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Literature summary for 7.6.2.2 extracted from

  • Loo, T.W.; Bartlett, M.C.; Clarke, D.M.
    Human P-glycoprotein is active when the two halves are clamped together in the closed conformation (2010), Biochem. Biophys. Res. Commun., 395, 436-440.
    View publication on PubMed
Search for more literature for 7.6.2.2

Activating Compound

Activating Compound Comment Organism Structure
Colchicine 450 microM, 50% stimulation Homo sapiens
rhodamine B 44 microM, 50% stimulation Homo sapiens
verapamil 12 microM, 50% stimulation Homo sapiens
vinblastine 2.2 microM, 50% stimulation Homo sapiens

Protein Variants

Protein Variants Comment Organism
L175C/N820C introduction of cysteine residues into regions of TM3, residues 175-178, and TM9, residues 820–822. Treatment with 1,1-methanediyl bismethanethiosulfonate results in cross-linking of the majority of protein. Cross-linking is not increased in the presence of ATP or drug substrates. Cross-linking increases the mutant's basal ATPase activity about 3fold. Activity can be increased further by drug substrates such as verapamil and rhodamine B Homo sapiens
additional information introduction of cysteine residues into regions of TM3, residues 175-178, and TM9, residues 820–822, that extend into the cytoplasm and are 4 A and 20 A apart in the closed and open conformations, respectively. Cross-linking of the double mutants with a short cross-linker, 1,1-methanediyl bismethanethiosulfonate at 0°C results only in cross-linking of mutant L175C/N820C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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General Information

General Information Comment Organism
physiological function P-gp in the membrane is in the closed conformation that has a high affinity for drug substrates Homo sapiens