mutations produce 2-hydroxyglutarate

(2009) Lenny Dang et al.   NATURE

Understanding the Warburg Effect: The Metabolic Requirements of Cell Proliferation

(2009) M. G. Vander Heiden et al.   SCIENCE

ATP-Citrate Lyase Links Cellular Metabolism to Histone Acetylation

(2009) K. E. Wellen et al.   SCIENCE

A History of Cancer Chemotherapy

(2008) Vincent T. DeVita et al.   CANCER RESEARCH

Oncogene Addiction

(2008) I. B. Weinstein et al.   CANCER RESEARCH

The Biology of Cancer: Metabolic Reprogramming Fuels Cell Growth and Proliferation

(2008) Ralph J. DeBerardinis et al.   Cell Metabolism

Pyruvate kinase M2 is a phosphotyrosine-binding protein

(2008) Heather R. Christofk et al.   NATURE