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 name||Inhibition of Amphiphysin association of clathrin terminal domain (IC50 in μM)||Reference||Publications 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|
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) »