Cellular Pharmacodynamics of a Novel Pyrrolo[3,2-d]pyrimidine Inhibitor Targeting Mitochondrial and Cytosolic One-Carbon Metabolism

Novel pyrrolo[3,2-d]pyrimidine compounds target mitochondrial and cytosolic one-carbon metabolism with broad-spectrum antitumor efficacy

(2019) Aamod S. Dekhne et al.   MOLECULAR CANCER THERAPEUTICS

Fluorine-Substituted Pyrrolo[2,3-d]Pyrimidine Analogues with Tumor Targeting via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of de Novo Purine Nucleotide Biosynthesis

(2018) Manasa Ravindra et al.   JOURNAL OF MEDICINAL CHEMISTRY

Serine Catabolism by SHMT2 Is Required for Proper Mitochondrial Translation Initiation and Maintenance of Formylmethionyl-tRNAs

(2018) Denise R. Minton et al.   MOLECULAR CELL

Mitochondrial translation requires folate-dependent tRNA methylation

(2018) Raphael J. Morscher et al.   NATURE

mTOR mediates a mechanism of resistance to chemotherapy and defines a rational combination strategy to treat KRAS-mutant lung cancer

(2018) Shun-Qing Liang et al.   ONCOGENE

Mitochondrial One-Carbon Pathway Supports Cytosolic Folate Integrity in Cancer Cells

(2018) Yuxiang Zheng et al.   CELL

Human SHMT inhibitors reveal defective glycine import as a targetable metabolic vulnerability of diffuse large B-cell lymphoma

(2017) Gregory S. Ducker et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Serine and Functional Metabolites in Cancer

(2017) Alice C. Newman et al.   TRENDS IN CELL BIOLOGY

Overexpression of mitochondrial serine hydroxyl-methyltransferase 2 is associated with poor prognosis and promotes cell proliferation and invasion in gliomas

(2017) Ming Wu et al.   OncoTargets and Therapy

The mTORC1 Signaling Network Senses Changes in Cellular Purine Nucleotide Levels

(2017) Gerta Hoxhaj et al.   Cell Reports

Reversal of Cytosolic One-Carbon Flux Compensates for Loss of the Mitochondrial Folate Pathway

(2016) Gregory S. Ducker et al.   Cell Metabolism

Tumour-specific proline vulnerability uncovered by differential ribosome codon reading

(2016) Fabricio Loayza-Puch et al.   NATURE

Prognostic and therapeutic value of mitochondrial serine hydroxyl-methyltransferase 2 as a breast cancer biomarker

(2016) Lahong Zhang et al.   ONCOLOGY REPORTS

KRAS-related proteins in pancreatic cancer

(2016) Karen M. Mann et al.   PHARMACOLOGY & THERAPEUTICS

Hypoxia induces the breast cancer stem cell phenotype by HIF-dependent and ALKBH5-mediated m6A-demethylation of NANOG mRNA

(2016) Chuanzhao Zhang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Serine one-carbon catabolism with formate overflow

(2016) J. Meiser et al.   Science Advances

6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Regioisomers as Targeted Antifolates for Folate Receptor α and the Proton-Coupled Folate Transporter in Human Tumors

(2015) Lei Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

SHMT2 drives glioma cell survival in ischaemia but imposes a dependence on glycine clearance

(2015) Dohoon Kim et al.   NATURE

Mammalian Mitochondrial and Cytosolic Folylpolyglutamate Synthetase Maintain the Subcellular Compartmentalization of Folates

(2014) Scott A. Lawrence et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Current clinical regulation of PI3K/PTEN/Akt/mTOR signalling in treatment of human cancer

(2014) Hui Jun Lim et al.   JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY

Metabolic enzyme expression highlights a key role for MTHFD2 and the mitochondrial folate pathway in cancer

