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Fragment-Based Phenotypic Lead Discovery To Identify New Drug Seeds That Target Infectious Diseases
- Source :
- ACS Chemical Biology, ACS Chemical Biology, 2021, 16 (11), pp.2158-2163. ⟨10.1021/acschembio.1c00657⟩
- Publication Year :
- 2021
-
Abstract
- International audience; Fragment-based lead discovery has emerged over the last decades as one of the most powerful techniques for identifying starting chemical matter to target specific proteins or nucleic acids in vitro. However, the use of such low-molecular-weight fragment molecules in cell-based phenotypic assays has been historically avoided because of concerns that bioassays would be insufficiently sensitive to detect the limited potency expected for such small molecules and that the high concentrations required would likely implicate undesirable artifacts. Herein, we applied phenotype cell-based screens using a curated fragment library to identify inhibitors against a range of pathogens including Leishmania, Plasmodium falciparum, Neisseria, Mycobacterium, and flaviviruses. This proof-of-concept shows that fragment-based phenotypic lead discovery (FPLD) can serve as a promising complementary approach for tackling infectious diseases and other drug-discovery programs.
- Subjects :
- biology
[SDV]Life Sciences [q-bio]
MESH: Anti-Infective Agents
Drug Evaluation, Preclinical
Plasmodium falciparum
General Medicine
Computational biology
biology.organism_classification
Leishmania
Biochemistry
Small molecule
Phenotype
Structure-Activity Relationship
MESH: Structure-Activity Relationship
MESH: Drug Discovery
Anti-Infective Agents
Drug Discovery
Nucleic acid
Molecular Medicine
Bioassay
MESH: Drug Evaluation, Preclinical
Neisseria
Mycobacterium
Subjects
Details
- ISSN :
- 15548937 and 15548929
- Volume :
- 16
- Issue :
- 11
- Database :
- OpenAIRE
- Journal :
- ACS chemical biology
- Accession number :
- edsair.doi.dedup.....520f95ea52cd1b9e6547f5e3c06e7b81