Inhibitors of glucose transport and glycolysis as novel anticancer therapeutics

Table 1 Glycolytic inhibitors and modulators

Compound name	Target protein	Status	Ref.
2-DG	Inhibits HK	Phase I-completed (Jul 2008) Phase I/II-terminated (Mar 2011)	NCT00096707 NCT00633087
3-BP	Inhibits HK	Pre-clinical	[66-74]
Lonidamine	Inhibits mitochondrial HK2	Phase II/III-terminated (Aug/Dec 2006)	NCT00237536 NCT00435448
3PO	Inhibits PFK2	Pre-clinical	[90]
N4A, YZ9	Inhibits PFK2	Pre-clinical	[91]
PGMI-004A	Inhibits PGAM1	Pre-clinical	[96]
MJE3	Inhibits PGAM1	Pre-clinical	[98]
TT-232	Inhibits PKM2	Phase II-completed (Mar 2008) Phase II-terminated (Oct 2010)	NCT00422786 NCT00735332
Shikonin/alkannin	Inhibits PKM2	Pre-clinical	[108]
ML265 (TEPP-46)	Activates PKM2	Pre-clinical	[116,117]
FX11	Inhibits LDHA	Pre-clinical	[126]
Quinoline 3-sulfonamides	Inhibit LDHA	Pre-clinical	[141]
DCA	Inhibits PDK	Phase I-ongoing Phase I-ongoing Phase II-completed (Aug 2009)	NCT00566410 NCT01111097 NCT00540176
6-AN	Inhibits G6PD	Pre-clinical	[159-161]
Oxythiamine	Inhibits TKTL1	Pre-clinical	[170-173]

2-DG: 2-deoxyglucose; 3-BP: 3-bromopyruvate; DCA: Dichloroacetate; 6-AN: 6-aminonicotinamide; HK: Hexokinase; PFK: Phosphofructokinase; PGAM: Phosphoglycerate mutase; PKM2: Pyruvate kinase M2; LDH: Lactate dehydrogenase; PDK: Pyruvate dehydrogenase kinase; G6PD: Glucose-6-phosphate dehydrogenase; TKTL1: Transketolase-like enzyme 1.