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Clathrin-mediated endocytosis (CME) or receptor-mediated endocytosis regulates many physiological processes including internalization of growth factors and receptors, synaptic transmission and entry of pathogens. This specific process of material uptake into a cell is achieved by using clathrin-coated vesicles (CCV). CME is a complex, highly orchestrated process requiring the interaction of at least 30 proteins with roles at different stages of the process. There are five stages of CCV cycle, each requiring the synchronization of a wide range of protein – protein interactions to ensure successful cargo internalization:
(i) initiation by FCHo and AP-2 proteins, which recruit clathrin for coat assembly
(ii) cargo selection
(iii) clathrin coat assembly
(v) clathrin uncoating.
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® are novel tools which selectively inhibit ligand association with clathrin's terminal domain.
By selectively inhibiting clathrin-mediated endocytosis, Pitstop® allows the further exploration of clathrin function whilst also providing potential applications as virus and pathogen entry inhibitors and cell signaling modulators.
Pitstop® compounds comparison table
|Product Name||IC50 (µM)*||Cell-permeable||Notes#|
|Pitstop® 2||12||Yes||Cited in Cell, J Neurosci, J Biol Chem|
|Pitstop® 1||18||No||Active in cells after microinjection. Cited in Cell|
|Pitstop® 2-100||7.5||Yes||Cited in J Biol Chem|
|Pitstop® 1-25||6.9||Low||Cited in J Med Chem|
|Pitstop® 2 - Negative Control||-||Yes|
|Pitstop® 1 - Negative Control||-||No|
|Pitstop® 2-100 - Negative Control||-||Yes|
* Inhibition of clathrin terminal domain-amphiphysin complex
# For the latest list of publications available please refer to the product's datasheet
Mousavi SA et al. Clathrin-dependent endocytosis. Biochem J 1:1-16 (2004). Read more (PubMed: 14505490)