Table 1.

Potential PIN1 inhibitors for cancer treatment

Drug	Details	Status
Juglone	First PIN1 inhibitor	Preclinical
	Irreversibly inhibits PIN1 PPIase activity
PiB	Specifically inhibits PIN1 PPIase activity	Preclinical
	Inhibits colon cancer cell proliferation
Dipentamethylene thiuram monosulfide	Specifically inhibits PIN1 PPIase activity	Preclinical
	Inhibits colon cancer cell proliferation
All-trans retinoic acid	Binds PIN1 and inhibits its activity	FDA approved for treatment of APL
	Inhibits breast cancer and APL cell proliferation
miRNAs	Bind to the 3’UTR of PIN1 mRNA	Preclinical
miR-200b/c	Suppress PIN1 expression in breast cancer and prostate cancer cells
miR-296-5p
Sorafenib	Multi-kinase inhibitor targeting Raf/Mek/Erk signalling pathway and tyrosine receptors	FDA approved for treatment of HCC
	Inhibits angiogenesis and growth of HCC tumours in vivo
	Inhibits phosphorylation of PIN1-interacting proteins (Mcl-1 and p70S6K)
	Improves overall survival and increases time to progression in HCC patients
Bortezomib	Proteasome inhibitor	FDA approved for treatment of multiple myeloma
	Suppresses expression of PIN1 and its transcription factor E2F
	Inhibits HCC cell proliferation in vitro

APL: Acute promyelocytic leukaemia; FDA: Food and Drug Administration; HCC: Hepatocellular carcinoma; PPIase: Peptidyl-prolyl isomerase.