Clathrin inhibitors - @ a glance

 

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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.

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

 

Clathrin inhibitors summary 

 

Product nameInhibition of Amphiphysin association of clathrin terminal domain (IC50 in μM)ReferencePublications featuring our products
Pitstop 1™ 18 von Kleist et al 2011  
Pitstop 1™ Negative Control N/A    
Pitstop 2™ 12 von Kleist et al 2011 View now
Pitstop 2™ Negative Control N/A   View now

 

References

von Kleist L et al. Role of the clathrin terminal domain in regulating coated pit dynamics revealed by small molecule inhibition. Cell 146:471-84 (2011). Read more (PubMed: 21816279) »
Le Roy C and Wrana JL. Clathrin- and non-clathrin-mediated endocytic regulation of cell signalling. Nat Rev Mol Cell Biol 6:112-26 (2005). Read more (PubMed: 15687999) »
Mousavi SA et al. Clathrin-dependent endocytosis. Biochem J 1:1-16 (2004). Read more (PubMed: 14505490) »

 

Recommended reviews from our technical team

Granseth B et al. Clathrin mediated endocytosis: the physiological mechanism of vesicle retrieval at hippocampal synapses. J Physiol 15:681-6 (2007). Read more (PubMed: 17599959) » 
Doherty GJ and McMahon. Mechanisms of endocytosis. Annu Rev Biochem 78:857-902 (2009). Read more (PubMed: 19317650) »

 

Technical resources

Endocytosis - @ a glance

Dynamin inhibitors - @ a glance

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