This document describes a targeted venom discovery array (T-VDA) for modulating kinase activity. It summarizes that: 1) The T-VDA contains venoms from the Chinese cobra (Naja atra) and hundred pace pit viper (Deinagkistrodon acutus) which contain peptides that bind to and modulate protein kinases and phosphatidylinositol 3-kinase, important drug targets. 2) Testing of these and other venoms like Naja melanoleuca on cancer cells has revealed effects on kinases involved in growth signaling like IGF-1R, Axl, and VEGF receptors. 3) Fractionated venom libraries are provided

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Evolved peptides
hit difficult targets
Target: Kinases
Format: Targeted Discovery Array
Code: T-VDAKinase
product description modulation of kinase activity…
Kinases are prime drug targets for a wide range
of disease areas including neurology,
ophthalmology and oncology. The venoms for T-
VDAKinase include Naja atra (Chinese cobra), which
contains unique three finger neurotoxins that
bind Protein Kinase C1; and Deinagkistrodon
acutus (hundred pace pit viper) venom, which
contains snaclec agglucetin, a lectin that signals
through phosphatidylinositol 3-kinase (PI3K)2.
With our collaborators at Canterbury Christ
Church University we have investigated the
effects of other venoms such as (Naja
melanoleuca) on many kinases in cancer cells.
More venoms from the T-VDAkinase are being
tested currently and a full hit-to-lead program is
underway. This data is currently being written up
for publication, but a summary is presented here.
Venoms are useful in many modes of kinase
signaling. This crude whole venom is composed of
several hundred components and thus 1D and 2D
fractionated libraries are provided for quicker
identification of specific hits. Naja melanoleuca
venom increased IGF-1R, Axl, VEGF-R2 and
VEGF-R3 phosphorylation and decreased RYK and
EphB7 phosphorylation, in A431 cells. Venoms act
directly on kinases as well as modulating
downstream affects of other modulators such as
growth factors. Venom dose in top row of spots.
IGF-1R Axl VEGF-R3 VEGF R2 RYK Eph-B7
+
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ready-to-use libraries normal safety rules apply
• Echo qualified 384 well plates
• 1D – 12 species per plate 10+ peptides per well.
• 2D – fewer peptides (1-5) per well for faster follow up
and less complexity for cell based assays.
• Follow-up Services – full support for hit ID. SAR and
bulk resupply for pharmacology
All products come with full international safety data sheets
(SDS). Evolved peptide libraries are as easy to use as small
molecule libraries and are fully soluble in aqueous buffers
for both biochemical and cell based assays. Also quantities
are optimised so there is no surplus wastes, the T-VDA’s
can be disposed in appropriate biohazardous waste streams
like you cells.
references
1. Chiou SH1, Raynor RL, Zheng B, Chambers TC, Kuo JF. (1993).
Cobra venom cardiotoxin (cytotoxin) isoforms and neurotoxin:
comparative potency of protein kinase C inhibition and cancer cell
cytotoxicity and modes of enzyme inhibition. Biochemistry.
2;32(8):2062-7.
2. Wang WJ. (2008). Agglucetin, a tetrameric C-type lectin-like venom
protein, regulates endothelial cell survival and promotes
angiogenesis by activating integrin alphavbeta3 signaling. Biochem.
Biophys. Res. Commun. 2;369(2):753-60.
contact: mayflower bioscience tel: 314-485-5210 web: www.mayflowerbio.com