Table 2.
Therapeutics Target | Drug | Mechanism | Cancer Type | Status | Reference |
---|---|---|---|---|---|
collagen type I | Baicalein | inhibiting collagen type I transcription by alleviating TGF-β1 stimulation | lung cancer, osteosarcoma cells, bladder cancer, breast cancer, pancreatic cancer, cervical cancer, oral cancer | a promising candidate awaiting further testing | [163,164,165] |
Phenylbutyrate, sodium phenylbutyrate | as a weak histone deacetylase inhibitor decreasing collagen type I Alpha 1 mRNA transcription | lung cancer, prostate cancer, liver cancer, breast cancer, ovarian cancer, bladder cancer | a promising candidate awaiting further testing | [166,167,168,169,170,171] | |
C9 | C9 inhibits collagen production by dissociating laribonucleoprotein domain family member 6 (LARP6) from type I collagen 50′SL RNA | - | awaiting further testing | [172] | |
Ethyl 3,4-dihydroxybenzoate (EDHB), 2-(5-carboxythiazol-2-yl) pyridine-5-carboxylic acid (pythiDC) |
inhibiting collagen synthesis by inhibiting Prolyl 4-hydroxylases (P4Hs), which is a synthesis and regulatory factor of collagen type I | colorectal cancer, breast cancer | awaiting further testing | [160,173,174] | |
Minoxidil | inhibiting collagen synthesis by inhibitor lysyl hydroxylases (LHs), which is a synthesis and regulatory factor of collagen type I | prostate cancer, breast cancer, ovarian cancer | a promising candidate awaiting further testing | [161,162,175,176] | |
AK-778 | inhibiting collagen synthesis by mitigating the interaction between collagen and HSP47, which is a molecule required for collagen type I maturation. | - | a promising candidate awaiting further testing | [177,178] | |
CCT365623 | decreasing collagen synthesis by inhibiting lysyl oxidase (LOX), which is a regulatory factor for collagen cross-linking | - | a promising candidate awaiting further testing | [179,180] | |
collagen type XI | LY2157299 | inhibiting collagen XI alpha 1 chain (COL11A1) expression by inhibiting the transforming growth factor beta receptor 1 (TβRI) | ovarian cancer, pancreatic cancer, breast cancer | phase II clinical trial | [181,182,183,184,185] |
SC66 | as an Akt inhibitor preventing the transcription of COL11A1 | colon cancer, ovarian cancer, bladder cancer, lung cancer | under clinical trials | [182,186,187,188,189] | |
collagen type XI | AK778 and its cleavage product Col003 | disrupted collagen binding with the molecular chaperone HSP47 and inhibited collagen secretion | - | awaiting further clinical studies | [177,182] |