Abstract
The superfamily of organic anion-transporting polypeptides (OATPs, gene symbol SLCO) includes important transporters handling a variety of endogenous and xenobiotic substrates. Currently, 11 human OATPs are known and their substrates include endogenous hormones and their conjugates, anticancer drugs, and imaging agents. The contribution of OATPs to the in vivo disposition of these substrates has been extensively investigated. An accumulating body of evidence also indicates that the expression of some OATPs may be up- or downregulated in several types of cancers, suggesting potential pathogenic roles during the development and progression of cancer. Given that the role of OATPs in handling cancer therapeutics has been already covered by several excellent reviews, this review will focus on the recent progresses on the topic, in particular the role of OATPs in the disposition of anticancer drugs, the impact of OATP genetic variations on the function of OATPs, and the OATPs differentially expressed in cancer and their potential roles in cancer development, progression, and treatment.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 535-545 |
| Number of pages | 11 |
| Journal | AAPS Journal |
| Volume | 17 |
| Issue number | 3 |
| DOIs | |
| State | Published - May 1 2015 |
| Externally published | Yes |
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Keywords
- cancer therapy
- organic anion-transporting polypeptides
- transporters
ASJC Scopus subject areas
- Pharmaceutical Science
Cite this
Role of Organic Anion-Transporting Polypeptides (OATPs) in Cancer Therapy. / Thakkar, Nilay; Lockhart, Albert; Lee, Wooin.
In: AAPS Journal, Vol. 17, No. 3, 01.05.2015, p. 535-545.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Role of Organic Anion-Transporting Polypeptides (OATPs) in Cancer Therapy
AU - Thakkar, Nilay
AU - Lockhart, Albert
AU - Lee, Wooin
PY - 2015/5/1
Y1 - 2015/5/1
N2 - The superfamily of organic anion-transporting polypeptides (OATPs, gene symbol SLCO) includes important transporters handling a variety of endogenous and xenobiotic substrates. Currently, 11 human OATPs are known and their substrates include endogenous hormones and their conjugates, anticancer drugs, and imaging agents. The contribution of OATPs to the in vivo disposition of these substrates has been extensively investigated. An accumulating body of evidence also indicates that the expression of some OATPs may be up- or downregulated in several types of cancers, suggesting potential pathogenic roles during the development and progression of cancer. Given that the role of OATPs in handling cancer therapeutics has been already covered by several excellent reviews, this review will focus on the recent progresses on the topic, in particular the role of OATPs in the disposition of anticancer drugs, the impact of OATP genetic variations on the function of OATPs, and the OATPs differentially expressed in cancer and their potential roles in cancer development, progression, and treatment.
AB - The superfamily of organic anion-transporting polypeptides (OATPs, gene symbol SLCO) includes important transporters handling a variety of endogenous and xenobiotic substrates. Currently, 11 human OATPs are known and their substrates include endogenous hormones and their conjugates, anticancer drugs, and imaging agents. The contribution of OATPs to the in vivo disposition of these substrates has been extensively investigated. An accumulating body of evidence also indicates that the expression of some OATPs may be up- or downregulated in several types of cancers, suggesting potential pathogenic roles during the development and progression of cancer. Given that the role of OATPs in handling cancer therapeutics has been already covered by several excellent reviews, this review will focus on the recent progresses on the topic, in particular the role of OATPs in the disposition of anticancer drugs, the impact of OATP genetic variations on the function of OATPs, and the OATPs differentially expressed in cancer and their potential roles in cancer development, progression, and treatment.
KW - cancer therapy
KW - organic anion-transporting polypeptides
KW - transporters
UR - http://www.scopus.com/inward/record.url?scp=84939998522&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84939998522&partnerID=8YFLogxK
U2 - 10.1208/s12248-015-9740-x
DO - 10.1208/s12248-015-9740-x
M3 - Article
C2 - 25735612
AN - SCOPUS:84939998522
VL - 17
SP - 535
EP - 545
JO - AAPS Journal
JF - AAPS Journal
SN - 1522-1059
IS - 3
ER -