Glutaminase inhibitors: a patent review

Glutaminase isoenzymes in the metabolic therapy of cancer

(2018) José M. Matés et al.   BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER

A natural inhibitor of kidney-type glutaminase: a withanolide from Physalis pubescens with potent anti-tumor activity

(2017) Canrong Wu et al.   Oncotarget

Breaking Cryo-EM Resolution Barriers to Facilitate Drug Discovery

(2016) Alan Merk et al.   CELL

Combination therapy with BPTES nanoparticles and metformin targets the metabolic heterogeneity of pancreatic cancer

(2016) Amira Elgogary et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The oncogenic transcription factor c-Jun regulates glutaminase expression and sensitizes cells to glutaminase-targeted therapy

(2016) Michael J. Lukey et al.   Nature Communications

Structural basis for exploring the allosteric inhibition of human kidney type glutaminase

(2016) Sarath Ramachandran et al.   Oncotarget

Inhibiting glutaminase in acute myeloid leukemia: metabolic dependency of selected AML subtypes

(2016) Polina Matre et al.   Oncotarget

Targeting glutaminolysis has antileukemic activity in acute myeloid leukemia and synergizes with BCL-2 inhibition

(2015) N. Jacque et al.   BLOOD

Alterations in cellular metabolome after pharmacological inhibition of Notch in glioblastoma cells

(2015) Ulf D. Kahlert et al.   INTERNATIONAL JOURNAL OF CANCER

Compensatory glutamine metabolism promotes glioblastoma resistance to mTOR inhibitor treatment

(2015) Kazuhiro Tanaka et al.   JOURNAL OF CLINICAL INVESTIGATION

Cross-talk between ER and HER2 regulates c-MYC-mediated glutamine metabolism in aromatase inhibitor resistant breast cancer cells

(2015) Zhike Chen et al.   JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY

Vemurafenib resistance reprograms melanoma cells towards glutamine dependence

(2015) Jenny E Hernandez-Davies et al.   Journal of Translational Medicine

Glutaminolysis and Transferrin Regulate Ferroptosis

(2015) Minghui Gao et al.   MOLECULAR CELL

Glutamine synthetase activity fuels nucleotide biosynthesis and supports growth of glutamine-restricted glioblastoma

(2015) Saverio Tardito et al.   NATURE CELL BIOLOGY

Metabolic reprogramming induces resistance to anti-NOTCH1 therapies in T cell acute lymphoblastic leukemia

(2015) Daniel Herranz et al.   NATURE MEDICINE

Regulation of mammalian nucleotide metabolism and biosynthesis

(2015) Andrew N. Lane et al.   NUCLEIC ACIDS RESEARCH

Glutamine-based PET imaging facilitates enhanced metabolic evaluation of gliomas in vivo

(2015) Sriram Venneti et al.   Science Translational Medicine

MYC-induced reprogramming of glutamine catabolism supports optimal virus replication

(2015) Minh Thai et al.   Nature Communications

Inhibition of mitochondrial glutaminase activity reverses acquired erlotinib resistance in non-small cell lung cancer

(2015) Caifeng Xie et al.   Oncotarget

Myc promotes glutaminolysis in human neuroblastoma through direct activation of glutaminase 2

(2015) Daibiao Xiao et al.   Oncotarget

Latent KSHV Infected Endothelial Cells Are Glutamine Addicted and Require Glutaminolysis for Survival

(2015) Erica L. Sanchez et al.   PLoS Pathogens

Abstract 1416: CB-839, a novel potent and selective glutaminase inhibitor, has broad antiproliferative activity in cell lines derived from both solid tumors and hematological malignancies

(2015) Francesco Parlati et al.   CANCER RESEARCH

Capturing the metabolomic diversity of KRAS mutants in non-small-cell lung cancer cells

(2015) Laura Brunelli et al.   Oncotarget

Hypoxic Regulation of Glutamine Metabolism through HIF1 and SIAH2 Supports Lipid Synthesis that Is Necessary for Tumor Growth

(2014) Ramon C. Sun et al.   Cell Metabolism

Determination of Glutamate Dehydrogenase Activity and Its Kinetics in Mouse Tissues using Metabolic Mapping (Quantitative Enzyme Histochemistry)

(2014) Dennis Botman et al.   JOURNAL OF HISTOCHEMISTRY & CYTOCHEMISTRY

Antitumor Activity of the Glutaminase Inhibitor CB-839 in Triple-Negative Breast Cancer

(2014) M. I. Gross et al.   MOLECULAR CANCER THERAPEUTICS

Glutamine Oxidation Maintains the TCA Cycle and Cell Survival during Impaired Mitochondrial Pyruvate Transport

(2014) Chendong Yang et al.   MOLECULAR CELL

Simultaneously Targeting Tissue Transglutaminase and Kidney Type Glutaminase Sensitizes Cancer Cells to Acid Toxicity and Offers New Opportunities for Therapeutic Intervention

(2014) William P. Katt et al.   MOLECULAR PHARMACEUTICS

Mechanism by which a recently discovered allosteric inhibitor blocks glutamine metabolism in transformed cells

(2014) Clint A. Stalnecker et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Synthetic lethality of combined glutaminase and Hsp90 inhibition in mTORC1-driven tumor cells

(2014) Jing Li et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural Basis for the Active Site Inhibition Mechanism of Human Kidney-Type Glutaminase (KGA)

(2014) K. Thangavelu et al.   Scientific Reports

Kinetic characterization of ebselen, chelerythrine and apomorphine as glutaminase inhibitors

