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Highly Preorganized Calixarene Tweezers for Protein Recognition.

Katrin Hommel¹, Sebastian Theisen², Mike Blueggel¹

¹Molecular Biology II, Center of Medical Biotechnology (ZMB) and Center for Nanointegration Duisburg-Essen (CENIDE), University of Duisburg-Essen, Universitätsstrasse 5, 45141 Essen, Germany.

Biomacromolecules

|July 23, 2025

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Researchers designed calixarene-based inhibitors to target Taspase 1, a cancer-related protease. Rigid, preorganized calixarene tweezers effectively disrupted the Taspase 1/Importin α-interaction, showing promise for enzyme inhibition.

Area of Science:

Supramolecular Chemistry
Medicinal Chemistry
Enzyme Inhibition

Background:

Calixarene scaffolds provide structural stability and tunable geometry for designing selective supramolecular inhibitors.
Taspase 1 is a cancer-related protease involved in cellular processes.

Purpose of the Study:

To develop and synthesize a focused library of preorganized multivalent calix[4]arene tweezers targeting Taspase 1.
To investigate the impact of linker rigidity, functionalization, and multivalency on Taspase 1 inhibition.

Main Methods:

Synthesis of seven cone-conformation calix[4]arene derivatives.
Meta-dynamics simulations to assess linker flexibility and preorganization.
Biochemical binding assays to evaluate enzyme inhibition and binding affinity.

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Main Results:

Rigid linkers, particularly benzyl linkers, promoted structural preorganization of calixarene tweezers.
Bivalent and upper-rim derivatives (c2Tl, uc2T, uc4T) most effectively disrupted the Taspase 1/Importin α-interaction.
Inhibition potency was enhanced by increased multivalency and linker rigidity, with low micromolar K_D values observed for c2Tl and uc4T.

Conclusions:

Rigid, preorganized calix[4]arene ligands are effective scaffolds for targeted Taspase 1 inhibition.
The design of calixarene tweezers can be optimized by controlling linker rigidity and multivalency for enhanced enzyme inhibition.
These findings establish a promising strategy for developing novel enzyme inhibitors for cancer therapy.