Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2021 Mar;35(3):e22659.
doi: 10.1002/jbt.22659. Epub 2020 Nov 6.

Discovery of novel 1,3,5-triazine as adenosine A2A receptor antagonist for benefit in Parkinson's disease

Anup Masih  1 , Amol K Agnihotri  1 , Jitendra K Srivastava  1 , Nidhi Pandey  2 , Hans R Bhat  3 , Udaya P Singh  1
Affiliations

Discovery of novel 1,3,5-triazine as adenosine A2A receptor antagonist for benefit in Parkinson's disease

Anup Masih et al. J Biochem Mol Toxicol. 2021 Mar.

Abstract

Parkinson's disease (PD) is a chronic neuro-degenerative ailment characterized by impairment in various motor and nonmotor functions of the body. In the past few years, adenosine A2 A receptor (A2 AR) antagonists have attracted much attention due to significant relief in PD. Therefore, in the current study, we intend to disclose the development of novel 1,3,5-triazines as A2 AR antagonist. The radioligand binding and selectivity of analogs were tested in HEK293 (human embryonic kidney) and the cells were transfected with pcDNA 3.1(+) containing full-length human A2 AR cDNA and pcDNA 3.1(+) containing full-length human A1 R cDNA, where they exhibit selective affinity for A2 AR. Molecular docking analysis was also conducted to rationalize the probable mode of action, binding affinity, and orientation of the most potent molecule (7c) at the active site of A2 AR. It has been shown that compound 7c form numerous nonbonded interactions in the active site of A2 AR by interacting with Ala59, Ala63, Ile80, Val84 Glu169, Phe168, Met270, and Ile274. The study revealed 1,3,5-triazines as a novel class of A2 AR antagonists.

Keywords: 1,3,5-triazine; Parkinson's disease; adenosine A2A receptor; antagonist; docking.

PubMed Disclaimer

References

REFERENCES

    1. R. Balestrino, A. H. V. Schapira, Eur. J. Neurol. 2020, 27(1), 27. https://doi.org/10.1111/ene.14108
    1. A. H. V. Schapira, K. R. Chaudhuri, P. Jenner, Nat. Rev. Neurosci. 2017, 18(7), 435. https://doi.org/10.1038/nrn.2017.62
    1. T.Wyss-Coray, Ageing, neurodegeneration and brain rejuvenation, Nature 2016, 539(7628), 180. https://doi.org/10.1038/nature20411
    1. E. R. Dorsey, R. Constantinescu, J. P. Thompson, K. M. Biglan, R. G. Holloway, K. Kieburtz, F. J. Marshall, B. M. Ravina, G. Schifitto, A. Siderowf, C. M. Tanner, Neurology 2007, 68(5), 384. https://doi.org/10.1212/01.wnl.0000247740.47667.03
    1. D. T. Dextera, P. Jenner, Free Radic. Biol. Med. 2013, 62, 132. https://doi.org/10.1016/j.freeradbiomed.2013.01.018

MeSH terms

LinkOut - more resources