Sunitinib (Sutent, SU11248), a Small-Molecule Receptor Tyrosine Kinase Inhibitor, Blocks Function of the ATP-Binding Cassette (ABC) Transporters P-Glycoprotein (ABCB1) and ABCG2

The Hallmarks of Cancer

2000 • 27,569 citations

New Colorimetric Cytotoxicity Assay for Anticancer-Drug Screening

1990 • 9,412 citations

Safety, Pharmacokinetic, and Antitumor Activity of SU11248, a Novel Oral Multitarget Tyrosine Kinase Inhibitor, in Patients With Cancer

2005 • 1,140 citations

Sunitinib: From Rational Design to Clinical Efficacy

2007 • 844 citations

Selection and characterization of BCR-ABL positive cell lines with differential sensitivity to the tyrosine kinase inhibitor STI571: diverse mechanisms of resistance

2000 • 789 citations

Human Multidrug Resistance ABCB and ABCG Transporters: Participation in a Chemoimmunity Defense System

2006 • 702 citations

The Role of ABC Transporters in Drug Resistance, Metabolism and Toxicity

2004 • 527 citations

Approval Summary: Sunitinib for the Treatment of Imatinib Refractory or Intolerant Gastrointestinal Stromal Tumors and Advanced Renal Cell Carcinoma

2007 • 471 citations

The Effect of Bcrp1 (Abcg2) on the In vivo Pharmacokinetics and Brain Penetration of Imatinib Mesylate (Gleevec): Implications for the Use of Breast Cancer Resistance Protein and P-Glycoprotein Inhibitors to Enable the Brain Penetration of Imatinib in Patients

2005 • 348 citations

Role of pharmacogenetics of ATP-binding cassette transporters in the pharmacokinetics of drugs

2006 • 347 citations

Mutations at amino-acid 482 in the ABCG2 gene affect substrate and antagonist specificity

2003 • 347 citations

High-Affinity Interaction of Tyrosine Kinase Inhibitors with the ABCG2 Multidrug Transporter

2004 • 338 citations

Overexpression of the ATP-binding cassette half-transporter, ABCG2 (Mxr/BCrp/ABCP1), in flavopiridol-resistant human breast cancer cells.

2001 • 338 citations

Pheophorbide a Is a Specific Probe for ABCG2 Function and Inhibition

2004 • 332 citations

P-glycoprotein-mediated drug efflux is a resistance mechanism of chronic myelogenous leukemia cells to treatment with imatinib mesylate

2004 • 310 citations

Erlotinib (Tarceva, OSI-774) Antagonizes ATP-Binding Cassette Subfamily B Member 1 and ATP-Binding Cassette Subfamily G Member 2–Mediated Drug Resistance

2007 • 299 citations

Regulation and targets of receptor tyrosine kinases

2002 • 260 citations

Food and Drug Administration Drug Approval Summary: Sunitinib Malate for the Treatment of Gastrointestinal Stromal Tumor and Advanced Renal Cell Carcinoma

2007 • 245 citations

Development of inhibitors of ATP-binding cassette drug transporters – present status and challenges

2008 • 241 citations

The Role of Efflux and Uptake Transporters inN-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine (GW572016, Lapatinib) Disposition and Drug Interactions

2008 • 234 citations

Multidrug Transporter ABCG2 Prevents Tumor Cell Death Induced by the Epidermal Growth Factor Receptor Inhibitor Iressa (ZD1839, Gefitinib)

2005 • 228 citations

The HER tyrosine kinase inhibitor CI1033 enhances cytotoxicity of 7-ethyl-10-hydroxycamptothecin and topotecan by inhibiting breast cancer resistance protein-mediated drug efflux.

2001 • 222 citations

Evidence for a requirement for ATP hydrolysis at two distinct steps during a single turnover of the catalytic cycle of human P-glycoprotein

2000 • 210 citations

Interaction of tyrosine kinase inhibitors with the human multidrug transporter proteins, MDR1 and MRP1

2002 • 209 citations

Chronic imatinib mesylate exposure leads to reduced intracellular drug accumulation by induction of the ABCG2 (BCRP) and ABCB1 (MDR1) drug transport pumps

2005 • 204 citations

Imatinib mesylate and nilotinib (AMN107) exhibit high-affinity interaction with ABCG2 on primitive hematopoietic stem cells

2007 • 201 citations

Gefitinib Enhances the Antitumor Activity and Oral Bioavailability of Irinotecan in Mice

2004 • 196 citations

[37] Drug-stimulatable ATPase activity in crude membranes of human MDR1-transfected mammalian cells

1998 • 194 citations

P-glycoprotein function involves conformational transitions detectable by differential immunoreactivity

1997 • 182 citations

Gefitinib Modulates the Function of Multiple ATP-Binding Cassette Transporters In vivo

2006 • 152 citations

Tyrosine kinase inhibitor resistance in cancer: role of ABC multidrug transporters

2005 • 147 citations

Effect of food on the pharmacokinetics of sunitinib malate (SU11248), a multi-targeted receptor tyrosine kinase inhibitor: results from a phase I study in healthy subjects

2006 • 134 citations

The Tyrosine Kinase Inhibitor Imatinib Mesylate Enhances the Efficacy of Photodynamic Therapy by Inhibiting ABCG2

2007 • 133 citations

Drug transporters: recent advances concerning BCRP and tyrosine kinase inhibitors

2008 • 107 citations

The Calcium Channel Blockers, 1,4-Dihydropyridines, Are Substrates of the Multidrug Resistance-Linked ABC Drug Transporter, ABCG2

2006 • 99 citations

Evidence for dual mode of action of a thiosemicarbazone, NSC73306: a potent substrate of the multidrug resistance–linked ABCG2 transporter

2007 • 96 citations

Gefitinib Reverses Chemotherapy Resistance in Gefitinib-Insensitive Multidrug Resistant Cancer Cells Expressing ATP-Binding Cassette Family Protein

2005 • 95 citations

The Molecular Basis of the Action of Disulfiram as a Modulator of the Multidrug Resistance-Linked ATP Binding Cassette Transporters MDR1 (ABCB1) and MRP1 (ABCC1)

2004 • 91 citations

Overexpression of P-glycoprotein in K562 cells does not confer resistance to the growth inhibitory effects of imatinib (STI571) in vitro

2003 • 86 citations

Inhibition of ABCG2-mediated transport by protein kinase inhibitors with a bisindolylmaleimide or indolocarbazole structure

2007 • 57 citations

Evidence for the Role of Glycosylation in Accessibility of the Extracellular Domains of Human MRP1 (ABCC1)

2002 • 54 citations

Analysis of MDR1 P-Glycoprotein Conformational Changes in Permeabilized Cells Using Differential Immunoreactivity

2001 • 53 citations

Loss of P-glycoprotein expression in hematopoietic stem cells does not improve responses to imatinib in a murine model of chronic myelogenous leukemia

2005 • 45 citations