[HTML][HTML] Molecular Determinants of High Affinity Phenylalkylamine Block of L-type Calcium Channels (∗)
GH Hockerman, BD Johnson, T Scheuer… - Journal of Biological …, 1995 - ASBMB
The high affinity phenylalkylamine (-) D888 blocks ion currents through L-type Ca 2+
channels containing the α 1C subunit with an apparent K d of 50 nM, but N-type Ca 2+
channels in the pheochromocytoma cell line PC12 are blocked with a 100-fold higher K d
value of 5 μM. L-type Ca 2+ channels containing α 1C subunits with the site-directed
mutations Y1463A, A1467S, or I1470A in the putative transmembrane segment S6 in
domain IV (IVS6) were 6-12 times less sensitive to block by (-) D888 than control α 1C. Ca …
channels containing the α 1C subunit with an apparent K d of 50 nM, but N-type Ca 2+
channels in the pheochromocytoma cell line PC12 are blocked with a 100-fold higher K d
value of 5 μM. L-type Ca 2+ channels containing α 1C subunits with the site-directed
mutations Y1463A, A1467S, or I1470A in the putative transmembrane segment S6 in
domain IV (IVS6) were 6-12 times less sensitive to block by (-) D888 than control α 1C. Ca …