TE~S 22 - MAY 1997
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LETTERS
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Kinetic data remiabitity
In a recent Talking Point article ~, Schuck
and Minton propose two simple
consistency tests to ascertain the
reliability of kinetic measurements
performed with surface plasmon
resonance (SPR) biosensors. We agree
totally with their suggestions and the
necessity to perform these tests. However,
we believe that the inclusion of some of our
published experiments ~as examples of
data that fail these tests is inappropriate.
The interaction we studied was
characterised by substantial re-binding of
dissociating material to the surface. This
is a common problem in binding studies,
especially for interactions with fast
as.sociation rates, and can be overcome
either by 'infinite' dilution (which is not
practical) or by the addition of an excess
of competing ligand during the
dissociation phase to prevent re, .nding :~
(see Fig. 2a in Ref. 2). Schuck and Minton
wrongly compare the k,,,~ values obtained
in this way (and shown in our Table !)
with the k,,~,~ calculated from Fig. ld. The
k,,,~ should be and is consistent with the
'apparent' low kd~,,value obtained in
buffer flow (Fig. 2a), not with the high
k,~,, value obtained in the presence of the
competing peptide.
Concerning consistency test 1, Schuck
and Minton somehow calculate a value of
approximately 1.3 nM for the equilibrium
constant K~ from our data shown in
Fig. la. These are six points with the first
and last differing by tenfold. We are sure
that Schuck and Minton would agree that,
in order to obtain an accurate value, a
range of concentrations differing by at
least several hundred-fold has to be used,
including points close to saturation 3. It is
also obvious from the same figure that
true equilibrium was not reached during
the time course of these experiments,
again making these data unsuitable for a
Eo calculation. Moreover, Schuck and
Minton compare the value of 1.3 nM with
the K n obtained using the 'true' off rate
from Table 1, not the 'apparent' one, as
discussed above. We have recently
repeated these experiments with
recombinant proteins that are not fused
to GST. This diminishes the re-binding
problem and equilibrium is reached much
faster than with the GST-fusion proteins.
Using this approach, both the association
and dissociation phases can be fitted
accurately with simple kinetic models,
confirming our published finding of fast
association and very fast dissociation
rates for SH2 domain-phosphopeptide
interactions. The calculated K~ values
also match those defined by equilibrium
binding assays. We conclude that our
published data are not 'self-inconsistent'
.....I ,~.., pro.~ded experimental conditions E,UaU LI IQL,
and materials are chosen carefully, SPR
biosensors using continuous flow (Bib.core)
can be reliably used for calculation of
kinetic and equilibrium constants.
References
1 Schuck, P. and Minton, A. P. (1996) Trends
Biochem. Sci. 21, 458-460
2 Panayotou, G. et al. (1993) Mol. Cell. Biol. 13,
3567-3576
3 LJmbJrd,L E. (1986) Jn Cell Surface Receptors:
a short course on theory and methods,
Martinus Nijhoff Publishing
GEORGE PANMGTGLIAND
MIKE WATERRELD
Ludwig Institute for Cancer Research,
91 Riding House Street, London, UK WlP 8BT.
Copyr|ght © 1997, El:~evler 5dence Ltd. All rights reserved. 0968-0004/97/$17.00
Reply to Paaayotou
and Wateffie[d
Panayotou et al. ~ have evaluated the
dissociation rate constant k via analysis
of a dissociation experiment conducted i '
the presence of a large excess of
competing peptide. We agree that this
value of k is much more likely to reflect
the true chemical rate constant for
dissociation of peptide from SH2 domain
than the value obtained from analysis of
the association experiment in the context
of the elementary 1:1 association model.
However, the use of a value of k obtained
from the same analysis of the same
association experiment with the same
oversimplified model only compounds
the internal inconsistency of the
calculation of the association equilibrium
constants K,, (mistakenly labeled
dissociation constants) in Table i o~
Panayotou et al.~. We have shown
Published by ElsevierScience Ltd. 0968-0004/97
(.
PII: S0968-0004(97)t) 1037-2
elsewhere 2 that mass transport effects
can result in quasi-linear plots of
dR/dr vs R, analysis of which via the
elementary association model (neglecting
mass transport) yields apparent rate
constants k and k~ s' that both are far
below the actual intrinsic chemical rate
constants for binding. If one calculates an
apparept equilibrium association
constant by dividing an artifactually low
estimate of k by a realistic estimate of k_,
then the resulting estimate of K a will be
depressed by the same factor as k.
The internal inconsistency inherent in
the analysts employed by Panayot'Ju and
colleagues ~is evident in the limiting
long-time behavior of the association
experiments plotted in Fig. la, c. One may
estimate the equilibrium response R= of
the system from Fig. la, d, as described in
our note (Table I caption) or, equivalently,
by extrapolating the straight lines plotted
in Fig. lc to the x-intercept (dR/dr = 0).
The resulting dependence of R= on free
ligand concentration can be modeled via
PII: S0968-0004(97)01038-4
our Eqn 4 to obtain a reasonable estimate
of K~ (or K,). We emphasize that this
calculation is not subject to the influence
of mass transport. When done, one
obtains a value of K. approximately equal
to 1 riM-= (Ref. 1) for the particular set of
data plotted in Fig. 1. It is quP" impossible
to describe the long-time limit of these
data using the value of 0.0237 nM-
(Ref. 1) for the association equilibrium
constant as reported by the authors.
References
I Panayotou, G. et al. (1993) Mol. Cell. Biol. 13,
3567-.3576
2 Schuck, P. and Minton, A. P. (1996) Anal.
B~octlem. 240, 262-272
P~ER $CHUCKAND
ALLEN P. M|NTON
Laboratory of Biochemical Pharmacology,
National Institute of Diabetes,
Digestive and Kidney Diseases,
National Institutes of Health, Bethesda,
MD 20892, USA.
149