Targeting cellular metabolism to improve cancer therapeutics

Y Zhao, EB Butler, M Tan - Cell death & disease, 2013 - nature.com
The metabolic properties of cancer cells diverge significantly from those of normal cells.
Energy production in cancer cells is abnormally dependent on aerobic glycolysis. In addition …

The Warburg effect then and now: from cancer to inflammatory diseases

EM Palsson‐McDermott, LA O'neill - Bioessays, 2013 - Wiley Online Library
Inflammatory immune cells, when activated, display much the same metabolic profile as a
glycolytic tumor cell. This involves a shift in metabolism away from oxidative phosphorylation …

Metabolic modulation of glioblastoma with dichloroacetate

ED Michelakis, G Sutendra, P Dromparis… - Science translational …, 2010 - science.org
Solid tumors, including the aggressive primary brain cancer glioblastoma multiforme,
develop resistance to cell death, in part as a result of a switch from mitochondrial oxidative …

Dichloroacetate (DCA) as a potential metabolic-targeting therapy for cancer

ED Michelakis, L Webster, JR Mackey - British journal of cancer, 2008 - nature.com
The unique metabolism of most solid tumours (aerobic glycolysis, ie, Warburg effect) is not
only the basis of diagnosing cancer with metabolic imaging but might also be associated …

Lactate inhibits lipolysis in fat cells through activation of an orphan G-protein-coupled receptor, GPR81

C Liu, J Wu, J Zhu, C Kuei, J Yu, J Shelton… - Journal of Biological …, 2009 - ASBMB
Lactic acid is a well known metabolic by-product of intense exercise, particularly under
anaerobic conditions. Lactate is also a key source of energy and an important metabolic …

Mitaplatin, a potent fusion of cisplatin and the orphan drug dichloroacetate

S Dhar, SJ Lippard - … of the National Academy of Sciences, 2009 - National Acad Sciences
The unique glycolytic metabolism of most solid tumors, known as the Warburg effect, is
associated with resistance to apoptosis that enables cancer cells to survive. Dichloroacetate …

Dichloroacetate and cancer: new home for an orphan drug?

S Kankotia, PW Stacpoole - Biochimica et Biophysica Acta (BBA)-Reviews …, 2014 - Elsevier
We reviewed the anti-cancer effects of DCA, an orphan drug long used as an investigational
treatment for various acquired and congenital disorders of mitochondrial intermediary …

New insights into p53 signaling and cancer cell response to DNA damage: implications for cancer therapy

R Mirzayans, B Andrais, A Scott… - BioMed Research …, 2012 - Wiley Online Library
Activation of the p53 signaling pathway by DNA‐damaging agents was originally proposed
to result either in cell cycle checkpoint activation to promote survival or in apoptotic cell …

Pyruvate dehydrogenase kinase as a novel therapeutic target in oncology

G Sutendra, ED Michelakis - Frontiers in oncology, 2013 - frontiersin.org
Current drug development in oncology is non-selective as it typically focuses on pathways
essential for the survival of all dividing cells. The unique metabolic profile of cancer, which is …

Surface-functionalization of Zr-fumarate MOF for selective cytotoxicity and immune system compatibility in nanoscale drug delivery

I Abánades Lázaro, S Haddad… - … applied materials & …, 2018 - ACS Publications
Metal–organic frameworks (MOFs), network structures wherein metal ions or clusters link
organic ligands into porous materials, are being actively researched as nanoscale drug …