Estrogen receptor-α (ER- α) is a principal endocrine regulatory protein in breast cancer. The progression of ER-α positive breast cancer is slowed by selective estrogen receptor modulators such as Tamoxifen. But, long term therapy with Tamoxifen leads to resistance. Therefore, it is of interest to document the Molecular docking and pharmacokinetic analysis of imeglimin derivatives with ER-alpha. Among the 166 derivatives of Imeglimin, only five derivatives were shortlisted after toxicity testing. The selected derivatives showed good binding affinity with favorable pharmacokinetic profiles. The selected compounds of Imeglimin were found to possess excellent anticancer potential and could be considered as novel, cost-effective anticancer agents effective against ER positive breast cancer for further investigation.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11414348 | PMC |
| http://dx.doi.org/10.6026/973206300200711 | DOI Listing |
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Imeglimin, unlike metformin, does not perturb differentiation of human induced pluripotent stem cells towards pancreatic β-like cells and rather enhances gain in β cell identity gene sets.
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Department of Metabolic Medicine, Osaka University Graduate School of Medicine, Osaka, Japan.
Aims/introduction: Metformin treatment for hyperglycemia in pregnancy (HIP) beneficially improves maternal glucose metabolism and reduces perinatal complications. However, metformin could impede pancreatic β cell development via impaired mitochondrial function. A new anti-diabetes drug imeglimin, developed based on metformin, improves mitochondrial function.
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J Diabetes Investig
December 2024
Department of Medicine, Kawasaki Medical School, Okayama, Japan.
Introduction: An increased rate of gastrointestinal (GI) symptoms is reported in patients with type 2 diabetes receiving imeglimin plus metformin vs monotherapy or in combination with other antidiabetic drugs. This post-hoc analysis explored GI symptom incidence, risk factors for their occurrence, and the impact on therapeutic efficacy during imeglimin and metformin combination therapy.
Materials And Methods: Data were derived from the 52-week, open-label, phase 3 TIMES-2 trial in Japanese type 2 diabetes patients.
Molecular docking analysis of imeglimin and its derivatives with estrogen receptor-alpha.
Bioinformation
July 2024
Department of Pharmacology, Tagore Medical College and Hospital, Chennai.
Estrogen receptor-α (ER- α) is a principal endocrine regulatory protein in breast cancer. The progression of ER-α positive breast cancer is slowed by selective estrogen receptor modulators such as Tamoxifen. But, long term therapy with Tamoxifen leads to resistance.
View Article and Find Full Text PDFImeglimin enhances glucagon secretion through an indirect mechanism and improves fatty liver in high-fat, high-sucrose diet-fed mice.
J Diabetes Investig
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Metabolic Signal Research Center, Institute for Molecular and Cellular Regulation, Gunma University, Gunma, Japan.
Aims/introduction: Imeglimin is a recently approved oral antidiabetic agent that improves insulin resistance, and promotes insulin secretion from pancreatic β-cells. Here, we investigated the effects of imeglimin on glucagon secretion from pancreatic α-cells.
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Department of Endocrinology and Metabolism, Ajou University School of Medicine, Suwon, 16499, Republic of Korea. Electronic address:
Imeglimin is a novel oral antidiabetic drug for treating type 2 diabetes. However, the effect of imeglimin on NLRP3 inflammasome activation has not been investigated yet. Here, we aimed to investigate whether imeglimin reduces LPS-induced NLRP3 inflammasome activation in THP-1 macrophages and examine the associated underlying mechanisms.
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