Discovery and optimization of withangulatin A derivatives as novel glutaminase 1 inhibitors for the treatment of triple-negative breast cancer

Molecularly Engineering Triptolide with Aptamers for High Specificity and Cytotoxicity for Triple-Negative Breast Cancer

(2020) Jiaxuan He et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Discovery of a Thiadiazole–Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models

(2019) M. Raymond V. Finlay et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective Inhibition of Lysine-Specific Demethylase 5A (KDM5A) Using a Rhodium(III) Complex for Triple-Negative Breast Cancer Therapy

(2018) Guan-Jun Yang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Chemoresistance Evolution in Triple-Negative Breast Cancer Delineated by Single-Cell Sequencing

(2018) Charissa Kim et al.   CELL

Highlights of the Structure–Activity Relationships of Benzimidazole Linked Pyrrolidines Leading to the Discovery of the Hepatitis C Virus NS5A Inhibitor Pibrentasvir (ABT-530)

(2018) Rolf Wagner et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel 1,3,4-Selenadiazole-Containing Kidney-Type Glutaminase Inhibitors Showed Improved Cellular Uptake and Antitumor Activity

(2018) Zhao Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

A new synthetic derivative of cryptotanshinone KYZ3 as STAT3 inhibitor for triple-negative breast cancer therapy

(2018) Wenda Zhang et al.   Cell Death & Disease

17β-Hydroxywithanolides as Sensitizers of Renal Carcinoma Cells to Tumor Necrosis Factor-α Related Apoptosis Inducing Ligand (TRAIL) Mediated Apoptosis: Structure–Activity Relationships

(2017) Ya-Ming Xu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Evaluation of Thiazolidine-2,4-dione Derivatives as a Novel Class of Glutaminase Inhibitors

(2017) Teng-Kuang Yeh et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a small molecule targeting ULK1-modulated cell death of triple negative breast cancer in vitro and in vivo

(2017) Lan Zhang et al.   Chemical Science

13,14-seco-Withanolides fromPhysalis minimawith Potential Anti-inflammatory Activity

(2016) Ru Lin et al.   CHEMISTRY & BIODIVERSITY

1 H NMR spectroscopy-guided isolation of new sucrose esters from Physalis alkekengi var. franchetii and their antibacterial activity

(2016) Chuan-Yang Zhang et al.   FITOTERAPIA

Natural Products as Sources of New Drugs from 1981 to 2014

(2016) David J. Newman et al.   JOURNAL OF NATURAL PRODUCTS

Withaphysalin-type withanolides from Physalis minima

(2016) Xiao-Ming Xu et al.   Phytochemistry Letters

Allosteric Glutaminase Inhibitors Based on a 1,4-Di(5-amino-1,3,4-thiadiazol-2-yl)butane Scaffold

(2016) Sarah C. Zimmermann et al.   ACS Medicinal Chemistry Letters

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

(2016) Sarath Ramachandran et al.   Oncotarget

Cytotoxic withanolides from Physalis angulata var. villosa and the apoptosis-inducing effect via ROS generation and the activation of MAPK in human osteosarcoma cells

(2016) Ting Ma et al.   RSC Advances

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

(2015) N. Jacque et al.   BLOOD

Targeting Metabolic Remodeling in Glioblastoma Multiforme

(2015)   Oncotarget

Glutaminase: A Hot Spot For Regulation Of Cancer Cell Metabolism?

(2015)   Oncotarget

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

Withanolides from Physalis minima and their inhibitory effects on nitric oxide production

(2014) Yu-Zhou Guan et al.   STEROIDS

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

(2014) K. Thangavelu et al.   Scientific Reports

Glutamine Sensitivity Analysis Identifies the xCT Antiporter as a Common Triple-Negative Breast Tumor Therapeutic Target

(2013) Luika A. Timmerman et al.   CANCER CELL

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 regulation in cancer cells: a druggable chain of events

(2013) William P. Katt et al.   DRUG DISCOVERY TODAY

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

(2013) Jaekyoung Son et al.   NATURE

Analysis of glutamine dependency in non-small cell lung cancer

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

The Metabolic Profile of Tumors Depends on Both the Responsible Genetic Lesion and Tissue Type

(2012) Mariia O. Yuneva et al.   Cell Metabolism

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

(2012) Anne Le et al.   Cell Metabolism

Design, Synthesis, and Pharmacological Evaluation of Bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl Sulfide 3 (BPTES) Analogs as Glutaminase Inhibitors

(2012) Krupa Shukla et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Docosahexaenoic acid induces autophagy through p53/AMPK/mTOR signaling and promotes apoptosis in human cancer cells harboring wild-type p53

(2011) Kaipeng Jing et al.   Autophagy

Full-Length Human Glutaminase in Complex with an Allosteric Inhibitor

(2011) Byron DeLaBarre et al.   BIOCHEMISTRY

Pyruvate carboxylase is required for glutamine-independent growth of tumor cells

(2011) T. Cheng et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Glutamine Synthetase Is a Genetic Determinant of Cell Type–Specific Glutamine Independence in Breast Epithelia

(2011) Hsiu-Ni Kung et al.   PLoS Genetics

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

Mitochondrial metabolism and ROS generation are essential for Kras-mediated tumorigenicity

(2010) F. Weinberg et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Mitochondrial reactive oxygen species regulate cellular signaling and dictate biological outcomes

(2010) Robert B. Hamanaka et al.   TRENDS IN BIOCHEMICAL SCIENCES

Understanding the Warburg Effect: The Metabolic Requirements of Cell Proliferation

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