Related Experiment Video
Updated: Apr 3, 2026

Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors
Published on: July 17, 2020
Understanding the Multifaceted Role of Ectonucleotide Pyrophosphatase/Phosphodiesterase 2 (ENPP2) and its Altered
1Center for Animal Sciences, School of Basic and Applied Sciences, Central University of Punjab, Bathinda, Pin Code: 151 001, Punjab, India. anilmantha@gmail.com.
Abstract:
Ectonucleotide pyrophosphatase/phosphodiesterase 2 (ENPP2) also known as Autotaxin, is a secreted lysophospholipase D, which hydrolyzes lysophosphatidylcholine (LPC) into Lysophosphatidic acid (LPA). LPA is the bioactive product of ENPP2 enzyme, which induces diverse signalling pathways via six LPA-G-protein coupled receptors (GPCRs). ENPP2 is an essential protein for normal development and its altered expression is associated with various human diseases. Cellular ENPP2 silencing results in lethality at the embryonic stage in mice. Initially, it is identified as an autocrine factor in melanoma cells. Different research groups are currently exploring to understand the multifaceted role of ENPP2 in various processes such as embryonic and neural development, migration, invasion, differentiation, proliferation, angiogenesis, and survival. Altered expression of ENPP2 is also associated with various diseases like inflammation, cancer, fibrosis, rheumatoid arthritis and neural defects. In this article, we have summarized structural aspects of ENPP2 and biochemical functions associated with its diverse cellular roles in various human diseases including cancer and Alzheimer's disease (AD). In addition, keeping in view and advocating findings, a note on various phytochemicals and synthetic inhibitors, which are currently explored as therapeutic agents targeting functions of ENPP2 for the treatment of various human diseases is also presented.
Related Concept Videos
Biosynthesis of Nucleic Acids
Protein Kinases and Phosphatases
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
Phosphodiester Linkages
Phosphodiester bond forms when a phosphoric acid molecule (H3PO4) links with two hydroxyl groups (–OH) of two other molecules, forming two ester bonds. Two water molecules are released in this process. The phosphodiester bond is commonly found in nucleic acids (DNA and RNA) and plays a critical role in their structure and function.
Phosphodiester Bonds Link Nucleotides Together
DNA and RNA are polynucleotides or long chains of nucleotides that are linked together. A nucleotide is...
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
Allosteric Proteins-ATCase
Aspartate transcarbamoylase (ATCase) is a cytosolic enzyme that catalyzes the condensation of L-aspartate and carbamoyl phosphate to N-carbamoyl-L-aspartate. This reaction is the first step in pyrimidine biosynthesis. UTP and CTP, the end products of the pyrimidine synthesis...
Pharmacogenetics of Phase II Enzymes: N-acetyltransferase, Thiopurine S-methyltransferase, UDP-glucuronosyltransferase

