Literature DB >> 30569503

Pharmacoinformatics and molecular docking reveal potential drug candidates against Schizophrenia to target TAAR6.

Rana Adnan Tahir1,2, Hao Wu3, Naima Javed2, Anila Khalique4, Seemab Amjad Fateh Khan5, Asif Mir6, Muhammad Saad Ahmed7, George E Barreto8, Hong Qing1, Ghulam Md Ashraf9, Sheikh Arslan Sehgal3,2,10.   

Abstract

Schizophrenia (SZ) is a complex disabling disorder that leads to the mental disability and afflicts 1% of the world's total population and placed in top ten medical disorders. In current work, bioinformatics analyses were carried out on Trace amine (TA)-associated receptor 6 (TAAR6) to recognize the potential drugs and compounds against SZ. Comparative modeling and threading-based approaches were utilized for the structure prediction of TAAR6. Fifty-nine predicted structures were evaluated by various model assessment techniques and final model having only eight amino acids in the outlier region and 98.5% overall quality factor was chosen for further pharmacoinformatics and molecular docking analyses. From an extensive literature review, 11 Food and Drug Administration (FDA) approved drugs were analyzed by computational techniques and Aripiprazole was found as the most effective drug against SZ by targeting TAAR6. Here, we report five novel molecules which exhibited the highest binding affinity, effective drug properties, and interestingly, observed better results than the approved selected drugs against SZ by targeting TAAR6. The docking analyses revealed that Arg-92, Trp-98, Gln-191, Thr-192, Ala-290, Cys-291, Tyr-293, and Glu-294 residues were observed as critical interacting residues in receptor-ligand interactions. Absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties, Lipinski rule of five, highest binding affinity coupled with virtual screening (VS), and pharmacophore modeling approach illustrated that aripiprazole (-8.6 kcal/mol) and TAAR6_0094 (-9.3 kcal/mol) are potential inhibitors for targeting TAAR6. It is suggested that schizophrenic patients have to use Aripiprazole for the medication of SZ by targeting TAAR6 and develop effective therapies by utilizing scrutinized novel compound.
© 2018 Wiley Periodicals, Inc.

Entities:  

Keywords:  in silico; molecular docking; pharmacoinformatics; schizophrenia (SZ); trace amine-associated receptor 6 (TAAR6); trace amines (TAs); virtual screening (VS)

Mesh:

Substances:

Year:  2018        PMID: 30569503     DOI: 10.1002/jcp.27999

Source DB:  PubMed          Journal:  J Cell Physiol        ISSN: 0021-9541            Impact factor:   6.384


  2 in total

1.  In Silico identification of angiotensin-converting enzyme inhibitory peptides from MRJP1.

Authors:  Rana Adnan Tahir; Afsheen Bashir; Muhammad Noaman Yousaf; Azka Ahmed; Yasmine Dali; Sanaullah Khan; Sheikh Arslan Sehgal
Journal:  PLoS One       Date:  2020-02-03       Impact factor: 3.240

2.  Public Transcriptomic Data Meta-Analysis Demonstrates TAAR6 Expression in the Mental Disorder-Related Brain Areas in Human and Mouse Brain.

Authors:  Anastasia N Vaganova; Nataliia V Katolikova; Ramilya Z Murtazina; Savelii R Kuvarzin; Raul R Gainetdinov
Journal:  Biomolecules       Date:  2022-09-07
  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.