DAPTA, an analog of peptide T, acts as a chemokine receptor 5 (CCR5) antagonist that inhibits the entry of the virus. It is used potentially for the treatment of HIV infection and HBV infection.
CAT No: R1013
CAS No:106362-34-9
Synonyms/Alias:DAPTA;106362-34-9;Adaptavir;(D-Ala1)-peptide T amide;D-Ala-peptide T-amide;RAP101;L-Threoninamide, D-alanyl-L-seryl-L-threonyl-L-threonyl-L-threonyl-L-asparaginyl-L-tyrosyl-;CHEMBL181276;J208V4ZMP2;(2S)-N-[(2S)-1-[[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]-2-[[(2S,3R)-2-[[(2S,3R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2R)-2-aminopropanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxybutanoyl]amino]butanediamide;D-Ala-Ser-Thr-Thr-Thr-Asn-Tyr-Thr-NH2;(S)-2-((2S,5S,8S,11S,14R)-14-Amino-2,5,8-tris((R)-1-hydroxyethyl)-11-(hydroxymethyl)-4,7,10,13-tetraoxo-3,6,9,12-tetraazapentadecanamido)-N1-((S)-1-(((2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl)amino)-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)succinamide;mDAPTA;monomeric D-Ala-peptide;D-Ala1-peptide T-amide;UNII-J208V4ZMP2;(D-Alanine1)Peptide T amide;Monomeric DAPTA;MFCD00076838;D-Ala1-peptide T-NH2;H-D-ALA-SER-THR-THR-THR-ASN-TYR-THR-NH2;[D-Ala1] Peptide T Amide;SCHEMBL7706935;monomeric d-Ala-peptide T-amide;GTPL11692;HY-P1034;PEPTIDE T AMIDE, 1(D-ALA);BDBM50607887;s8501;AKOS024457091;CCG-270535;CS-7601;NCGC00599627-01;AC-31499;AS-58148;DA-59547;FA109659;D-Ala-Ser-Thr-Thr-Thr-Asn-Tyr-Thr-NH(2);A11871;BRD-K37151368-001-01-7;Q27281035;
DAPTA, also known as D-Ala1-peptide T-amide, is a synthetic peptide derivative designed with a modified N-terminal D-alanine residue and an amidated C-terminus. As a member of the peptide T family, DAPTA is recognized for its unique sequence motifs that enable selective binding interactions with specific cellular receptors, particularly those involved in immune modulation and chemokine signaling. Its biochemical properties and structural features have made it a valuable investigational tool in peptide-based research, especially in studies exploring receptor-ligand dynamics, cell signaling pathways, and peptide structure-activity relationships. DAPTA's defined sequence and stability confer distinct advantages for probing molecular mechanisms in vitro and in various biochemical assays.
Receptor Binding Studies: DAPTA's primary application lies in its use as a research probe for receptor binding investigations. Its affinity for certain chemokine receptors, such as CCR5, makes it instrumental in elucidating the molecular basis of ligand-receptor interactions. Researchers employ this peptide to map receptor binding domains, characterize competitive binding kinetics, and assess the impact of specific amino acid modifications on receptor affinity. These studies contribute to a deeper understanding of chemokine receptor biology and the broader principles of peptide-mediated cellular communication.
Peptide Structure-Activity Relationship Analysis: The defined sequence and functional modifications of DAPTA render it highly suitable for structure-activity relationship (SAR) studies. By systematically analyzing how alterations in its amino acid composition affect biological activity, scientists can identify critical determinants of peptide function. Such SAR analyses are integral to the rational design of novel peptide analogs with tailored properties, supporting advancements in peptide engineering and the development of specialized research tools.
Cellular Signaling Pathway Elucidation: DAPTA is frequently utilized to dissect cellular signaling cascades initiated by chemokine engagement. Its selective receptor interactions provide a controlled means to trigger or inhibit downstream signaling pathways in cultured cells or cell-free systems. These experimental approaches help clarify the roles of specific receptors in modulating immune cell migration, activation, and communication, thereby advancing the field of immunological signaling research.
Peptide-Based Assay Development: The stability and specificity of DAPTA make it a preferred standard or control in peptide-based assay systems. In vitro assays leveraging this peptide enable quantitative measurement of receptor activity, competitive binding, or cellular responses to peptide stimuli. Its consistent performance supports assay validation, optimization, and reproducibility, which are essential for generating reliable experimental data in academic and industrial research environments.
Analytical Method Validation: In addition to its use in functional studies, DAPTA serves as a reference compound for the calibration and validation of analytical methods such as high-performance liquid chromatography (HPLC) and mass spectrometry. Its well-characterized properties allow for precise monitoring of peptide purity, stability, and degradation profiles, facilitating the development of robust analytical protocols for peptide quantification and quality assessment. This application is particularly valuable in laboratories focused on peptide synthesis, formulation, and analytical chemistry.
A pre-HAART era placebo-controlled trial showed that DAPTA caused cognitive improvements, and a later analysis of stored samples suggests a clinically significant reduction in plasma viral load (K. Goodkin, University of Miami, personal communication). A more recent uncontrolled clinical trial reports that DAPTA substantially suppressed virus in persistently infected cellular reservoirs in both HAART experienced and naïve to treatment patients.
Chemokine receptor-5 (CCR5) is a receptor for the HIV entry inhibitor peptide T (DAPTA)
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