Table 1 ECM as a therapeutic target in cancer

From: Extracellular matrix and its therapeutic potential for cancer treatment

Drug illustration

Function

Characteristic

Halofuginone

Inhibiting TGF-β signaling pathway and collagen synthesis

Anticoccidial drug

Fresolimumab

Inhibiting collagen synthesis

Monoclonal antibody targeting TGF-β

Collagenases

Collagen degradation

Enzyme

Relaxin

Promoting the synthesis of collagenase

Hormone

MMPs

Collagen degradation

Enzyme

GS-6624

Inhibition of collagen cross-linking

Monoclonal antibody targeting LOXL2

SB-431542 and SB-505124

Inhibiting ALK4/5/7 kinase to block TGF-β pathway

Imidazole analog

Ki26894

Inhibitor of TGFβR1

Small-molecule inhibitor

Candesartan

Angiotensin receptor blockers

Long-acting angiotensin receptor antagonist

4-methylumbelliferone (4-MU)

Inhibitor of HA synthesis

Umbelliferone derivatives

Hyaluronidase

HA degradation

Enzyme

BC-1

Targeting fibronectin for drug delivery

Monoclonal antibody

L19

Targeting fibronectin for delivering drugs and radionuclide

Monoclonal antibody

APTEDB

Targeting fibronectin for drug delivery

High-affinity peptides

Vitaxin

Targeting integrin and preventing angiogenesis

Monoclonal antibody targeting integrin αvβ3

Volociximab

Targeting integrin and inhibiting neoangiogenesis

Monoclonal antibody targeting α5β1 integrin

1a-RGD

Targeting the RGD-integrins interaction

Small-molecule integrin antagonist

Cilengitide

Inhibitor of αvβ3 and αvβ5 integrins

Specific peptide antagonist

Imatinib, nilotinib, and dasatinib

Inhibiting tyrosine kinase and DDR signaling pathway

Benzene ammonia pyrimidine derivatives

Bivatuzumab

Blocking CD44-HA interaction

Monoclonal antibody against CD44v6

Verbascoside

Inhibitor for CD44 dimerization

phenylpropanoids

Tranilast

Suppressing TGF-β signaling and expression of extracellular matrix components

Derivative of the amino acid tryptophan

Pirfenidone

Inhibiting TGF-β/Smad and anti-inflammation

Pyridones

Fasudil

Rho-kinase inhibitor

Isoquinoline sulfonamide derivatives

Metformin

Reducing TGF-β signaling, IL-1β, and M2 tumor-associated macrophages infiltration

Biguanides

Dexamethasone

Suppressing angiogenesis and normalizes vessel morphology

Glucocorticoid steroid

Hydroxychloroquine

Macropinocytosis inhibitors

Derivatives of 4-aminoquinoline

All-trans retinoic acid

Retinoic acid receptor agonists

Vitamin

Defactinib

FAK inhibitors and antiangiogenic effect

Benzamides

Ibrutinib

Inhibitor of Bruton tyrosine kinase to interrupt BCR signaling in CLL

Benzene ammonia pyrimidine derivatives

RG7356

Blocking the signaling of CD44 in CLL

Humanized monoclonal antibody for CD44