Drug intelligence / Profile preview

[44AANA47]-RANTES

Development stage
Preclinical
Modality
Recombinant Proteins and Enzymes, Peptides
Administration
Intraperitoneal, Intravenous (preclinical/experimental Models)[9]
01

Overview

[44AANA47]-RANTES is a site-directed mutant of the chemokine CCL5 (also known as RANTES: regulated upon activation, normal T cell expressed and secreted), with alanine substitutions at amino acid positions 44-47 that disrupt the main glycosaminoglycan (GAG) binding site of native RANTES[1][7][9]. This mutation impairs chemokine oligomerization and binding to GAGs, reducing inflammatory cell recruitment in vivo and altering the resulting immune response. [44AANA47]-RANTES acts as a **RANTES (CCL5) antagonist** by competitively inhibiting leukocyte recruitment via the native RANTES/CCL5 pathways[1][7][9]. Its anti-inflammatory effects have been demonstrated in animal models, where it reduces atherosclerotic plaque formation, decreases proinflammatory cytokines, and promotes more stable vascular plaques[1][9]. The protein is used as a tool in preclinical research to explore the role of RANTES/GAG interactions in inflammation and immune cell migration[1][7][9].

02

Targets

HSPG (Basement membrane-specific heparan sulfate proteoglycan core protein (perlecan))CCR5 (C-C chemokine receptor type 5)CCR1CCR3 (C-C chemokine receptor type 3)

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