GENETIC TARGET VALIDATION FOR ATP-CITRATE LYASE INHIBITION
Sign Up to like & getrecommendations! Published in 2017 at "Journal of the American College of Cardiology"
DOI: 10.1016/s0735-1097(17)35044-1
Abstract: Background: Bempedoic acid is a novel oral agent that reduces hepatic cholesterol synthesis by inhibiting ATP-citrate lyase (ACL) leading to upregulation of the LDL receptor and a reduction in plasma low-density lipoprotein cholesterol (LDL-C). Although… read more here.
Keywords: citrate lyase; atp citrate; target validation; genetic target ... See more keywords
METTL3 from Target Validation to the First Small-Molecule Inhibitors: A Medicinal Chemistry Journey
Sign Up to like & getrecommendations! Published in 2023 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.2c01601
Abstract: RNA methylation is a critical mechanism for regulating the transcription and translation of specific sequences or for eliminating unnecessary sequences during RNA maturation. METTL3, an RNA methyltransferase that catalyzes the transfer of a methyl group… read more here.
Keywords: medicinal chemistry; mettl3 target; chemistry; validation first ... See more keywords
Facile target validation in an animal model with intracellularly expressed monobodies
Sign Up to like & getrecommendations! Published in 2018 at "Nature chemical biology"
DOI: 10.1038/s41589-018-0099-z
Abstract: Rapidly determining the biological effect of perturbing a site within a potential drug target could guide drug discovery efforts, but it remains challenging. Here, we describe a facile target validation approach that exploits monobodies, small… read more here.
Keywords: monobody; validation; target; facile target ... See more keywords
New directions in antimalarial target validation
Sign Up to like & getrecommendations! Published in 2020 at "Expert Opinion on Drug Discovery"
DOI: 10.1080/17460441.2020.1691996
Abstract: ABSTRACT Introduction: Malaria is one of the most prevalent human infections worldwide with over 40% of the world’s population living in malaria-endemic areas. In the absence of an effective vaccine, emergence of drug-resistant strains requires… read more here.
Keywords: directions antimalarial; validation; new directions; drug ... See more keywords
Mendelian Randomization in Stroke: A Powerful Approach to Causal Inference and Drug Target Validation
Sign Up to like & getrecommendations! Published in 2021 at "Frontiers in Genetics"
DOI: 10.3389/fgene.2021.683082
Abstract: Stroke is a leading cause of death and disability worldwide. However, our understanding of its underlying biology and the number of available treatment options remain limited. Mendelian randomization (MR) offers a powerful approach to identify… read more here.
Keywords: powerful approach; mendelian randomization; drug; target validation ... See more keywords
The Importance of Being Presented: Target Validation by Immunopeptidomics for Epitope-Specific Immunotherapies
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Immunology"
DOI: 10.3389/fimmu.2022.883989
Abstract: Presentation of tumor-specific or tumor-associated peptides by HLA class I molecules to CD8+ T cells is the foundation of epitope-centric cancer immunotherapies. While often in silico HLA binding predictions or in vitro immunogenicity assays are… read more here.
Keywords: target validation; importance; importance presented; presented target ... See more keywords
A Combined Human in Silico and CRISPR/Cas9-Mediated in Vivo Zebrafish Based Approach to Provide Phenotypic Data for Supporting Early Target Validation
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2022.827686
Abstract: The clinical heterogeneity of heart failure has challenged our understanding of the underlying genetic mechanisms of this disease. In this respect, large-scale patient DNA sequencing studies have become an invaluable strategy for identifying potential genetic… read more here.
Keywords: crispr cas9; zebrafish; cas9 mediated; target validation ... See more keywords