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Afimoxifene

Afimoxifene is a selective estrogen receptor modulator (SERM) used in the treatment of certain types of breast cancer.
It acts by binding to and modulating the activity of estrogen receptors, thereby inhibiting the growth of estrogen-dependent tumors.
Afimoxifene has been studied for its potential to improve outcomes in patients with estrogen receptor-positive breast cancer, and has shown promise in clinical trials.
However, further research is needed to fully understand its efficacy and optimal use in clinical practice.
This MeSH term provides a concise overview of the key facts and uses of Afimoxifene in the treatment of breast cancer.

Most cited protocols related to «Afimoxifene»

1
Purification and Characterization of Sulfotransferases
Cited 2 times
The experimental materials and their sources
are as follows. Adenosine
monophosphate (AMP), dithiothreitol (DTT), dimethyl sulfoxide (DMSO),
ethylenediaminetetraacetic acid (EDTA), 1-hydroxypyrene (1-HP), 4-hydroxytamoxifen
(afimoxifene, TAM), imidazole, isopropyl thio-β-d-galactopyranoside
(IPTG), Luria broth (LB), lysozyme, β-mercaptoethanol (β-ME),
pepstatin A, Na2HPO4, and NaH2PO4 were obtained from Sigma. Ampicillin, HEPES, KCl, KOH, MgCl2, NaCl, and phenylmethanesulfonyl fluoride (PMSF) were purchased
from Fisher Scientific. Glutathione- and nickel-chelating resins were
obtained from GE Healthcare. Competent Escherichia coli [BL21(DE3)] cells were purchased from Agilent Technologies. PAP,
PAPS, and [35S]PAPS were synthesized in house as previously
described12 (link),16 (link),17 (link) and were ≥98%
pure as assessed by anion-exchange high-performance liquid chromatography.
Wang T., Cook I, & Leyh T.S. (2014). 3′-Phosphoadenosine 5′-Phosphosulfate Allosterically Regulates Sulfotransferase Turnover. Biochemistry, 53(44), 6893-6900.
Publication 2014
1-hydroxypyrene 2-Mercaptoethanol ACPP protein, human afimoxifene Ampicillin Anions Cells Dithiothreitol Edetic Acid Escherichia coli Galactose Glutathione HEPES High-Performance Liquid Chromatographies imidazole Isopropyl Thiogalactoside Magnesium Chloride Muramidase Nickel pepstatin Phenylmethylsulfonyl Fluoride Resins, Plant Sodium Chloride Sulfoxide, Dimethyl
2
Quantitative Analysis of SERMs

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Publication 2022
acetonitrile afimoxifene droloxifene Lasofoxifene Nafoxidine Tamoxifen Toremifene
3
Structures and Conformations of Estrogen-Related Ligands
Structures of ligands (Figure 2) were retrieved from the PubChem database [60 (link)]: 17β-estradiol (ID: 5757), estrone (ID: 5870), DES (ID: 448537), tamoxifen (ID: 2733526), endoxifen (ID: 10090750) and afimoxifene (ID: 449459). For accurate 3D ligand model generation and conformational sampling, all ligands were subjected to structure refinement, tautomeric and ionization state prediction, and an optimization procedure using LigPrep suite [61 ] in Schrödinger software with application of the OPLS3e force field. Protonated states were generated at pH 7.4 ± 1.0 with implementation of the Epik algorithm version 4.4 [62 (link)]. For each ligand, 32 possible stereo-isomeric forms were set.
Moldogazieva N.T., Ostroverkhova D.S., Kuzmich N.N., Kadochnikov V.V., Terentiev A.A, & Porozov Y.B. (2020). Elucidating Binding Sites and Affinities of ERα Agonists and Antagonists to Human Alpha-Fetoprotein by In Silico Modeling and Point Mutagenesis. International Journal of Molecular Sciences, 21(3), 893.
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Publication 2020
4-hydroxy-N-desmethyltamoxifen afimoxifene Estradiol Estrone Isomerism Ligands Tamoxifen
4
Biodistribution of Selective Estrogen Receptor Modulators

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Publication 2022
afimoxifene Animals BLOOD Bones Brain droloxifene Females Heart Hemizygote Intestines Kidney Lasofoxifene Liver Lung Males Mice, House Mouse mammary tumor virus Muscle Tissue Nafoxidine Neoplasms Pad, Fat Pancreas Pharmaceutical Preparations Plasma Skin Spleen Stomach Tamoxifen Tandem Mass Spectrometry Toremifene Uterus
5
Quantitative LC-MS/MS Analysis of SERMs

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Publication 2022
acetonitrile afimoxifene Biological Assay Biopharmaceuticals BLOOD droloxifene formic acid High-Performance Liquid Chromatographies Lasofoxifene Nafoxidine Neoplasms Plasma Raloxifene Tamoxifen Tandem Mass Spectrometry Toremifene

Most recents protocols related to «Afimoxifene»

1
Quantitative Analysis of SERMs

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Publication 2022
acetonitrile afimoxifene droloxifene Lasofoxifene Nafoxidine Tamoxifen Toremifene
2
Biodistribution of Selective Estrogen Receptor Modulators

