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Updated: Jun 27, 2025

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
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Inhibition of SRC-3 as a potential therapeutic strategy for aggressive mantle cell lymphoma

Imani Bijou1, Yang Liu2, Dong Lu1

  • 1Department of Biochemistry and Molecular Pharmacology, Baylor College of Medicine, Houston, Texas, United States of America.

Plos One
|April 29, 2024
PubMed

Insights

Novel SRC-3 inhibitors, SI-10 and SI-12, show promise against mantle cell lymphoma (MCL). SI-10 demonstrated effectiveness in preclinical models, offering a potential new strategy for treating this aggressive B cell lymphoma.

Area of Science:

  • Oncology
  • Hematology
  • Molecular Biology

Background:

  • Mantle cell lymphoma (MCL) presents a poor prognosis and frequent relapse, driving the need for innovative therapies.
  • SRC-3 is implicated in B cell lymphoma progression, with high expression observed in patient lymph nodes.
  • SRC-3 inhibition has shown efficacy in other B cell lymphomas.

Purpose of the Study:

  • To investigate the efficacy of novel SRC-3 inhibitors, SI-10 and SI-12, in mantle cell lymphoma.
  • To evaluate the anti-lymphoma activity of SI-10 in preclinical models of MCL.

Main Methods:

  • In vitro cytotoxicity assays of SI-10 and SI-12 against MCL cell lines.
  • In vivo efficacy studies of SI-10 in immunocompetent disseminated A20 mouse model and a human PDX model of MCL.
  • Assessment of SI-10's impact on survival and toxicity in ibrutinib-resistant models.

Main Results:

  • SI-10 and SI-12 exhibited dose-dependent cytotoxicity against a panel of MCL cell lines in vitro.
  • SI-10 demonstrated in vivo efficacy in two distinct ibrutinib-resistant models of B-cell lymphoma and MCL.
  • SI-10 treatment significantly extended survival with low toxicity in these preclinical models.

Conclusions:

  • SI-10 functions as a novel anti-lymphoma compound by inhibiting SRC-3 activity.
  • Targeting SRC-3 warrants further investigation as a combination strategy to enhance therapeutic outcomes in lymphoma.
  • These findings suggest a potential new therapeutic avenue for mantle cell lymphoma, particularly in resistant cases.

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