Topological Polar Surface Area Defines Substrate Transport by Multidrug Resistance Associated Protein 1 (MRP1/ABCC1)

被引：86

作者：

Fernandes, Janaina ^{[1
]}

Gattass, Cerli R. ^{[1
]}

机构：

[1] Univ Fed Rio de Janeiro, Inst Biofis Carlos Chagas Filho, Ctr Ciencias Saude, Lab Imunol Celular, BR-21949900 Rio De Janeiro, Brazil

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 52卷 / 04期

关键词：

GLUTATHIONE-S-TRANSFERASE; MEDIATED VINCRISTINE RESISTANCE; ATP-DEPENDENT EFFLUX; LEUKOTRIENE C-4; P-GLYCOPROTEIN; MRP1; CONJUGATE; INHIBITION; DRUGS; DETOXIFICATION;

D O I：

10.1021/jm801389m

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Multidrug resistance-associated protein 1 (MRP1/ABCC1) is a very promiscuous transporter. Herein we used topological polar surface area (TPSA), a descriptor defined as the sum of surfaces of polar atoms in a molecule, to analyze drug transport by MRP1. We suggested that compounds with high TPSA are transported while those with low TPSA are not. The conjugation to GSH increases TPSA values favoring transport. A strong correlation between TPSA and transport properties (K-m) was also found.

引用

下载

页码：1214 / 1218

页数：5

共 50 条

[21] Identification of multidrug resistance protein 1 (MRP1/ABCC1) as a molecular gate for cellular export of cobalamin
Beedholm-Ebsen, Rasmus
van de Wetering, Koen
Hardlei, Tore
Nexo, Ebba
Borst, Piet
Moestrup, Soren K.
BLOOD, 2010, 115 (08) : 1632 - 1639
[22] The structure of the multidrug resistance protein 1 (MRP1/ABCC1) - Crystallization and single-particle analysis
Rosenberg, MF
Mao, QC
Holzenburg, A
Ford, RC
Deeley, RG
Cole, SPC
JOURNAL OF BIOLOGICAL CHEMISTRY, 2001, 276 (19) : 16076 - 16082
[23] Role of GSH in estrone sulfate binding and translocation by the multidrug resistance protein 1 (MRP1/ABCC1)
Rothnie, Alice
Callaghan, Richard
Deeley, Roger G.
Cole, Susan P. C.
JOURNAL OF BIOLOGICAL CHEMISTRY, 2006, 281 (20) : 13906 - 13914
[24] Cloning and functional characterization of the multidrug resistance-associated protein (MRP1/ABCC1) from the cynomolgus monkey
Godinot, N
Iversen, PW
Tabas, L
Xia, XL
Williams, DC
Dantzig, AH
Perry, WL
MOLECULAR CANCER THERAPEUTICS, 2003, 2 (03) : 307 - 316
[25] Modulation of multidrug resistance protein (MRP1/ABCC1) expression: a novel physiological role for ouabain
Valente, R. C.
Capella, L. S.
Nascimento, C. R.
Lopes, A. G.
Capella, M. A. M.
CELL BIOLOGY AND TOXICOLOGY, 2007, 23 (06) : 421 - 427
[26] Modulation of multidrug resistance protein (MRP1/ABCC1) expression: a novel physiological role for ouabain
R. C. Valente
L. S. Capella
C. R. Nascimento
A. G. Lopes
M. A. M. Capella
Cell Biology and Toxicology, 2007, 23 : 421 - 427
[27] Arsenic transport by the human multidrug resistance protein 1 (MRP1/ABCC1) - Evidence that a tri-glutathione conjugate is required
Leslie, EM
Haimeur, A
Waalkes, MP
JOURNAL OF BIOLOGICAL CHEMISTRY, 2004, 279 (31) : 32700 - 32708
[28] Interaction of plant cannabinoids with the multidrug transporter ABCC1 (MRP1)
Holland, Michelle L.
Allen, John D.
Arnold, Jonathon C.
EUROPEAN JOURNAL OF PHARMACOLOGY, 2008, 591 (1-3) : 128 - 131
[29] The multidrug resistance-associated protein 1 (MRP1/ABCC1) protects the testicular tubules against methoxychlor damage.
Bain, L
Bruner, RH
Tribull, TE
TOXICOLOGICAL SCIENCES, 2003, 72 : 87 - 87
[30] HTLV-1 alters the multidrug resistance associated protein 1 (ABCC1/MRP1) expression and activity in human T cells
Echevarria-Lima, Juliana
Rumjanek, Vivian M.
Kyle-Cezar, Fernanda
Harab, Ramza C.
Leite, Ana Claudia Celestino B.
Ornellas, Debora dos Santos
Moralles, Marcelo Marcos
Araujo, Abelardo Q. C.
Andrada-Serpa, Maria Jose
JOURNAL OF NEUROIMMUNOLOGY, 2007, 185 (1-2) : 175 - 181

← 1 2 3 4 5 →