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. 2013 Dec 17;170(8):1607–1651. doi: 10.1111/bph.12447
Nomenclature HGNC, UniProt Activators (EC50) Channel Blockers (IC50) Functional characteristics Comment
CFTR CFTR, P13569 apigenin (Potentiation), capsaicin (Potentiation), CBIQ (Potentiation), felodipine (Potentiation), genistein (Potentiation), nimodipine (Potentiation), NS004 (Potentiation), phenylglycine-01 (Potentiation), SF-01 (Potentiation), UCCF-029 (Potentiation), UCCF-339 (Potentiation), UCCF-853 (Potentiation), VX-770 (Potentiation) intracellular CFTRinh-172 (intracellular application prolongs mean closed time), GaTx1, glibenclamide, extracellular GlyH-101 γ = 6–10 pS; permeability sequence = Br- ≥ Cl- > I- > F-, (PI/PCl = 0.1–0.85); slight outward rectification; phosphorylation necessary for activation by ATP binding at binding nucleotide binding domains (NBD)1 and 2; positively regulated by PKC and PKGII (tissue specific); regulated by several interacting proteins including syntaxin 1A, Munc18 and PDZ domain proteins such as NHERF (EBP50) and CAP70 UCCF-339, UCCF-029, apigenin and genistein are examples of flavones. UCCF-853 and NS004 are examples of benzimidazolones. CBIQ is an example of a benzoquinoline. felodipine and nimodipine are examples of 1,4-dihydropyridines. phenylglycine-01 is an example of a phenylglycine. SF-01 is an example of a sulfonamide. Malonic acid hydrazide conjugates are also CFTR channel blockers (see Verkman and Galietta, 135 155)