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Development and Characterization of a High-Affinity Selective Galectin-3 Mouse Tool Compound in Mouse Models of
Kristoffer Peterson1, Ulf J Nilsson1,2, Lise Gravelle3
1Galecto Biotech AB, Sahlgrenska Science Park, Medicinaregatan 8 A, SE-413 46 Gothenburg, Sweden.
A new galectin-3 inhibitor, GB2095, was developed to improve preclinical cancer studies. This compound effectively reduced breast and melanoma tumor growth in mouse models, aiding translation to human clinical trials.
Area of Science:
- Oncology
- Pharmacology
Background:
- Galectin-3 is a growing drug target for cancer and fibrosis.
- Existing inhibitors like GB1211 show reduced efficacy in mouse models due to species-specific structural differences.
Purpose of the Study:
- To develop an improved mouse galectin-3 inhibitor for better preclinical translation.
- To evaluate the efficacy of the new compound, GB2095, in syngeneic mouse cancer models.
Main Methods:
- Development of GB2095, a tool compound with enhanced affinity for mouse galectin-3.
- In vivo testing of GB2095 in syngeneic mouse models of breast and melanoma cancer.
Main Results:
- GB2095 demonstrates improved binding affinity for mouse galectin-3 compared to GB1211.
- GB2095 administration significantly reduced tumor growth in both breast and melanoma models.
Conclusions:
- GB2095 is a valuable tool compound for preclinical cancer research, facilitating better translation of galectin-3 inhibitor studies to clinical settings.
- The development of GB2095 addresses limitations of previous inhibitors in mouse models, supporting future clinical development for galectin-3 targeted therapies.
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