Abstract
ABCB1 is the best-characterized member of the ABC superfamily of transmembrane proteins. ABCB1 transports structurally diverse substrates, including anticancer drugs. This, in combination with protein overexpression in cancer cells, hampers interactions with the drugs intracellular targets and jeopardizes chemotherapy treatments. The ATP-driven transport mechanism allows ABCB1 to alternate between an inward-facing (IF) conformation, where the protein adopts an inverted conical shape, and an outward-facing (OF) conformation, with a cylinder-like shape.
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