Table 4 inhibitors and drugs targeting collagen modifications
From: Understanding the matrix: collagen modifications in tumors and their implications for immunotherapy
Therapy target | Name drug | Drug format | Disease | Research stage |
|---|---|---|---|---|
P4HA1 | Diethyl-pythiDC | Small molecule inhibitor | Colorectal cancer | Preclinical [131] |
P4HA2 | Aspirin | Small molecule inhibitor | Hepatocellular carcinoma | Preclinical [132] |
P4H | EDHB | Small molecule inhibitor | Breast cancer | Preclinical [160] |
BMP1.3 | Anti-BMP1.3 | mAb | Myocardial infarction | Preclinical [134] |
LOX | BAPN (β-aminopropionitrile) PXS-5505 | Irreversible inhibitor Small molecule inhibitor | Cancer Pancreatic cancer | Preclinical [139] Preclinical [161] |
LOXL2 | Simtuzumab GS341 | mAb pAb | Fibrosis, Cancer | Phase II [162] |
LOXL2 | PXS-S1A PXS-S2A PAT-1251 PXS-5382A Epigallocatechin gallate (EGCG) | Small molecule inhibitors | Fibrosis, heart failure, glaucoma, oncological and angiogenic diseases | Phase II [135] Phase II [135] Phase I [135] Phase I [166] |
Copper | tetrathiomolybdate (TM)I d-penicillamine (D-pen) | Copper chelators | Cancer Breast cancer | |
Dual LOX/LOXL | PXS-5153A CCT365623 | Inhibitor | Fibrosis Cancer | Preclinical [169] |
MMP9 MMP9 MMP14 MMP1, MMP2, MMP3 | Andecaliximab (GS-5745) AB0041, AB0046, DX-2400 Single Chain Fragment Variables | mAb mAb mAb mAb | Cancer, Colorectal cancer Breast, melanoma, sarcoma Breast cancer | Preclinical [175] Preclinical [176] |
PAD4 PAD4 PAD4 PAD4 | TDFA TDCA Cl-amidine F-amidine GSK199, GSK484 JBI-589 | Selective Irreversible small molecule inhibitors Reversible inhibitors Small molecule | Inflammatory disorders and Cancer Cancer | Preclinical [177] Preclinical [177] Preclinical [114] |