Vinca alkaloid and MDR1

Nagio Takigawa, Mitsune Tanimoto

Research output: Contribution to journalArticle

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Abstract

Vinca alkaloids inhibit microtubule formation by binding to tubulin. There are four clinically available vinca alkaloids including vincristine, vinblastine, vindesine, and vinorelbine. P-glycoprotein(P-gp)is the one of the efflux adenosine triphosphate(ATP)-binding cassette family transporters and is the encoded product of MDR1 gene. P-gp is overexpressed not only in tumor cells resistant to multiple anticancer agents but also found in normal cells such as liver, gastrointestinal tract and kidney, working as a biological defense mechanism. Single nucleotide polymorphisms for MDR1 in exon 12(1236), exon 21(2677), and exon 26(3435)have been well studied. Although C1236T and C3435T do not change the amino acid, G2677T and G2677A result in amino acid substitution of Ala893Ser and Ala893Thr, respectively. In the use of haplotypes to predict vincristine pharmacokinetics, the correlation between the haplotypes and the elimination half-life was reported. Many studies of the relationship between polymorphism/haplotype for MDR1 and pharmacodynamics including efficacy and toxicity of chemotherapy have been explored.

Original languageEnglish
Pages (from-to)1086-1089
Number of pages4
JournalGan to kagaku ryoho. Cancer & chemotherapy
Volume35
Issue number7
Publication statusPublished - Jul 2008

Fingerprint

Vinca Alkaloids
Haplotypes
Exons
P-Glycoprotein
Vincristine
Vindesine
Vinblastine
Amino Acid Substitution
Tubulin
Microtubules
Antineoplastic Agents
Single Nucleotide Polymorphism
Half-Life
Gastrointestinal Tract
Pharmacokinetics
Adenosine Triphosphate
Kidney
Amino Acids
Drug Therapy
Liver

ASJC Scopus subject areas

  • Cancer Research
  • Pharmacology

Cite this

Takigawa, N., & Tanimoto, M. (2008). Vinca alkaloid and MDR1. Gan to kagaku ryoho. Cancer & chemotherapy, 35(7), 1086-1089.

Vinca alkaloid and MDR1. / Takigawa, Nagio; Tanimoto, Mitsune.

In: Gan to kagaku ryoho. Cancer & chemotherapy, Vol. 35, No. 7, 07.2008, p. 1086-1089.

Research output: Contribution to journalArticle

Takigawa, N & Tanimoto, M 2008, 'Vinca alkaloid and MDR1', Gan to kagaku ryoho. Cancer & chemotherapy, vol. 35, no. 7, pp. 1086-1089.
Takigawa N, Tanimoto M. Vinca alkaloid and MDR1. Gan to kagaku ryoho. Cancer & chemotherapy. 2008 Jul;35(7):1086-1089.
Takigawa, Nagio ; Tanimoto, Mitsune. / Vinca alkaloid and MDR1. In: Gan to kagaku ryoho. Cancer & chemotherapy. 2008 ; Vol. 35, No. 7. pp. 1086-1089.
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