Generic placeholder image

Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Nanobodies and their Use in GPCR Drug Discovery

Author(s): Karen D. Cromie, Gino Van Heeke and Carlo Boutton

Volume 15, Issue 24, 2015

Page: [2543 - 2557] Pages: 15

DOI: 10.2174/1568026615666150701113549

Price: $65


Nanobodies are therapeutic proteins derived from the variable domain (VHH) of naturally occurring heavy-chain antibodies. These VHH domains are the smallest functional fragments derived from a naturally occurring immunoglobulin. Nanobodies can be easily produced in prokaryotic or eukaryotic host organisms and their unique biophysical characteristics render these molecules ideal candidates for drug development. They are also emerging as an interesting new class of potential therapeutics for targets such as GPCRs, which have historically been challenging for small molecule drug discovery and even more difficult for biologics discovery. The ability to easily combine Nanobodies with different binding sites and different modes of action can be used to generate highly selective and highly potent drug candidates with very attractive pharmacological profiles. In addition, Nanobodies have been used as crystallization chaperones to enable or facilitate the structural determination of an active GPCR conformation.

Keywords: β2AR, CXCR2, CXCR4, CXCR7, Crystallization chaperone, GPCR, Nanobodies, VHH.

Graphical Abstract

Rights & Permissions Print Export Cite as
© 2023 Bentham Science Publishers | Privacy Policy