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Biological effects and activity optimization of small-molecule, drug-like synthetic anion transporters
- Source :
- European journal of medicinal chemistry. 184
- Publication Year :
- 2019
-
Abstract
- The balance of normal anion concentrations in cells provides basis for maintaining cellular morphology and function. Disrupting the homeostasis of cellular anions and lysosomal pH, in particular with high selectivity for cancer cells over normal cells may serve as a promising approach for the treatment of cancers. Small-molecule organic compounds with transmembrane anion transport activity, namely synthetic anion transporters are able to destroy the homeostasis of cellular anions, in particular chloride anions to trigger cell death and thus may be developed as a new class of anti-tumor drugs. This paper reviews the latest advance in the investigation into the in vitro anion transport, promising anti-tumor activity and probable mechanism of biological action of synthetic anion transporters. The strategies for optimizing the biological activity of synthetic anion transporters and improving the selectivity for cancer cells over normal cells are also discussed.
- Subjects :
- Pharmacology
Chemistry
Organic Chemistry
Organic Anion Transporters
Biological activity
Transporter
Antineoplastic Agents
Apoptosis
Biological Transport
General Medicine
Chloride
Small molecule
Transmembrane protein
Anion homeostasis
Small Molecule Libraries
Neoplasms
Drug Discovery
Cancer cell
medicine
Biophysics
Homeostasis
Humans
Function (biology)
medicine.drug
Cell Proliferation
Subjects
Details
- ISSN :
- 17683254
- Volume :
- 184
- Database :
- OpenAIRE
- Journal :
- European journal of medicinal chemistry
- Accession number :
- edsair.doi.dedup.....ce0ef8aa66af527b0b398bc017dc835e