[^99mTc]Tc-PentixaTec: development, extensive pre-clinical evaluation, and first human experience.

ABSTRACT:

Purpose

The clinical success non-invasive imaging of CXCR4 expression using [⁶⁸ Ga]Ga-PentixaFor-PET warrants an expansion of the targeting concept towards conventional scintigraphy/SPECT with their lower cost and general availability. To this aim, we developed and comparatively evaluated a series of ^99mTc-labeled cyclic pentapeptides based on the PentixaFor scaffold.

Methods

Six mas₃-conjugated CPCR4 analogs with different 4-aminobenzoic acid (Abz)-D-Ala-D-Arg-aa₃ linkers (L1-L6) as well as the corresponding HYNIC- and N₄-analogs of L6-CPCR4 were synthesized via standard SPPS. Competitive binding studies (IC₅₀ and IC₅₀inv) were carried out using Jurkat T cell lymphoma cells and [¹²⁵I]FC-

SUBMITTER: Konrad M 

PROVIDER: S-EPMC10611619 | biostudies-literature | 2023 Nov

REPOSITORIES: biostudies-literature