About: Deamidated Human Triosephosphate Isomerase is a Promising Druggable Target

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An Entity of Type : schema:ScholarlyArticle, within Data Space : wasabi.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Deamidated Human Triosephosphate Isomerase is a Promising Druggable Target
Creator	Cabrera, Nallely De La Mora-De La Mora, Ignacio Enríquez-Flores, Sergio Flores-López, García-Torres, Itzhel Gutiérrez-Castrellón, Pedro Luis, Antonio López-Velázquez, Gabriel Martínez-Pérez, Yoalli
Source	Medline; PMC
abstract	Therapeutic strategies for the treatment of any severe disease are based on the discovery and validation of druggable targets. The human genome encodes only 600–1500 targets for small-molecule drugs, but posttranslational modifications lead to a considerably larger druggable proteome. The spontaneous conversion of asparagine (Asn) residues to aspartic acid or isoaspartic acid is a frequent modification in proteins as part of the process called deamidation. Triosephosphate isomerase (TIM) is a glycolytic enzyme whose deamidation has been thoroughly studied, but the prospects of exploiting this phenomenon for drug design remain poorly understood. The purpose of this study is to demonstrate the properties of deamidated human TIM (HsTIM) as a selective molecular target. Using in silico prediction, in vitro analyses, and a bacterial model lacking the tim gene, this study analyzed the structural and functional differences between deamidated and nondeamidated HsTIM, which account for the efficacy of this protein as a druggable target. The highly increased permeability and loss of noncovalent interactions of deamidated TIM were found to play a central role in the process of selective enzyme inactivation and methylglyoxal production. This study elucidates the properties of deamidated HsTIM regarding its selective inhibition by thiol-reactive drugs and how these drugs can contribute to the development of cell-specific therapeutic strategies for a variety of diseases, such as COVID-19 and cancer.
has issue date	2020-07-15(xsd:dateTime)
bibo:doi	10.3390/biom10071050
bibo:pmid	32679775
has license	cc-by
sha1sum (hex)	e0cd141b2e94c7571ec2d87134998e6b5a81c496
schema:url	https://doi.org/10.3390/biom10071050
resource representing a document's title	Deamidated Human Triosephosphate Isomerase is a Promising Druggable Target
has PubMed Central identifier	PMC7407242
has PubMed identifier	32679775
schema:publication	Biomolecules
resource representing a document's body	covid:e0cd141b2e94c7571ec2d87134998e6b5a81c496#body_text
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