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Related Experiment Videos

Acyclovir transport into human erythrocytes.

W B Mahony1, B A Domin, R T McConnell

  • 1Experimental Therapy Department, Wellcome Research Laboratories, Research Triangle Park, North Carolina 27709.

The Journal of Biological Chemistry
|July 5, 1988
PubMed
Summary
This summary is machine-generated.

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Acyclovir (ACV) enters human red blood cells via the nucleobase carrier, not the nucleoside transport system. This antiviral drug shares transport with adenine, guanine, and hypoxanthine.

Area of Science:

  • Pharmacology
  • Cell Biology
  • Biochemistry

Background:

  • Acyclovir (ACV) is a crucial antiviral medication.
  • Understanding ACV transport into human erythrocytes is vital for optimizing drug delivery and efficacy.
  • Existing research suggests potential involvement of nucleoside transporters.

Purpose of the Study:

  • To elucidate the specific mechanism of acyclovir (ACV) transport into human erythrocytes.
  • To determine if ACV utilizes the established nucleoside transport system or an alternative pathway.
  • To identify potential carriers involved in ACV influx.

Main Methods:

  • Utilized an

Main Results:

  • ACV influx into erythrocytes was found to be rate-saturable (Km = 260 +/- 20 microM) but nonconcentrative.

Related Experiment Videos

  • Potent nucleoside transport inhibitors (dipyridamole, etc.) showed minimal inhibition (<8%) of ACV influx.
  • ACV transport was competitively inhibited by adenine, guanine, and hypoxanthine, and ACV competitively inhibited their transport.
  • Structurally related antivirals, desciclovir and ganciclovir, also inhibited ACV influx.

    • Conclusions:

    • Acyclovir (ACV) primarily enters human erythrocytes via the nucleobase carrier system.
    • ACV transport is distinct from the canonical nucleoside transport system.
    • The findings suggest a shared transport mechanism for ACV and natural nucleobases like adenine and guanine.