Disitertide (P144) is a TGF-β1 antagonist peptide; induces apoptosis in GBM cell lines and reduces SMAD2 phosphorylation with downregulation of SKI and upregulation of SMAD7 at both transcriptional and translational levels; active in vivo.
CAT No: 10-101-282
CAS No:272105-42-7
Synonyms/Alias:Disitertide;272105-42-7;Disitertide [INN];UNII-3N988KP8HD;3N988KP8HD;P144;Disitertide TFA;P144 TFA;GLXC-26360;AKOS032945122;DA-52587;Thr-Ser-Leu-Asp-Ala-Ser-Ile-Ile-Trp-Ala-Met-Met-Gln-Asn-OH;
Disitertide is a synthetic peptide compound recognized for its ability to modulate protein-protein interactions, particularly those involving transforming growth factor-beta (TGF-β) signaling pathways. Structurally derived from a sequence within the TGF-β type III receptor, Disitertide is designed to selectively interfere with TGF-β-mediated cellular responses. Its unique biochemical properties have made it a valuable research tool for investigating fibrotic processes, cellular signaling mechanisms, and the regulation of extracellular matrix components. By specifically targeting molecular interactions central to tissue remodeling and fibrosis, Disitertide has become increasingly relevant in studies focused on understanding the molecular basis of fibrogenesis and related pathophysiological conditions.
Peptide-based signaling research: Disitertide is widely utilized in studies examining the intricate mechanisms of TGF-β signaling, a pathway central to numerous cellular processes including proliferation, differentiation, and extracellular matrix production. By introducing this peptide into cell culture or in vitro biochemical assays, researchers can selectively inhibit or modulate TGF-β receptor interactions, enabling precise dissection of downstream signaling cascades. This targeted approach aids in identifying key regulatory nodes and understanding how aberrant signaling contributes to fibrotic disease progression or tissue remodeling.
Fibrosis and extracellular matrix studies: The compound's ability to disrupt TGF-β-mediated signaling has positioned it as an important tool for probing the molecular underpinnings of fibrosis. In experimental models, Disitertide is employed to investigate the synthesis and deposition of extracellular matrix proteins, such as collagen and fibronectin, which are hallmarks of fibrotic tissue. By modulating these pathways, scientists can elucidate the cellular events that drive excessive matrix accumulation and identify potential molecular targets for anti-fibrotic intervention.
Peptide structure-function analysis: Disitertide serves as a model system for exploring the relationship between peptide sequence, structure, and biological activity. Through mutagenesis, analog synthesis, and biophysical characterization, researchers can assess how specific amino acid residues within the peptide influence its binding affinity, selectivity, and inhibitory potency. These studies not only advance fundamental understanding of peptide-receptor interactions but also inform the rational design of next-generation peptide modulators with improved specificity and efficacy.
In vitro screening and assay development: The compound is frequently incorporated into high-throughput screening platforms and cell-based assays aimed at evaluating the efficacy of novel antifibrotic agents or small molecule inhibitors. By serving as a benchmark or control, Disitertide enables comparative analysis of compound activity, facilitating the identification of candidates with superior inhibitory profiles. Its predictable and well-characterized mode of action enhances assay reproducibility and supports the development of robust experimental workflows.
Mechanistic studies of tissue remodeling: Beyond fibrosis, Disitertide is employed in broader investigations of tissue repair, wound healing, and organ regeneration, where TGF-β signaling plays a pivotal role. By modulating the activity of this pathway, the peptide allows researchers to dissect the dynamic interplay between cellular populations, growth factors, and matrix components during tissue remodeling events. These mechanistic insights contribute to a deeper understanding of both physiological and pathological tissue responses, supporting the advancement of regenerative biology and biomaterials research.
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