Scientific capability / Ligand-Induced pKa Design and Cation Placement

Design the local environment around the reacting residue.

A ligand can influence the chemistry around the site it recognizes. BioTwin investigates whether placing a charged group near that site could change cysteine ionization and useful reaction behavior, subject to geometry, exposure and kinetic trade-offs.

Current work Computational design studies

Move from predicting pKa to choosing a placement

PROPKA already estimates pKa values in proteins and protein–ligand complexes. BioTwin’s design operation asks where a candidate cation could be placed, then evaluates electrostatic effects, clashes and solvent exposure. The resulting geometry can become a constraint for a linker or recognition element.

More thiolate does not guarantee the desired rate

Changing acidity also changes nucleophilic behavior. The model includes Brønsted compensation so a predicted pKa shift is interpreted through its effect on reaction kinetics. Combined with recognition, tether geometry and exposure, this gives a specific molecular hypothesis to compare with simply increasing intrinsic warhead reactivity.

The matched compound is the meaningful test

The design lever has been used in computational Lp(a) work. Actual local pKa shifts and the benefit of a synthesized compound remain unmeasured. A matched pair with and without the charged feature should distinguish changes in binding, local reactivity and off-target capture. Desolvation and molecular realization can overturn a favorable electrostatic estimate.

Further reading

Turn the electrostatic idea into a matched comparison.

A charged feature and its control can separate a local-reactivity benefit from changed binding or nonspecific capture.