(2014) Roland Nilsson et al.   Nature Communications

Serine Catabolism Regulates Mitochondrial Redox Control during Hypoxia

(2014) J. Ye et al.   Cancer Discovery

Discovery of 5-Substituted Pyrrolo[2,3-d]pyrimidine Antifolates as Dual-Acting Inhibitors of Glycinamide Ribonucleotide Formyltransferase and 5-Aminoimidazole-4-carboxamide Ribonucleotide Formyltransferase in De Novo Purine Nucleotide Biosynthesis: Implications of Inhibiting 5-Aminoimidazole-4-carboxamide Ribonucleotide Formyltransferase to AMPK Activation and Antitumor Activity

(2013) Shermaine Mitchell-Ryan et al.   JOURNAL OF MEDICINAL CHEMISTRY

The human proton-coupled folate transporter

(2012) Sita Kugel Desmoulin et al.   CANCER BIOLOGY & THERAPY

Metabolite Profiling Identifies a Key Role for Glycine in Rapid Cancer Cell Proliferation

(2012) M. Jain et al.   SCIENCE

Oxidative Stress and Antioxidant Defense

(2012) Esra Birben et al.   World Allergy Organization Journal

Mechanisms of Membrane Transport of Folates into Cells and Across Epithelia

(2011) Rongbao Zhao et al.   Annual Review of Nutrition

Regulation and function of ribosomal protein S6 kinase (S6K) within mTOR signalling networks

(2011) Brian Magnuson et al.   BIOCHEMICAL JOURNAL

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

Tetrahydrofolate Recognition by the Mitochondrial Folate Transporter

(2011) Scott A. Lawrence et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Synthesis, Biological, and Antitumor Activity of a Highly Potent 6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Antifolate Inhibitor with Proton-Coupled Folate Transporter and Folate Receptor Selectivity over the Reduced Folate Carrier That Inhibits β-Glycinamide Ribonucleotide Formyltransferase

(2011) Lei Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Therapeutic Targeting of a Novel 6-Substituted Pyrrolo [2,3-d]pyrimidine Thienoyl Antifolate to Human Solid Tumors Based on Selective Uptake by the Proton-Coupled Folate Transporter

(2011) S. Kugel Desmoulin et al.   MOLECULAR PHARMACOLOGY

The Ras-ERK and PI3K-mTOR pathways: cross-talk and compensation

(2011) Michelle C. Mendoza et al.   TRENDS IN BIOCHEMICAL SCIENCES

Compartmentalization of Mammalian Folate-Mediated One-Carbon Metabolism

(2010) Anne S. Tibbetts et al.   Annual Review of Nutrition

Biochemical and biophysical characterization of succinate: Quinone reductase from Thermus thermophilus

(2010) Olga Kolaj-Robin et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOENERGETICS

Pemetrexed Indirectly Activates the Metabolic Kinase AMPK in Human Carcinomas

(2010) S. B. Rothbart et al.   CANCER RESEARCH

Therapeutics by Cytotoxic Metabolite Accumulation: Pemetrexed Causes ZMP Accumulation, AMPK Activation, and Mammalian Target of Rapamycin Inhibition

(2009) Alexandra C. Racanelli et al.   CANCER RESEARCH

Synthesis and Biological Activity of a Novel Series of 6-Substituted Thieno[2,3-d]pyrimidine Antifolate Inhibitors of Purine Biosynthesis with Selectivity for High Affinity Folate Receptors over the Reduced Folate Carrier and Proton-Coupled Folate Transporter for Cellular Entry†

(2009) Yijun Deng et al.   JOURNAL OF MEDICINAL CHEMISTRY

N-linked glycosylation and its impact on the electrophoretic mobility and function of the human proton-coupled folate transporter (HsPCFT)

(2008) Ersin Selcuk Unal et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

A Role for the Proton-coupled Folate Transporter (PCFT-SLC46A1) in Folate Receptor-mediated Endocytosis

(2008) Rongbao Zhao et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Synthesis and Discovery of High Affinity Folate Receptor-Specific Glycinamide Ribonucleotide Formyltransferase Inhibitors with Antitumor Activity

(2008) Yijun Deng et al.   JOURNAL OF MEDICINAL CHEMISTRY