(2013) Ajit G. Thomas et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

In Vivo HIF-Mediated Reductive Carboxylation Is Regulated by Citrate Levels and Sensitizes VHL-Deficient Cells to Glutamine Deprivation

(2013) Paulo A. Gameiro et al.   Cell Metabolism

Glutaminase Isoenzymes as Key Regulators in Metabolic and Oxidative Stress Against Cancer

(2013) J.M. Mates et al.   CURRENT MOLECULAR MEDICINE

Therapeutic strategies impacting cancer cell glutamine metabolism

(2013) Michael J Lukey et al.   Future Medicinal Chemistry

Active Glutaminase C Self-assembles into a Supratetrameric Oligomer That Can Be Disrupted by an Allosteric Inhibitor

(2013) Amanda Petrina Scotá Ferreira et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Glutamine and cancer: cell biology, physiology, and clinical opportunities

(2013) Christopher T. Hensley et al.   JOURNAL OF CLINICAL INVESTIGATION

MYC-driven accumulation of 2-hydroxyglutarate is associated with breast cancer prognosis

(2013) Atsushi Terunuma et al.   JOURNAL OF CLINICAL INVESTIGATION

Glutamine supports pancreatic cancer growth through a KRAS-regulated metabolic pathway

(2013) Jaekyoung Son et al.   NATURE

Pan-cancer patterns of somatic copy number alteration

(2013) Travis I Zack et al.   NATURE GENETICS

A comparative study of short- and long-TE1H MRS at 3 T forin vivodetection of 2-hydroxyglutarate in brain tumors

(2013) Changho Choi et al.   NMR IN BIOMEDICINE

Small Angle X-Ray Scattering Studies of Mitochondrial Glutaminase C Reveal Extended Flexible Regions, and Link Oligomeric State with Enzyme Activity

(2013) Magda Møller et al.   PLoS One

Analysis of glutamine dependency in non-small cell lung cancer

(2012) A. Pieter J. van den Heuvel et al.   CANCER BIOLOGY & THERAPY

Glucose-Independent Glutamine Metabolism via TCA Cycling for Proliferation and Survival in B Cells

(2012) Anne Le et al.   Cell Metabolism

Analysis of Tumor Metabolism Reveals Mitochondrial Glucose Oxidation in Genetically Diverse Human Glioblastomas in the Mouse Brain In Vivo

(2012) Isaac Marin-Valencia et al.   Cell Metabolism

Modifying metabolically sensitive histone marks by inhibiting glutamine metabolism affects gene expression and alters cancer cell phenotype

(2012) Natalie E. Simpson et al.   Epigenetics

Comparative Evaluation of 18F-Labeled Glutamic Acid and Glutamine as Tumor Metabolic Imaging Agents

(2012) K. Ploessl et al.   JOURNAL OF NUCLEAR MEDICINE

Dibenzophenanthridines as Inhibitors of Glutaminase C and Cancer Cell Proliferation

(2012) William P. Katt et al.   MOLECULAR CANCER THERAPEUTICS

Glutaminolysis Activates Rag-mTORC1 Signaling

(2012) Raúl V. Durán et al.   MOLECULAR CELL

Structural basis for the allosteric inhibitory mechanism of human kidney-type glutaminase (KGA) and its regulation by Raf-Mek-Erk signaling in cancer cell metabolism

(2012) K. Thangavelu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Mitochondrial localization and structure-based phosphate activation mechanism of Glutaminase C with implications for cancer metabolism

(2012) A. Cassago et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Full-Length Human Glutaminase in Complex with an Allosteric Inhibitor

(2011) Byron DeLaBarre et al.   BIOCHEMISTRY

PET Imaging of Glutaminolysis in Tumors by 18F-(2S,4R)4-Fluoroglutamine

(2011) B. P. Lieberman et al.   JOURNAL OF NUCLEAR MEDICINE

Oncogenic K-Ras decouples glucose and glutamine metabolism to support cancer cell growth

(2011) D. Gaglio et al.   Molecular Systems Biology

Hypoxia promotes isocitrate dehydrogenase-dependent carboxylation of  -ketoglutarate to citrate to support cell growth and viability

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

Targeting Mitochondrial Glutaminase Activity Inhibits Oncogenic Transformation

(2010) Jian-Bin Wang et al.   CANCER CELL

Inhibition of Glutaminase Preferentially Slows Growth of Glioma Cells with Mutant IDH1

(2010) M. J. Seltzer et al.   CANCER RESEARCH

Glutaminase 2, a novel p53 target gene regulating energy metabolism and antioxidant function

(2010) W. Hu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

c-Myc suppression of miR-23a/b enhances mitochondrial glutaminase expression and glutamine metabolism

(2009) Ping Gao et al.   NATURE

Q's next: the diverse functions of glutamine in metabolism, cell biology and cancer

(2009) R J DeBerardinis et al.   ONCOGENE

Glutamine Deprivation Induces Abortive S-Phase Rescued by Deoxyribonucleotides in K-Ras Transformed Fibroblasts

(2009) Daniela Gaglio et al.   PLoS One

Tumor Cell Metabolism: Cancer's Achilles' Heel

(2008) Guido Kroemer et al.   CANCER CELL

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

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

Silibinin inhibits hypoxia-inducible factor-1α and mTOR/p70S6K/4E-BP1 signalling pathway in human cervical and hepatoma cancer cells: implications for anticancer therapy

(2008) P García-Maceira et al.   ONCOGENE

The Rag GTPases Bind Raptor and Mediate Amino Acid Signaling to mTORC1

(2008) Y. Sancak et al.   SCIENCE