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. 2022 Sep 10;23(18):10509. doi: 10.3390/ijms231810509

Table 2.

A summary of drugs targeting the synthesis and secretion of collagens.

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]