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Table 1 Question

Posted by SRegner on 27 Feb 2010 at 21:24 GMT

Hello,

I was reading through the article and was wondering if you could clarify one quick thing for me. Figure 1 shows the HDAC 1 IC(50) of compound 106 to be 13 nM yet it is the highest relative Ki to any of the other compounds is it possible this 13 nM is meant to be 13 uM? If not, do you believe this may, with such a low IC(50) for HDAC 1, cause upregulation of the repsective genes to HDAC 1 binding due to the higher dosing that would be needed to ellicit a response with respect to HDAC 3.


Thanks in advance for any clarification

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RE: Table 1 Question

massimop replied to SRegner on 03 Mar 2010 at 07:22 GMT

We thank SRegner for having spotted a typo in Table1. These data were generated in Dr. Gottesfeld's lab. Going back to the data for 106 generated by James Chou, who was a postdoc in the lab, here is what is found:
IC50 HDAC1 IC50 HDAC3 Ki HDAC1 Ki HDAC3

106 380 nM 140 nM 148 ± 36 nM 14 ± 3 nM

106 is a slow-on inhibitor, so the IC50 is a misleading value (see Chou et al., JBC, 2008). From the Ki values, clearly this compound has a preference for HDAC3, which we also see in activity profiling experiments (Xu et al., Chem. Biol. 2009).
We apologize for this error that escaped our checks.
In behalf of all authors:

Massimo Pandolfo
ULB, Brussels, Belgium

Competing interests declared: This is reply by the authors of this paper.
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