DTP3

DTP3 is a first‑in‑class, cancer‑selective D‑tripeptide inhibitor of the GADD45β/MKK7 complex, rationally identified from a combinatorial library as Ac‑D‑Tyr‑D‑Arg‑D‑Phe‑NH2 and further developed as a drug candidate targeting the NF‑κB–dependent survival pathway in hematologic malignancies.[1][4] By binding to MKK7 and disrupting its interaction with the NF‑κB–inducible anti‑apoptotic factor GADD45β, DTP3 relieves GADD45β‑mediated suppression of MKK7 and induces MKK7/JNK‑dependent apoptosis selectively in multiple myeloma and diffuse large B‑cell lymphoma cells, with minimal activity in normal cells or GADD45β‑low tumors.[1][4][6] Preclinical studies have shown potent, highly selective antitumor activity and favorable pharmacokinetics, and DTP3 has progressed into first‑in‑human phase I/IIa trials in patients with relapsed or refractory multiple myeloma and diffuse large B‑cell lymphoma.[1][5][6][9]