|
Signalling proteins and transcription factors
|
|
|
mTORC1 |
Temsirolimus and Everolimus |
Metastatic/non-metastatic solid tumors |
US FDA approved |
| Ridaforolimus and other rapalogues |
Pancreatic, endometrial and glioblastoma; lymphoma. |
Phase I/II |
| mTORC1 and mTORC2 |
Torin1 and PP242 |
- |
Preclinical |
| HIF1α |
PX-478 |
Advanced solid tumor and lymphoma |
Phase I |
| Acriflavine |
- |
Preclinical |
| Hypoxia |
Tirapazamine and other bioreductive compounds |
Cervical, SCLC, NSCLC |
Phase III |
| Hypoxia, VEGF and VEGFR |
Bevacizumab |
Malignant glioma, NSCLC, ovarian and colorectal |
US FDA approved |
| IGF1R |
Dalotuzumab (MK-0646), BIIB022, AVE1642 etc. |
Solid tumors of NSCLC, pancreatic, hepatocellular carcinoma (HCC) and metastatic breast cancer |
Phase I/II |
| PI3K and mTOR |
BEZ235, XL765, SF1126 and BGT226 |
Malignant glioma and NSCLC |
Phase I/II |
| PI3K |
GDC-0941 and PX866 |
Metastatic breast cancer and non-Hodgkin’s lymphoma |
Phase I |
| AKT |
Perifosine and GSK690693 |
Renal cancer, NSCLC and lymphoma |
Phase I/II |
| AMPK and Complex I (mitochondrial) |
Metformin |
Solid tumors and lymphoma |
US FDA approved |
| Metabolic pathway enzymes |
| Nucleotide biosynthesis pathway |
DNA and RNA synthesis |
5-FU, cytarabine and methotrexate |
Different types of tumors |
US FDA approved |
| DNA synthesis |
Folate, choline, methionine, |
|
Lab studies |
| Methyltransferases |
Betaine, selected B vitamins, Flavonoids, EGCG, genistein |
|
Lab studies |
| Histone deacetylases (HDAC) |
Butyrate, sulforaphane, Allylmercaptan, 3,3-Diindolylmethane |
|
Lab studies |
| Histone acetyltranferase |
Anacardic acid, garcinol, Curcumin, EGCG, Genistein |
|
|
| Acetylation of non-histone proteins |
Butyrate, cambinol, Dihydrocoumarin, genistein |
|
|
| Glycolysis pathway |
GLUT1 |
Phloretin |
Colon cancer and leukemia |
- |
| GLUT1 |
WZB117 |
Lung cancer and breast cancer |
- |
| GLUT4 |
Ritonavir |
Multiple myeloma |
- |
| Hexokinase |
2-deoxyglucose (2-DG) |
Leukemia, cervical cancer, hepatocarcinoma, breast cancer, small lung cancer, lymphoma and prostate cancer |
PhaseI/II |
| Hexokinase Hexokinase |
Lonidamine (LND) |
Benign prostatic hyperplasia, leukemia and lymphoma |
Phase III |
| 3-bromopyruvate (3-BrPA) |
Leukemia, multiple myeloma, colon cancer and leukemia |
Preclinical |
| Pyruvate kinase M2 (PKM2) |
shRNA |
Lung cancer |
- |
| Pyruvate kinase (PK) |
TLN-232 |
Metastatic melanoma and renal cell carcinoma |
Phase II |
| Lactate dehydrogenase (LDHA) |
Oxamate |
Breast cancer |
|
| Pentose phosphate pathway (PPP) |
Glucose-6-phosphate dehydrogenase (G6PDH) |
Resveratrol |
Colon cancer |
|
| Transketolase (TK) |
Oxythiamine (OT) |
Colon cancer |
|
| G6PDH and TK |
Avemar |
Jurkat T cells (Leukemia) |
|
| G6PDH, 6PGDH and Transaldolase TA |
Combination of arginine and ascorbic acid |
Human hepatoma cell lines (HA2T/VGH) |
|
| G6PDH, also depletion of ribose-5-phosphate (R-5P) |
Dehydroepiandrosterone (DHEA) |
Indirect study on polycystic ovary syndrome |
|
| TCA cycle |
Pyruvate dehydrogenase kinase (PDK3) |
siRNA |
Cervical cancer and breast cancer |
|
| Pyruvate dehydrogenase kinase (PDK1) |
Dichloroacetate (DCA) |
Fibrosarcoma, colon cnacer, lung cancer, squamous cell carcinoma and prostate cancer |
|
| Fatty acid synthesis |
FASN |
Cerulenin and C75 |
Breast cancer |
|
| Orlistat |
Breast and pancreatic cancer |
Preclinical |
|
|
ATP-citrate lyase |
SB-204990 |
- |
Preclinical |
| Amino acid metabolism pathway |
Glutamine |
Phenylacetate |
Brain tumors |
Phase II |
| Asparagine |
Asparaginase and pegasparaginase |
Acute lymphoblastic leukaemia (ALL), T-cell lymphoma (TCL) and B-cell lymphoma (BCL) |
Phase II/III |
| Arginine |
Arginine deiminase |
Metastatic melanoma and hepatocellular carcinoma |
Phase I/II |
