Table 4.

Selected examples of HSPG targeting-based therapeutics for cancers.

Type of Drug	Target	Type(s) of Cancer	Reference(s)
Anti-GPC1 monoclonal antibody	Glypican-1	Esophageal squamous cell carcinoma	[244]
Monoclonal antibody HS20	Glypican-3 HS chain	Hepatocellular carcinoma	[245,246]
Human single-domain antibody specific for GPC2	Glypican-2	Neuroblastoma	[247]
Human recombinant antibody OC-46F2	Syndecan-1 ectodomain	Melanoma Ovarian carcinoma	[193] [248]
Antibody-pyrrolobenzodiazepine conjugate	Glypican-2	Neuroblastoma	[249]
Antibody-auristatin F conjugate	Glypican-1	Uterine cervical squamous cell carcinoma	[250]
HS mimetics G2.2	HSPG induced MAPK activation	Colon cancer stem cells	[251,252]
HS mimetics OTR4120 and OTR4131	HSPGs-mediated RANTES signaling	Hepatocellular carcinoma	[253]
Peptidic HS mimetics Synstatin	Syndecan-1/integrin/IGF1 complex formation	Mammary tumors Hepatocellular carcinoma	[210,226] [254]
Xylosides	HSPG biosynthesis	Glioma Lung cancer	[165,255,256] [257]
HS mimetics RK-682	Heparanase	Bladder cancer	[92,258,259]
HS mimetics PG545 (Pixatimod)	Heparanase	Mesothelioma Lymphoma Breast cancer	[260] [261] [262]
HS mimetics SST0001 (Roneparstat)	Heparanase	Sarcoma Myeloma	[263,264] [101]
HS mimetics M402 (Necuparanib)	Heparanase	Pancreatic cancer	[251,263,265]
HS mimetics PI-88 (Mupafostat)	Heparanase and Endoglucosamine 6-sulfatase	Hepatocellular carcinoma	[251,263]
Monoclonal antibodies 9E8 and H1023	Heparanase	Lymphoma Myeloma	[266] [266]
Triazolo-thiadiazoles	Heparanase	Hepatocellular carcinoma Lung cancer	[267] [267]
Phenyl sulfonyl compound OKN-007	Sulfatase 2	Hepatocellular carcinoma Glioblastoma	[268] [269]
Proteasome inhibitor (Bortezomib)	Sulfatase 2	Breast cancer	[270]