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. 2009 Aug 17;10(12):1955-8.
doi: 10.1002/cbic.200900079.

Surface binding inhibitors of the SCF-KIT protein-protein interaction

David Margulies  1 , Yarden Opatowsky, Steven Fletcher, Ishu Saraogi, Lun K Tsou, Sourav Saha, Irit Lax, Joseph Schlessinger, Andrew D Hamilton
Affiliations

Surface binding inhibitors of the SCF-KIT protein-protein interaction

David Margulies et al. Chembiochem. .
No abstract available

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Figures

Figure 1
Figure 1
A) Electrostatic potential map of KIT (left) and SCF monomer (right) at the interface. The negatively charged surface is shown in red and the positive in blue. B) Electrostatic surface potential (left) of a porphyrin-based synthetic receptor (P2; right) possessing two distinct hydrophobic (highlighted by the circle) and charged domains. P2 is presented on the same scale as SCF and KIT in Figure 1A.
Figure 2
Figure 2
Three synthetic scaffolds were used to generate 18 potential inhibitors; their functional groups are shown in Table 1. Arrow heads and tails correspond to charged functional groups and hydrophobic domains, respectively. An additional compound, P9, is a simple meso-tetrakis (4-carboxyphenyl)porphine (TCPP) to which four aspartic acids are appended.
Figure 3
Figure 3
A) Saturation-binding curve of HRP-labeled SCF (SCF*) binding to ELISA plates coated with the whole extracellular ligand-binding domain of KIT (KD(app) = 16 nm). B) Competition-binding curves for the lead inhibitors (In.) P2 (formula image) and P3 (●); KI(app) = 31 and 33 nm, respectively. C) Cell-based assays testing the efficiency of the lead compounds (IC50 < 10 µm) to inhibit SCF-induced KIT phosphorylation. Four compounds (P1–3, C10) strongly inhibited cell stimulation; P2 completely abolished KIT phosphorylation (p-KIT).
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