Abstract:
:Human multidrug resistance protein (MRP/ABCC) family contains 9 members (MRP1-9) which transport a structurally diverse array of anticancer and antimicrobial drugs and several important endogenous substances including prostaglandins (PGs) and leukotrienes (LTs) with different substrate specificity. MRP1-5 can collectively confer resistance to natural product anticancer drugs and their conjugated metabolites, platinum compounds, folate antimetabolites, nucleoside and nucleotide analogs, and alkylating agents. MRP1-3 are often associated with tumor resistance which is often caused by an increased efflux and decreased intracellular accumulation of natural product anticancer drugs and other anticancer agents. Both PGE(1) and PGE(2) are known high-affinity substrates of MRP4, but not MRP1, MRP2, MRP3 and MRP5. LTC(4) is a substrate of MRP1, MRP2, MRP3, and MRP6-8. MRP2 is also able to transport LTD(4) and LTE(4). Experimental studies in Abcc1-difficient mice have demonstrated a role of MRP1 in inflammation process in vivo. Abcc3-difficient mice have normal bile salt transport, however they have decreased blood bilirubin glucuronide levels. Abcc6-difficient mice show remarkable mineraliztion of the connective tissues, including skin, arterial blood vessels, and retina. Most MRP/ABCC transporters are subject to inhibition by a variety of compounds. Drug targeting of these transporters to overcome MRP/ABCC-mediated multidrug resistance may play a role in cancer and infection (e.g. HIV infection) chemotherapy. Some modulators of MRPs have shown reversing effects on MDR phenotype in preliminary clinical studies and some modulators of MRPs may modify the inflammatory process and consequently ameliorate the inflammatory symptoms. A better understanding of the interactions of these modulators with MRPs has important implications in development of novel drugs for treatment of cancer, infection and inflammation.
journal_name
Curr Top Med Chemjournal_title
Current topics in medicinal chemistryauthors
Yang AK,Zhou ZW,Wei MQ,Liu JP,Zhou SFdoi
10.2174/156802610792928040subject
Has Abstractpub_date
2010-01-01 00:00:00pages
1732-56issue
17eissn
1568-0266issn
1873-4294pii
BSP/ CTMC /E-Pub/-0109-10-18journal_volume
10pub_type
杂志文章,评审abstract:INTRODUCTION:Anxiety disorders manifest in women more than in men by almost twofold. This narrative review aims to summarize the sex-related biological factors, which underpin anxiety, focusing on the interactions of sex and tryptophan/serotonin with anxiety. METHODS:A literature search was conducted using Google Scho...
journal_title:Current topics in medicinal chemistry
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journal_title:Current topics in medicinal chemistry
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journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
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journal_title:Current topics in medicinal chemistry
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journal_title:Current topics in medicinal chemistry
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journal_title:Current topics in medicinal chemistry
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journal_title:Current topics in medicinal chemistry
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