Receptor Tyrosine Phosphatases as Drug Targets

Receptor Tyrosine Phosphatases as Drug Target Background

Receptor tyrosine phosphatases (RTPs) are considered next-generation drug targets for the reason that dysregulation of receptor tyrosine phosphorylation is a major cause of human diseases, such as cancers, diabetes, autoimmune disorders, and neurological diseases.

Indeed, receptor tyrosine phosphorylation-mediated signaling events offer ample therapeutic targets, and drug discovery efforts to date have brought over two dozen kinase inhibitors to the clinic.

For instance, PTP1B is a well-known drug targets of type 2 diabetes and obesity, and recent studies indicate that it is also a promising target for breast cancer. SHP2 is a bona-fide oncoprotein, mutations of which cause juvenile myelomonocytic leukemia, acute myeloid leukemia, and solid tumors. In addition, LYP is strongly associated with type 1 diabetes and many other autoimmune diseases.

Receptor tyrosine phosphatases (RTPs) reversibly and coordinately control cellular protein tyrosine phosphorylation levels, which are important for nearly all cellular processes, such as growth, differentiation, migration, survival, and apoptosis.

Receptor Tyrosine Phosphatases as Drug Target List

Drug target HGNC-approved name
PTPRA Protein tyrosine phosphatase, receptor type, A
PTPRC Protein tyrosine phosphatase, receptor type, C
PTPRD Protein tyrosine phosphatase, receptor type, D
PTPRJ Protein tyrosine phosphatase, receptor type, J
PTPRK Protein tyrosine phosphatase, receptor type, K
PTPRR Protein tyrosine phosphatase, receptor type, R
PTPRS Protein tyrosine phosphatase, receptor type, S

Non-Receptor Tyrosine Phosphatases as Drug Target List

Drug target HGNC-approved name
PTPN1 Protein tyrosine phosphatase, non-receptor type 1
PTPN2 Protein tyrosine phosphatase, non-receptor type 2
PTPN3 Protein tyrosine phosphatase, non-receptor type 3
PTPN6 Protein tyrosine phosphatase, non-receptor type 6
PTPN9 Protein tyrosine phosphatase, non-receptor type 9
PTPN11 Protein tyrosine phosphatase, non-receptor type 11
PTPN12 Protein tyrosine phosphatase, non-receptor type 12
PTPN22 Protein tyrosine phosphatase, non-receptor type 22 (lymphoid)

References

1. He R, et al. Protein tyrosine phosphatases as potential therapeutic targets[J]. Acta Pharmacologica Sinica, 2014, 35(10): 1227-1246.

2. M Scott L, et al. Targeting protein tyrosine phosphatases for anticancer drug discovery[J]. Current pharmaceutical design, 2010, 16(16): 1843-1862.