Journal ArticleDOI
Efficacy of RNAi targeting of pyruvate kinase M2 combined with cisplatin in a lung cancer model
Wenhao Guo,Yu Zhang,Ting Chen,Yongsheng Wang,Jianxin Xue,Yonggang Zhang,Wenjing Xiao,Xianming Mo,You Lu +8 more
TLDR
Use of RNA interfering (RNAi) targeting PKM2 significantly inhibited tumor growth when combined with cisplatin in a human A549 lung cancer xenograft model, and may result in part from increased induction of apoptosis and augmented inhibition of cancer cell proliferation.Abstract:
Purpose
Pyruvate kinase isoenzyme M2 (PKM2) is a key enzyme in aerobic glycolysis; inhibition of PKM2 leads to the tumor growth inhibition. In this study, the effects of combined treatment with cisplatin (DDP) and a plasmid that expresses a short hairpin RNA (shRNA) targeting PKM2 on the growth of human A549 xenograft lung cancer model were investigated.read more
Citations
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Journal ArticleDOI
Targeting cellular metabolism to improve cancer therapeutics
TL;DR: The relationship between dysregulated cellular metabolism and cancer drug resistance is discussed and how targeting of metabolic enzymes can enhance the efficacy of common therapeutic agents or overcome resistance to chemotherapy or radiotherapy is discussed.
Journal ArticleDOI
Principles in the design of ligand-targeted cancer therapeutics and imaging agents
TL;DR: This Review describes the major principles in the design of ligand-targeted drugs and provides an overview of lig and–drug conjugates and ligand–imaging-agent conjugate that are currently in development.
Journal ArticleDOI
Emerging roles of PKM2 in cell metabolism and cancer progression.
Weibo Luo,Gregg L. Semenza +1 more
TL;DR: Pyruvate kinase M2 (PKM2) expression is increased and facilitates lactate production in cancer cells and represents an attractive target for cancer therapy.
Journal ArticleDOI
Review of aerobic glycolysis and its key enzymes – new targets for lung cancer therapy
TL;DR: The discovery of aerobic glycolysis in the 1920s has provided new means and potential therapeutic targets for lung cancer, and can be regulated by many oncoproteins to promote tumor proliferation, migration, and metastasis with dependence or independence of gly colysis.
Journal ArticleDOI
Pyruvate kinase M2-specific siRNA induces apoptosis and tumor regression
TL;DR: Knockdown of pyruvate kinase M2 induces apoptosis and tumor regression of multiple cancer types and is associated with death in several cancer types.
References
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Journal ArticleDOI
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TL;DR: This report examines cancer incidence, mortality, and survival by site, sex, race/ethnicity, education, geographic area, and calendar year, as well as the proportionate contribution of selected sites to the overall trends.
Journal ArticleDOI
The M2 splice isoform of pyruvate kinase is important for cancer metabolism and tumour growth
Heather R. Christofk,Matthew G. Vander Heiden,Marian H. Harris,Arvind Ramanathan,Robert E. Gerszten,Robert E. Gerszten,Ru Wei,Mark D. Fleming,Stuart L. Schreiber,Stuart L. Schreiber,Lewis C. Cantley,Lewis C. Cantley +11 more
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Journal ArticleDOI
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Rodrigo Arriagada,Bengt Bergman,Ariane Dunant,Le Chevalier T,J.P. Pignon,Johan Vansteenkiste +5 more
TL;DR: Cisplatin-based adjuvant chemotherapy improves survival among patients with completely resected non-small-cell lung cancer and had a significantly higher survival rate than those assigned to observation.
Journal ArticleDOI
Mitosis-specific phosphorylation of histone H3 initiates primarily within pericentromeric heterochromatin during G2 and spreads in an ordered fashion coincident with mitotic chromosome condensation.
Michael J. Hendzel,Y Wei,Michael A. Mancini,A. Van Hooser,Tamara A. Ranalli,Bill R. Brinkley,David P. Bazett-Jones,C D Allis +7 more
TL;DR: It is proposed that the singular phosphorylation of the amino-terminus of histone H3 may be involved in facilitating two key functions during mitosis: (1) regulate protein-protein interactions to promote binding of trans-acting factors that “drive” chromatin condensation as cells enter M-phase and (2) coordinate chromatin decondensation associated with M- phase.