EUROPEAN JOURNAL OF
PHARMACEUTICAL AND MEDICAL RESEARCH

( An ISO 9001:2015 Certified International Journal )

An International Peer Reviewed Journal for Pharmaceutical, Medical & Biological Sciences

An Official Publication of Society for Advance Healthcare Research (Reg. No. : 01/01/01/31674/16)

European Journal of Pharmaceutical and Medical Research (EJPMR) has indexed with various reputed international bodies like : Google Scholar , Indian Science Publications , InfoBase Index (In Process) , SOCOLAR, China , Research Bible, Fuchu, Tokyo. JAPAN , International Society for Research activity (ISRA) , Scientific Indexing Services (SIS) , Polish Scholarly Bibliography , Global Impact Factor (GIF) (Under Process) , Universal Impact Factor , International Scientific Indexing (ISI), UAE  , Index Copernicus , CAS (A Division of American Chemical Society) USA (Under Process) , Directory of Open Access Journal (DOAJ, Sweden, in process) , UDLedge Science Citation Index , CiteFactor , Directory Of Research Journal Indexing (DRJI) , Indian citation Index (ICI) , Journal Index (JI, Under Process) , Directory of abstract indexing for Journals (DAIJ) , Open Access Journals (Under Process) , Impact Factor Services For International Journals (IFSIJ) , Cosmos Impact Factor , Jour Informatics (Under Process) , Eurasian Scientific Journal Index (ESJI) , International Innovative Journal Impact Factor (IIJIF) , Science Library Index, Dubai, United Arab Emirates , Pubmed Database [NLM ID: 101669306] (Under Process) , IP Indexing (IP Value 2.40) , Web of Science Group (Under Process) , Directory of Research Journals Indexing , Scholar Article Journal Index (SAJI) , International Scientific Indexing ( ISI ) , Scope Database , Academia , 

 ISSN 2394-3211

Impact Factor: 7.065

 ICV - 79.57

Abstract

DESIGNING A POTENT INHIBITOR FOR HUMAN EIF2AK3 (PERK) - A THERAPEUTIC TARGET FOR PROGRESSIVE SUPRANUCLEAR PALSY

Prashant Kumar* and Satyavani Guttula

ABSTRACT

For a typical drug action, proteins are considered as the major targets as they are the functional molecules in living systems. Conventional laboratory techniques takes minimum ten years in designing a single drug. This time-span is drastically reduced via the use of computational/in-silico tools. Rational designing of a drug starts with finding out the proteins having the potential to be considered as drug targets in disease pathogenesis. Proteomics plays a big role in identification of the same and thus aid in multi-step drug-development process. The process basically comprises of identification and validation of target, selection of lead, molecular screening and optimization, and toxicity testing. This paper aims at designing a computer-assisted, structure based drug of an effective inhibitor of human EIF2AK3 (PERK) gene, a target protein for Progressive Supranuclear Palsy (PSP), a degenerative neurological disorder of uncertain aetiology, caused mainly by mutation of tau gene. Discovery of potent and selective inhibitors which has the potential to inhibit PERK activity in cells and display growth inhibition of human tumour has helped in identifying selective lead compounds as drug candidates. The drug selected via virtual screening and ADME analysis though having a low drug score of 0.27 had no toxicity risks and was good enough for inhibition of the protein expression, so can be used for drug development for further application. The study also provides hints for the future design of new derivatives with higher potency and specificity.

Keywords: Proteomics, Virtual screening, Docking, Drug designing, Drug target.


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Google Scholar Indian Science Publications InfoBase Index (In Process) SOCOLAR, China Research Bible, Fuchu, Tokyo. JAPAN International Society for Research activity (ISRA) Scientific Indexing Services (SIS) Polish Scholarly Bibliography Global Impact Factor (GIF) (Under Process) Universal Impact Factor International Scientific Indexing (ISI), UAE Index Copernicus CAS (A Division of American Chemical Society) USA (Under Process) Directory of Open Access Journal (DOAJ, Sweden, in process) UDLedge Science Citation Index CiteFactor Directory Of Research Journal Indexing (DRJI) Indian citation Index (ICI) Journal Index (JI, Under Process) Directory of abstract indexing for Journals (DAIJ) Open Access Journals (Under Process) Impact Factor Services For International Journals (IFSIJ) Cosmos Impact Factor Jour Informatics (Under Process) Eurasian Scientific Journal Index (ESJI) International Innovative Journal Impact Factor (IIJIF) Science Library Index, Dubai, United Arab Emirates Pubmed Database [NLM ID: 101669306] (Under Process) IP Indexing (IP Value 2.40) Web of Science Group (Under Process) Directory of Research Journals Indexing Scholar Article Journal Index (SAJI) International Scientific Indexing ( ISI ) Scope Database Academia