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Targeted Cancer Therapies

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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
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An Orally Available Halothiazole Glycomimetic as a Cancer-Targeting Dual Galectin-1 and Galectin-3 Inhibitor.

Fredrik R Zetterberg¹, Kristoffer Peterson¹, Ulf J Nilsson^1,2

¹Galecto Biotech AB, Sahlgrenska Science Park, Medicinaregatan 8 A, Gothenburg SE-413 46, Sweden.

Journal of Medicinal Chemistry

|April 29, 2026

Summary

Targeting galectins (galectin-1 and galectin-3) offers a novel cancer therapy approach. A new dual inhibitor, GB1841, effectively reduced lung cancer cell growth in preclinical studies.

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Published on: July 12, 2018

Area of Science:

Oncology
Biochemistry
Medicinal Chemistry

Background:

The 10 hallmarks of cancer necessitate broader therapeutic strategies beyond current treatments.
Galectins, specifically galectin-1 and galectin-3, are implicated in all cancer hallmarks.
Targeting both galectin-1 and galectin-3 simultaneously presents a promising therapeutic avenue.

Purpose of the Study:

To develop novel dual inhibitors of galectin-1 and galectin-3.
To optimize compounds for high affinity and favorable in vitro ADME properties.
To evaluate the efficacy of dual galectin inhibition in a preclinical cancer model.

Main Methods:

Design and synthesis of 3-(halothiazolyl)triazolyl derivatives.
Structure-activity relationship (SAR) studies and in vitro ADME profiling.
In vivo evaluation of compound GB1841 in a syngeneic LL/2 lung cancer mouse model.

Main Results:

Discovery and optimization of a new class of dual galectin-1/3 inhibitors.
Compound GB1841 demonstrated high affinity for both galectin-1 (Kd 0.027 μM) and galectin-3 (Kd 0.14 μM).
Both selective and dual inhibition significantly reduced LL/2 lung cancer cell growth in vivo.

Conclusions:

Dual inhibition of galectin-1 and galectin-3 is a viable strategy for cancer treatment.
GB1841 is a promising dual galectin inhibitor candidate for further preclinical development.
Targeting galectins offers a potential approach to address multiple cancer hallmarks.