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. 2019 Oct 29;11(11):626. doi: 10.3390/toxins11110626

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© 2019 by the authors.

Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).

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“Spider-plot” of Site 4 and Site 3 targeting spider knottins. (A) The pIC₅₀ of Site 4 spider knottins normalized against Na_V1.7 are shown. These data are from assays performed on human Na_V subtypes, except JzTx-14 which was performed at mammalian Na_V subtypes. Data for GpTx-1 [122], ProTx-III [80], Cd1a [110], and CcoTx-2 [110] were obtained from Fluorescence Imaging Plate Reader (FLIPR) experiments, while the remainder were acquired using electrophysiology. Black dots indicate that the IC₅₀ values for the corresponding knottins were less potent than the value indicated. (B) The pEC₅₀ of Site 3 targeting spider knottins are shown. JzTx-I [100] was tested on rat Na_V1.2–1.4 and human Na_V1.5 and Na_V1.7. JzTx-II [98] was tested on rat Na_V1.3 and human Na_V1.5. PnTx2-1 [147] was tested on rat Na_V1.1 and Na_V1.8, and human Na_V1.5. Hm1a [20] was tested on human Na_V subtypes.