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Publication 2022
afimoxifene Animals BLOOD Bones Brain droloxifene Females Heart Hemizygote Intestines Kidney Lasofoxifene Liver Lung Males Mice, House Mouse mammary tumor virus Muscle Tissue Nafoxidine Neoplasms Pad, Fat Pancreas Pharmaceutical Preparations Plasma Skin Spleen Stomach Tamoxifen Tandem Mass Spectrometry Toremifene Uterus
3
Quantitative LC-MS/MS Analysis of SERMs

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Publication 2022
acetonitrile afimoxifene Biological Assay Biopharmaceuticals BLOOD droloxifene formic acid High-Performance Liquid Chromatographies Lasofoxifene Nafoxidine Neoplasms Plasma Raloxifene Tamoxifen Tandem Mass Spectrometry Toremifene
4
Prostate Organoid Culture and Xenograft Modeling
The lobes of the prostate were isolated from TMPRSS2Cre‐ERT2‐IRES‐GFP; Ptenfl/fl mice, minced into small pieces (∼1 mm3), digested at 37°C on a shaking platform and sorted by GFP expression to isolate prostate luminal cells. Cells were resuspended in phosphate buffered saline (PBS) mixed with Matrigel (BD Biosciences, volume ratio = 1:1), and the suspensions were plated into 24‐well plates covered with prostate organoid culture. Afimoxifene (4‐OHT, Sigma–Aldrich, H7904) was added to the culture to induce CreERT2 and Pten deletion. Then, the packaged lentivirus was added to the organoids, and infected cells were selected by puromycin. The numbers, size and formation efficiency of the organoids were determined on day 10. Urogenital sinus mesenchyme (UGSM) cell isolation and the organoid transplantation assay were performed as previously described.17 A total of 1×106 UGSM cells were mixed with 1×106 organoid cells stably expressing luciferase and then used to generate xenografts. The cells were resuspended in Matrigel (BD Biosciences, 1:1) and then injected into the VPs of 6‐week‐old male NSG mice. Two months later, a NightOWL II LB 983 Imaging System (Berthold Technologies) was used to conduct BLI and determine the tumour volumes in mice.
Biopsy specimens from PCa patients were minced into small pieces (∼1 mm3) and digested at 37°C on a shaking platform in 5 ml of 5 mg/ml type II collagenase (Invitrogen) in Advanced DMEM/F12 (ADMEM/F12) for 2 h. Dissociated cells were washed and resuspended in PBS mixed with Matrigel (BD Biosciences, volume ratio = 1:1), and the suspensions were plated into 24‐well plates covered with prostate organoid culture. Human PCa organoids were weekly passaged at a 1:3 passage ratio, digested by TrypLE (Sigma–Aldrich) at 37°C for 5 min. The organoids were cultured and collected for Western blotting (WB). The reagents used for the organoid culture are listed in the Supporting information.
Ding Y., Shao J., Shi T., Yu H., Wang X., Chi H, & Wang X. (2022). Leukemia inhibitory factor receptor homodimerization mediated by acetylation of extracellular lysine promotes prostate cancer progression through the PDPK1/AKT/GCN5 axis. Clinical and Translational Medicine, 12(2), e676.
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Publication 2022
afimoxifene Biological Assay Biopsy Cells Cell Separation Collagenase Deletion Mutation Homo sapiens Internal Ribosome Entry Sites Lentivirus Luciferases Males matrigel Mesenchyma Mesenchymal Stem Cells mitogen-activated protein kinase 3, human Mus Organoids Patients Phenobarbital Phosphates PTEN protein, human Puromycin Saline Solution Sinuses, Nasal System, Genitourinary Transplantation Type II Mucolipidosis Xenografting
5
Molecular Docking of Breast Cancer Compounds
Not available on PMC !
ER-α (protein data bank ID: 3ERT) was used in this research for screening compound mechanism against breast cancer cells activity. The 3-dimensional structures were retrieved from RSCB Protein Data Bank (https://www.rcsb.org/) obtained in PDB format. Afimoxifene (4-OHT) was used as a positive control ligand and estradiol ligand for comparison. The 3D structures of the compounds were modeled by using Biovia Discovery Studio program (Mukund et al., 2019) .
Autodock Vina (open-source software PyRx 0.8) was used for the ligand-protein docking and virtual screening for anticancer activity of the compounds. Compound 1, compound 2, 4-OHT, and estradiol were subjects for binding to ER-α as protein target, the ligand was free for blind docking. Before the ligand is thetered to the receptor, it is necessary to identify the active pocked that binds to the receptor through grid parameters. The grid box was produced by redocking tamoxifen against ERα is x=30.282; y=1.1913; z=24.207 with a space volume of 40x40x40 points. The conformation was selected based on binding energy, the one with the lowest binding affinity score. The docking simulation was performed at the center of the active side of the receptor with coordinates (x = 30.010, y = -1.913, and z = 24.207) selected.
The docking results were visualized by using Biovia Discovery Studio program. Ligand-residue interaction and docking poses in the 3-dimension molecular picture were showed by the program. The docking pose of each protein-ligand complex was compared by looking at the side of the amino acid residue that binds the ligand. The similarity from ligation poses of compound 1 and 2, 4-OHT, and estradiol that bound on amino acid residues was determined and the relation of the docking pose of the ligands and protein targets being studied was selected. Prediction of pharmacokinetics was carried out with a SMILE structure analyzed using swiss ADME http://www.swissadme.ch/index.php) (Daina et al., 2017) .
Purwani S., Nahar J., Zulfikar Z., Nurlelasari N., & Mayanti T. (2021). Molecular Docking on Kokosanolide A and C for Anticancer Activity Against Human Breast Cancer Cell MCF-7. Jurnal Kimia VALENSI, 7(1), 52-57.
Publication 2021

