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Details on Person Binding of ABCB1 (also known as MDR1, P-glycoprotein, or PGP...

Class:IdSummation:9659965
_displayNameBinding of ABCB1 (also known as MDR1, P-glycoprotein, or PGP...
_timestamp2019-09-23 02:23:56
created[InstanceEdit:9659971] Orlic-Milacic, Marija, 2019-09-06
literatureReference[LiteratureReference:9659671] Investigational ABC transporter inhibitors
modified[InstanceEdit:9661012] Orlic-Milacic, Marija, 2019-09-12
[InstanceEdit:9661013] Orlic-Milacic, Marija, 2019-09-12
[InstanceEdit:9661022] Orlic-Milacic, Marija, 2019-09-12
[InstanceEdit:9662357] Orlic-Milacic, Marija, 2019-09-23
textBinding of ABCB1 (also known as MDR1, P-glycoprotein, or PGP) to inhibitory drugs inhibits ABCB1-mediated export of xenobiotics from the cytosol to the extracellular space. The first generation of ABCB1 inhibitors were drugs used to treat disease other than cancer that were repurposed to be used as adjuvants for multi-drug resistant cancers. The second and third generation ABCB1 inhibitors were developed to specifically target ABCB1 and to reduce toxicity (reviewed by Falasca and Linton 2012). Inhibition of ABCB1, however, has not improved the treatment regiments and outcomes for the vast majority of cancers.

The first generation of ABCB1 inhibitors includes:
verapamil (Yusa and Tsuruo 1989);
quinine ();
cyclosporin A (Tamai and Safa 1990, Charuk et al. 1994).

The second generation of ABCB1 inhibitors includes:
valspodar ();
biricodar ().

The third generation ABCB1 inhibitors include:
tariquidad ();
elacridar ()
zosuquidar ():
tetrandrine ();
laniquidar ().
(summation)[Reaction:9659967] ABCB1 binds ABCB1 inhibitors [Homo sapiens]
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