Recent Advances In Developing Novel Anti-Cancer Drugs Targeting Tumor Hypoxic and Acidic Microenvironments.

Show simple item record Li, Weidong en Sun, Xueying en 2020-05-08T00:44:26Z en 2018-01 en
dc.identifier.issn 1574-8928 en
dc.identifier.uri en
dc.description.abstract BACKGROUND:Solid tumors often contain hypoxic microenvironments due to abnormal vasculatures and outweighing demands of oxygen. Cancer cells rely on anaerobic respiration, leading to sequential acidic microenvironments. Hypoxic and acidic microenvironments cause genetic instability and activate signaling pathways, contributing to cancer progression and therapy resistance, and have become targets for developing novel anti-cancer agents. OBJECTIVE:This article reviews recent advances in the development of novel anti-cancer drugs targeting hypoxic and acidic microenvironments. METHODS:Recent patents and published literature related to anti-cancer agents targeting tumor hypoxic and acidic microenvironments were searched and reviewed. Key termed used in the searching included cancer, anti-cancer drug, neoplasm, clinical trials, tumor microenvironment, hypoxic microenvironment, acidic microenvironment, hypoxia-inducible factors, hypoxia; metabolism; Warburg effect and aerobic glycolysis. RESULTS:A number of Hypoxia-Inducible Factor (HIF) inhibitors have been developed or discovered, but most of them have only exhibited indirect effects on HIFs, and a limited number of drugs are able to directly interfere with mRNA and protein of HIFs, the dimerization of α and β subunits, or the interaction between HIFs and its activators. The development of agents targeting acidic microenvironments focuses on V-ATPase, monocarboxylic acid transporters, Na+/H+ exchangers and carbonic anhydrases. Proton pump inhibitors as V-ATPase inhibitors have been applied in treating various tumors as an adjuvant therapy, but none of the other inhibitors has been approved for cancer treatment. CONCLUSION:Developing more specific agents, and seeking sensitive, applicable and accurate biomarkers may improve the efficacy of drugs targeting hypoxic and acidic microenvironments. en
dc.format.medium Print en
dc.language eng en
dc.relation.ispartofseries Recent patents on anti-cancer drug discovery en
dc.rights Items in ResearchSpace are protected by copyright, with all rights reserved, unless otherwise indicated. Previously published items are made available in accordance with the copyright policy of the publisher. en
dc.rights.uri en
dc.subject Animals en
dc.subject Humans en
dc.subject Neoplasms en
dc.subject Antineoplastic Agents en
dc.subject Drug Delivery Systems en
dc.subject Cell Hypoxia en
dc.subject Acid-Base Equilibrium en
dc.subject Hydrogen-Ion Concentration en
dc.subject Tumor Microenvironment en
dc.subject Drug Development en
dc.title Recent Advances In Developing Novel Anti-Cancer Drugs Targeting Tumor Hypoxic and Acidic Microenvironments. en
dc.type Journal Article en
dc.identifier.doi 10.2174/1574892813666180831102519 en
pubs.issue 4 en
pubs.begin-page 455 en
pubs.volume 13 en
dc.rights.holder Copyright: The author en
pubs.end-page 468 en
pubs.publication-status Published en
dc.rights.accessrights en
pubs.subtype Review en
pubs.subtype Journal Article en
pubs.elements-id 755359 en
dc.identifier.eissn 2212-3970 en
pubs.record-created-at-source-date 2018-09-04 en
pubs.dimensions-id 30173649 en

Files in this item

There are no files associated with this item.

Find Full text

This item appears in the following Collection(s)

Show simple item record


Search ResearchSpace