Top products related to «Afimoxifene»

1
Imidazole by Merck Group
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Imidazole is a heterocyclic organic compound with the chemical formula C3H4N2. It is a five-membered aromatic ring containing two nitrogen atoms. Imidazole serves as a core functional group in various chemical and biological applications.
2
Toremifene by Merck Group
Sourced in United States
Toremifene is a selective estrogen receptor modulator (SERM) used in pharmaceutical research and development. It functions as an antagonist of the estrogen receptor, binding to the receptor and inhibiting the effects of estrogen. Toremifene is commonly used in cell culture and in vivo studies to investigate the role of estrogen signaling in various biological processes.
3
Tamoxifen by Merck Group
Sourced in United States, Germany, Sao Tome and Principe, United Kingdom, Switzerland, Macao, China, Australia, Canada, Japan, Spain, Belgium, France, Italy, New Zealand, Denmark
Tamoxifen is a drug used in the treatment of certain types of cancer, primarily breast cancer. It is a selective estrogen receptor modulator (SERM) that can act as both an agonist and antagonist of the estrogen receptor. Tamoxifen is used to treat and prevent breast cancer in both men and women.
4
Milli q water system by Merck Group
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The Milli-Q water system is a laboratory water purification device that produces high-quality, ultrapure water. The system utilizes a multi-stage filtration process to remove impurities, resulting in water that meets the stringent requirements for various laboratory applications.
5
Pepstatin a by Merck Group
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Pepstatin A is a peptide inhibitor that specifically targets aspartic proteases. It is commonly used in biochemical research applications to inhibit the activity of proteases such as pepsin, renin, and cathepsin D.
6
Luria broth by Merck Group
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Luria broth is a nutrient-rich microbial growth medium commonly used in laboratory settings. It provides essential nutrients and support for the cultivation of a variety of bacterial species, including Escherichia coli. The broth, also known as LB, is formulated to promote the growth and proliferation of microorganisms, facilitating their use in various experimental and research applications.
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Xbridge c18 column by Waters Corporation
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HEPES is a buffering agent commonly used in cell culture and biochemical applications. It maintains a stable pH within a physiological range and is compatible with a variety of biological systems.
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Abi 5500 qtrap by AB Sciex
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Mgcl2 by Thermo Fisher Scientific
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Magnesium chloride (MgCl2) is an inorganic compound that is commonly used in laboratory settings. It is a white, crystalline solid that is soluble in water and other polar solvents. Magnesium chloride is a versatile compound that can be used in various applications, including as a desiccant, a coagulant, and a source of magnesium ions.

More about "Afimoxifene"

Afimoxifene, also known as 4-Hydroxytamoxifen or Metabolite of Tamoxifen, is a selective estrogen receptor modulator (SERM) that has been studied extensively for the treatment of certain types of breast cancer.
As a SERM, Afimoxifene binds to and modulates the activity of estrogen receptors, effectively inhibiting the growth of estrogen-dependent tumors.
Afimoxifene is closely related to other well-known SERMs, such as Toremifene and Tamoxifen, which have also been used in the management of breast cancer.
These compounds share a similar mechanism of action, but may have subtle differences in their pharmacokinetic properties and clinical efficacy.
In the research and development of Afimoxifene, various analytical techniques and tools have been employed.
For example, high-performance liquid chromatography (HPLC) utilizing an XBridge C18 column and a Milli-Q water system has been used to separate and quantify Afimoxifene and its metabolites.
Additionally, mass spectrometry techniques, like the ABI-5500 Qtrap, have been utilized to identify and characterize the chemical structure of Afimoxifene.
The optimization of Afimoxifene research protocols is an area of ongoing interest.
Researchers have explored the use of buffer systems, such as HEPES, as well as the inclusion of protease inhibitors, like Pepstatin A, to ensure the stability and integrity of Afimoxifene during experimental procedures.
Furthermore, the use of Luria broth for cell culture and the manipulation of magnesium chloride (MgCl2) concentrations have been investigated to enhance the efficacy and reproducibility of Afimoxifene-related studies.
While Afimoxifene has shown promise in clinical trials for the treatment of estrogen receptor-positive breast cancer, further research is needed to fully understand its optimal use and long-term efficacy in clinical practice.
The insights gained from the continued exploration of Afimoxifene and related compounds can contribute to the development of more effective and personalized breast cancer therapies.