Last call to you our next Webinar on 1 March! - Sulfate Conjugates as Solute Carrier Transporter Substrates; Probes, Biomarkers, and Utility?

February 28, 2017

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Title: Sulfate Conjugates as Solute Carrier Transporter Substrates; Probes, Biomarkers, and Utility?

Presenter:

A. David Rodrigues, PhD
Head of Transporter Sciences Group,
Pfizer Inc.,
Groton CT USA

Date: Wednesday, 1 March, 2017

Time: 4:00 PM (CET)
      3:00 PM (GMT)
      7:00 AM (PST)
      10:00 AM (EDT)
      8:30 PM (IST, India)
      5:00 PM (IST, Israel)


Summary of the presentation:

Sulfotransferases (SULTs) are expressed in numerous tissues and catalyze the sulfation of many steroidal drugs and endogenous compounds.  Examples include 17α-ethinylestradiol, estrone, various bile acids, and dehydroepiandrosterone (DHEA).  Once formed, sulfate conjugates present as transporter [solute carrier (SLC) and ATP-binding cassette (ABC)] substrates and are secreted into bile, circulate, and eliminated in urine.  Consequently, attention has focused on the study of the “SULT-transporter axis” and vectorial (sequential SLC-ABC) transport of sulfo-conjugates in clearance organs like the intestine, liver and kidney.  In particular, various groups have sort to identify, develop and validate individual sulfate conjugates as clinical biomarkers for different transporters; the availability of such tools could facilitate transporter phenotyping and drug-drug interaction assessment.  For example, the 3-O-sulfate of DHEA (DHEAS) has been proposed as a hepatic OATP (organic anion transporting polypeptide) biomarker.  Likewise, the 3-O-sulfate form of glycochenodeoxycholic acid (GCDCA-S) has been studied as a biomarker of renal OAT3 (organic anion transporter 3).  Numerous groups have also deployed estrone 3-O-sulfate (E3S) as an OATP probe, which has supported relative activity factor-based SLC phenotyping in vitro.  The webinar will focus on examples of steroidal sulfate conjugates as transporter substrates, probes, and potential biomarkers.  As an uptake organ, the liver will be presented in terms of the “big seven” SLCs [OATP1B1, OATP1B3, OATP2B1, organic cation transporter 1 (OCT1), sodium-taurocholate co-transporting polypeptide (NTCP), OAT2, and OAT7]. 

Please click here for the speaker’s Bio.

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