Current development of sigma-2 receptor radioligands as potential tumor imaging agents

Bioorg Chem. 2021 Jul 13;115:105163. doi: 10.1016/j.bioorg.2021.105163. Online ahead of print.ABSTRACTSigma receptors are transmembrane proteins with two different subtypes: σ1 and σ2. Because of its overexpression in tumors, the σ2 receptor (σ2R) is a well-known biomarker for cancer cells. A large number of small-molecule ligands for the σ2Rs have been identified and tested for imaging the proliferative status of tumors using single photon emission computed tomography (SPECT) and positron emission tomography (PET). These small molecules include derivatives of bicyclic amines, indoles, cyclohexylpiperazines and tetrahydroisoquinolines. This review discusses various aspects of small molecule ligands, such as chemical composition, labeling strategy, affinity for σ2Rs, and in vitro/in vivo investigations. The recent studies described here could be useful for the development of σ2R radioligands as potential tumor imaging agents.PMID:34289426 | DOI:10.1016/j.bioorg.2021.105163
Source: Bioorganic Chemistry - Category: Chemistry Authors: Source Type: research