Effect of UGT1A1 and UGT1A3 polymorphisms on Pharmacokinetics of Telmisartan in Korean

Shin, Hyun-June; Kim, J.-E.; Lim, Siew-Eng; Seo, Junghwa; Kim, M.H.; Hoon, O.K.; Kim, H.S.; Hasanuzzaman, Md.; Parvez, Md. Masud; Kim, D.-H.; Shin, Jae‐Gook

doi:10.1016/j.clinthera.2015.05.253

Cited by 2 publications

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“…However, we demonstrate higher moxifloxacin concentrations with heterozygous TA5/6 genotypes compared with TA6/6, TA6/7 and TA7/8 genotypes. Similar findings were reported with telmisartan [39] raloxifene [40] and moxifloxacin in healthy individuals [19], where higher concentrations of metabolites and resultant lower drug exposures were observed with TA7 (UGT1A1*28). The reasons for this contrasting effect are not entirely clear, but may be linked to extensive sharing of exons in the UGT1A family and genetic linkage between many UGT variants (which may differ between ethnic groups) contributing to discordance between findings.…”

Section: Discussionsupporting

confidence: 82%

Effect of Genetic Variation in UGT1A and ABCB1 on Moxifloxacin Pharmacokinetics in South African Patients with Tuberculosis

et al. 2017

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Section: Discussionsupporting

confidence: 82%

Effect of Genetic Variation in UGT1A and ABCB1 on Moxifloxacin Pharmacokinetics in South African Patients with Tuberculosis

et al. 2017

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“…It is widely used in the treatment of hypertension in the clinic. Telmisartan is metabolised by UGTs (Shin HJ. et al, 2015).…”

Section: Discussionmentioning

confidence: 99%

In Silico Approach For Detection Of The Effect Of UGT1A1 Polymorphisms On Telmisartan Response

KÜÇÜK>

2022

Bulletin of Biotechnology

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Hypertension is a cardiovascular disease that manifests itself with a continuous increase in systemic arterial blood pressure and can lead to serious complications over time. It is estimated that 37% of hypertensive patients receive treatment and one-third of them are under control. Telmisartan is an angiotensin receptor blocker used in the treatment of hypertension. Uridine 5'-diphospho-glucuronyltransferase 1 (UGT1A1) gene encodes the Uridine 5'-diphospho-glucuronyltransferase (UGT) enzyme and metabolizes the telmisartan. Single nucleotide polymorphisms cause amino acid, protein structure, and function to change. These changes affect the drug response and therapy. Polymorphisms of the UGT1A1 gene (rs4148323, rs28934877) cause telmisartan resistance. In this study, the SWISS-MODEL database and Chimera 1.15 ver. Programs were used to create homology models. The HOPE database was used to calculate the damage of mutation on protein structure and show the mutation effects on protein. The HDock server was used to demonstrate interactions between telmisartan and wild-type protein and, mutant type protein. It was detected that the mutant residue of UGT1A1 (rs4148323) is located in an important domain for protein activity. Mutation might disturb the protein function. rs28934877 was detected that this mutation is probably damaging to the protein. These mutations cause the loss of interactions and affect the drug response. By docking analysis, Telmisartan drug interactions were shown between wild and mutant types protein Possible drug conformation is designed for the effective treatment of patients carrying the common mutation.

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Effect of UGT1A1 and UGT1A3 polymorphisms on Pharmacokinetics of Telmisartan in Korean

Cited by 2 publications

References 0 publications

Effect of Genetic Variation in UGT1A and ABCB1 on Moxifloxacin Pharmacokinetics in South African Patients with Tuberculosis

Effect of Genetic Variation in UGT1A and ABCB1 on Moxifloxacin Pharmacokinetics in South African Patients with Tuberculosis

In Silico Approach For Detection Of The Effect Of UGT1A1 Polymorphisms On Telmisartan Response

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