Microtiter plate-based antibody-competition assay to determine binding affinities and plasma/blood stability of CXCR4 ligands.

ABSTRACT: C-X-C chemokine receptor type 4 (CXCR4) is involved in several intractable disease processes, including HIV infection, cancer cell metastasis, leukemia cell progression, rheumatoid arthritis, asthma and pulmonary fibrosis. Thus, CXCR4 represents a promising drug target and several CXCR4 antagonizing agents are in preclinical or clinical development. Important parameters in drug lead evaluation are determination of binding affinities to the receptor and assessment of their stability and activity in plasma or blood of animals and humans. Here, we designed a microtiter plate-based CXCR4 antibody competition assay that enables to measure inhibitory concentrations (IC₅₀ values) and affinity constants (K_i values) of CXCR4 targeting drugs. The assay is based on the observati

SUBMITTER: Harms M 

PROVIDER: S-EPMC7525492 | biostudies-literature | 2020 Sep

REPOSITORIES: biostudies-literature