Drug intelligence / Profile preview

SRI31277

Development stage
Preclinical
Lead developer
Southern Research
Modality
Small Molecules, Peptides
Administration
Intravenous
01

Overview

SRI31277 is a **synthetic tripeptide inhibitor** (sequence: serine-lysine-leucine) developed to block thrombospondin-1 (TSP-1)-mediated activation of latent transforming growth factor-beta (TGF-β). By selectively blocking the interaction between TSP-1 and latent TGF-β, SRI31277 inhibits activation of TGF-β signaling pathways. This mechanism targets a source of TGF-β activation implicated in drug resistance in cancers such as multiple myeloma and thyroid carcinoma, as well as fibrosis. SRI31277 has been found to be effective in preclinical models for both cancer drug resistance (e.g., overcoming bortezomib resistance in multiple myeloma) and fibrosis, though it has a short plasma half-life and is generally administered via infusion in animal studies. It was originated as a lead compound from research aiming to develop TSP-1/TGF-β antagonists, with analogs under further development for improved stability and bioavailability[1][3][5][7].

Other names
SRI-31277SRI31277SRI 31277
02

Targets

TSR1 (Thrombospondin-1 type-1 repeat domain)CCL21 (Chemokine (C-C motif) ligand 21)

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