Characterization and Activity Profiling of Candidate Drugs Against PFD0975W from Plasmodium Falciparum

Simple item page
dc.contributor.authorChakraborty, Arnish
dc.date.accessioned2016-02-29T04:25:42Z
dc.date.accessioned2023-10-19T11:05:13Z
dc.date.available2016-02-29T04:25:42Z
dc.date.available2023-10-19T11:05:13Z
dc.date.issued2016
dc.descriptionSupervisors: Vishal Trivedi and Vibin Ramakrishnanen_US
dc.description.abstractMalaria is a life-threatening disease caused by the protozoan parasite Plasmodium falciparum. Emergence of drug resistance necessitates the identification of new drug targets. PFD0975w is identified as an RIO-2 kinase in the malaria parasite, believed to play crucial roles in cell cycle coordination and ribosome maturation. Homology modeling enabled the structural characterization of the kinase and virtual screening identified several potential hits. The putative kinase was cloned, expressed and purified as a 35 KDa active enzyme capable of binding ATP. Plasmodium RIO-2 kinase localizes in the parasite cytosol with discrete localization during each RBC stage and a maximum expression is observed in trophozoites. The localization pattern of the enzyme is sensitive to cellular stresses. Several candidate drugs were identified and a series of synthetic molecules were designed to target this kinase. Most of the above molecules exhibit excellent antimalarial activity. The molecules are parasitocidal and disrupt the parasite’s antioxidant machinery. Stress induced upon drug treatment influences the localization of the kinase within the iRBC. Studies suggest Plasmodium RIO-2 kinase as an essential gene capable of being an excellent antimalarial drug target. The work has also identified several promising antimalarial molecules for further drug development.en_US
dc.identifier.otherROLL NO. 11610601
dc.identifier.urihttps://gyan.iitg.ac.in/handle/123456789/656
dc.language.isoenen_US
dc.relation.ispartofseriesTH-1445;
dc.subjectBIOSCIENCES AND BIOENGINEERINGen_US
dc.titleCharacterization and Activity Profiling of Candidate Drugs Against PFD0975W from Plasmodium Falciparumen_US
dc.typeThesisen_US
Files
Original bundle
Now showing 1 - 2 of 2
No Thumbnail Available
Name:
Abstract-TH-1445_11610601.pdf
Size:
430.88 KB
Format:
Adobe Portable Document Format
Description:
Abstract
Download
No Thumbnail Available
Name:
TH-1445_11610601.pdf
Size:
15.42 MB
Format:
Adobe Portable Document Format
Description:
Thesis
Download
License bundle
Now showing 1 - 1 of 1
No Thumbnail Available
Name:
license.txt
Size:
1.71 KB
Format:
Plain Text
Description:
Download
Collections
PhD Theses (Biosciences and Bioengineering)