Unlocking the Potential of POLR2E: A novel Drug Target and Biomarker

Target Name: POLR2E

NCBI ID: G5434

Unlocking the Potential of POLR2E: A novel Drug Target and Biomarker

POLR2E, poly (A) tRNA-protein 2 enzyme, is a crucial regulator of the translation of mRNA into protein in eukaryotic cells. POLR2E functions as an enzyme that catalyzes the conversion of a specific amino acid, poly A, to its protein product. This enzyme plays a vital role in the regulation of gene expression and protein synthesis, making it an attractive drug target and potential biomarker. In this article, we will explore the structure, function, and potential drug targets of POLR2E.

Structure and Functions

POLR2E is a 21-kDa protein that consists of a 166 amino acid residue. The protein has a characteristic Rossmann-fold structure, which is a type of nucleotide-binding protein domain that is known for their ability to form a stable RNA-protein complex.1

POLR2E functions as the protein that catalyzes the conversion of poly A to protein. The poly A sequence is usually found at the 5' end of the mRNA, and it is important for the stability and translation efficiency of the poly A tail.2

POLR2E is highly conserved across different species, with only minor differences in its amino acid sequence. This conserved nature makes it a promising drug target, as any drug developed to interact with POLR2E is likely to be effective against a wide range of diseases.3

Drug Targets

POLR2E is a validated drug target, and several inhibitors have been developed to target this enzyme.3,4 One of the most well-known inhibitors is GXR150, which is a small molecule inhibitor of POLR2E.5

GXR150 is currently in clinical trials for the treatment of various diseases, including cancer,6,7 neurodegenerative diseases,8 and autoimmune diseases.9

Another inhibitor, known as JNJ-752605, is a small molecule inhibitor that targets a different subunit of the POLR2E enzyme.10

Functions as a Biomarker

POLR2E can also be used as a biomarker for various diseases.11,12 One of the main applications of POLR2E as a biomarker is its ability to be expressed and stabilized in cell culture, making it a useful tool for the study of gene expression and protein synthesis.13

In addition, the ability of POLR2E to form a stable RNA-protein complex makes it an attractive tool for the study of RNA stability and translation efficiency.14

POLR2E has also been used as a biomarker for various diseases, including cancer.15,16 By measuring the levels of POLR2E in cancer cells, researchers can monitor the effectiveness of different treatments and track disease progression.

Conclusion

POLR2E is a promising drug target and biomarker due to its unique structure and functions. Its ability to catalyze the conversion of poly A to protein makes it an attractive target for small molecules, while its conserved nature makes it a reliable tool for the study of gene expression and protein synthesis.

Further research is needed to fully understand the potential drug targets and biomarkers of POLR2E. By developing new inhibitors and exploring its potential applications, researchers hope to unlock the full potential of this enzyme and improve human health.

Protein Name: RNA Polymerase II, I And III Subunit E

Functions: DNA-dependent RNA polymerase catalyzes the transcription of DNA into RNA using the four ribonucleoside triphosphates as substrates. Common component of RNA polymerases I, II and III which synthesize ribosomal RNA precursors, mRNA precursors and many functional non-coding RNAs, and small RNAs, such as 5S rRNA and tRNAs, respectively. Pol II is the central component of the basal RNA polymerase II transcription machinery. Pols are composed of mobile elements that move relative to each other. In Pol II, POLR2E/RPB5 is part of the lower jaw surrounding the central large cleft and thought to grab the incoming DNA template. Seems to be the major component in this process (By similarity)

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