The binding process of BmKTX and BmKTX-D33H toward to Kv1.3 channel: a
molecular dynamics simulation study
Abstract
The potassium channel Kv1.3 is an important pharmacological target and
the Kaliotoxin-type toxins (α-KTX-3 family) are its specific blockers.
Here, we study the binding process of two kinds of Kaliotoxin-type
toxins:BmKTX and its mutant (BmKTX-D33H) toward to Kv1.3 channel using
MD simulation and umbrella sampling simulation, respectively. The
calculated binding free energies are -27 kcal/mol and -34 kcal/mol for
BmKTX and BmKTX-D33H, respectively, which are consistent with
experimental results. The further analysis indicate that the
characteristic of electrostatic potential of the α-KTX-3 have important
effect on their binding modes with Kv1.3 channel; the residue 33 in
BmKTX and BmKTX-D33H plays a key role in determine their binding
orientations toward to Kv1.3 channel; when residue 33( or 34) has
negative electrostatic potential, the anti-parallel β-sheet domain of
α-KTX-3 toxin peptide will keep away from the filter region of Kv1.3
channel, as BmKTX; when residue 33(or 34) has positive electrostatic
potential, the anti-parallel β-sheet domain of α-KTX-3 toxin peptide
will interact with the filter region of Kv1.3 channel, as BmKTX-D33H.
Above all, electrostatic potential differences on toxin surfaces and
correlations motions within the toxins will determine the
toxin-potassium channel interaction model. In addition, the hydrogen
bond interaction is the pivotal factor for the Kv1.3- Kaliotoxin
association. Understanding the binding mechanism of toxin–potassium
channel will facilitate the rational development of new toxin analogue.