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Biological effects and activity optimization of small-molecule, drug-like synthetic anion transporters.
Eur J Med Chem 2019; 184:111782EJ

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.

Authors+Show Affiliations

School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, PR China.School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, PR China.School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, PR China; Department of Pharmacy, Maoming Academy of Health, Maoming, 525000, PR China.School of Biotechnology and Health Sciences, International Healthcare Innovation Institute (Jiangmen), Wuyi University, Jiangmen, 529020, PR China. Electronic address: whchen@wyu.edu.cn.

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

31634785

Citation

Yu, Xi-Hui, et al. "Biological Effects and Activity Optimization of Small-molecule, Drug-like Synthetic Anion Transporters." European Journal of Medicinal Chemistry, vol. 184, 2019, p. 111782.
Yu XH, Hong XQ, Mao QC, et al. Biological effects and activity optimization of small-molecule, drug-like synthetic anion transporters. Eur J Med Chem. 2019;184:111782.
Yu, X. H., Hong, X. Q., Mao, Q. C., & Chen, W. H. (2019). Biological effects and activity optimization of small-molecule, drug-like synthetic anion transporters. European Journal of Medicinal Chemistry, 184, p. 111782. doi:10.1016/j.ejmech.2019.111782.
Yu XH, et al. Biological Effects and Activity Optimization of Small-molecule, Drug-like Synthetic Anion Transporters. Eur J Med Chem. 2019 Oct 14;184:111782. PubMed PMID: 31634785.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Biological effects and activity optimization of small-molecule, drug-like synthetic anion transporters. AU - Yu,Xi-Hui, AU - Hong,Xiao-Qiao, AU - Mao,Qin-Chao, AU - Chen,Wen-Hua, Y1 - 2019/10/14/ PY - 2019/05/30/received PY - 2019/10/08/revised PY - 2019/10/09/accepted PY - 2019/10/22/pubmed PY - 2019/10/22/medline PY - 2019/10/22/entrez KW - Activity optimization KW - Anion homeostasis KW - Anion transporter KW - Bioactivity KW - Mechanism of biological action SP - 111782 EP - 111782 JF - European journal of medicinal chemistry JO - Eur J Med Chem VL - 184 N2 - 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. SN - 1768-3254 UR - https://www.unboundmedicine.com/medline/citation/31634785/Biological_effects_and_activity_optimization_of_small-molecule,_drug-like_synthetic_anion_transporters L2 - https://linkinghub.elsevier.com/retrieve/pii/S0223-5234(19)30934-1 DB - PRIME DP - Unbound Medicine ER -