Next Article in Journal
Characterization of miR-206 Promoter and Its Association with Birthweight in Chicken
Next Article in Special Issue
Intra-Articular Injection of Cross-Linked Hyaluronic Acid-Dexamethasone Hydrogel Attenuates Osteoarthritis: An Experimental Study in a Rat Model of Osteoarthritis
Previous Article in Journal
Induction of ROS Overload by Alantolactone Prompts Oxidative DNA Damage and Apoptosis in Colorectal Cancer Cells
Previous Article in Special Issue
GL-1196 Suppresses the Proliferation and Invasion of Gastric Cancer Cells via Targeting PAK4 and Inhibiting PAK4-Mediated Signaling Pathways
Article Menu
Issue 4 (April) cover image

Export Article

Open AccessReview
Int. J. Mol. Sci. 2016, 17(4), 561; doi:10.3390/ijms17040561

Linkers Having a Crucial Role in Antibody–Drug Conjugates

1,2,†
,
1,2,3,†
,
1,2,* and 1,2,*
1
Institute for Advancing Translational Medicine in Bone & Joint Diseases, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong, China
2
Institute of Integrated Bioinfomedicine & Translational Science, Hong Kong Baptist University Shenzhen Research Institute and Continuing Education, Shenzhen 518000, China
3
Institute of Precision Medicine and Innovative Drug Discovery, HKBU (Haimen) Institute of Science and Technology, Haimen 226100, China
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Wenbin Deng
Received: 21 February 2016 / Revised: 29 March 2016 / Accepted: 8 April 2016 / Published: 14 April 2016
(This article belongs to the Special Issue Translational Molecular Medicine & Molecular Drug Discovery)
View Full-Text   |   Download PDF [3579 KB, uploaded 14 April 2016]   |  

Abstract

Antibody–drug conjugates (ADCs) comprised of a desirable monoclonal antibody, an active cytotoxic drug and an appropriate linker are considered to be an innovative therapeutic approach for targeted treatment of various types of tumors and cancers, enhancing the therapeutic parameter of the cytotoxic drug and reducing the possibility of systemic cytotoxicity. An appropriate linker between the antibody and the cytotoxic drug provides a specific bridge, and thus helps the antibody to selectively deliver the cytotoxic drug to tumor cells and accurately releases the cytotoxic drug at tumor sites. In addition to conjugation, the linkers maintain ADCs’ stability during the preparation and storage stages of the ADCs and during the systemic circulation period. The design of linkers for ADCs is a challenge in terms of extracellular stability and intracellular release, and intracellular circumstances, such as the acid environment, the reducing environment and cathepsin, are considered as the catalysts to activate the triggers for initiating the cleavage of ADCs. This review discusses the linkers used in the clinical and marketing stages for ADCs and details the fracture modes of the linkers for the further development of ADCs. View Full-Text
Keywords: antibody–drug conjugates; cytotoxic drug; monoclonal antibody; linker; attachment site; tumor antibody–drug conjugates; cytotoxic drug; monoclonal antibody; linker; attachment site; tumor
Figures

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Lu, J.; Jiang, F.; Lu, A.; Zhang, G. Linkers Having a Crucial Role in Antibody–Drug Conjugates. Int. J. Mol. Sci. 2016, 17, 561.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Int. J. Mol. Sci. EISSN 1422-0067 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top