Clathrin inhibitors - @ a glance

Clathrin-mediated endocytosis or receptor-mediated endocytosis is a predominant form of endocytosis. Clathrin mediated endocytosis regulates many physiological processes including internalisation of growth factors and receptors, entry of pathogens and synaptic transmission.

Clathrin is the most abundant of a number of proteins which are found in coated pits. These coated pits are essential in endocytosis and bud and pinch off from the membrane in a dynamin-dependent manner to form clathrin-coated vesicles, allowing endocytosis to occur.

Within a clathrin coated pit, clathrin acts as a central hub for coated pit assembly and dissociation via its terminal domain. The clathrin inhibitors Pitstop 1™ and Pitstop 2™ are novel tools which selectively inhibit ligand association with clathrin's terminal domain and selectively inhibit amphiphysin association of the clathrin terminal domain.

By selectively inhibiting clathrin-mediated endocytosis, Pitstop 1 and 2™ allow the further exploration of clathrin function whilst also providing potential applications as virus and pathogen entry inhibitors and cell signalling modulators.

Interactive clathrin diagram

Roll your mouse over our novel clathrin inhibitors Pitstop 1™ and Pitstop 2™ to see what they do. Click them to find out more!

• Pitstop 1™
  (Requires microinjecting) Clathrin Inhibition: IC₅₀ ~18 μM^[1]
• Pitstop 2™
  (Cell permeable) Clathrin Inhibition: IC₅₀ ~12 μM^[1]

References

1. von Kleist et al (2011) Role of the clathrin terminal domain in regulating coated pit dynamics revealed by small molecule inhibition. Abstract
2. Roy and Wrana (2005) Clathrin- and non-clathrin-mediated endocytic regulation of cell signalling. Nat Rev Mol Cell Biol. 6:112-26. Abstract
3. Mousavi et al (2004) Clathrin-dependent endocytosis. Biochem J. 1:1-16. Abstract

Recommended reviews from our technical team

1. Granseth et al (2007) Clathrin mediated endocytosis: the physiological mechanism of vesicle retrieval at hippocampal synapses. Abstract
2. Doherty and McMahon (2009) Mechanisms of endocytosis. Annu Rev Biochem. 78:857-902. Abstract

Technical resources

Endocytosis - @ a glance

Dynamin inhibitors - @ a glance