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acrylic acid/kanker payudara
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Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer.
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Tetrahydroisoquinoline 40 has been identified as a potent ERα antagonist and selective estrogen receptor degrader (SERD), exhibiting good oral bioavailability, antitumor efficacy, and SERD activity in vivo. We outline the discovery and chemical optimization of the THIQ scaffold leading to THIQ 40
In vitro detection of human breast cancer cells (SK-BR3) using herceptin-conjugated liquid crystal microdroplets as a sensing platform.
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The present study utilizes antibody-protein interactions to develop an LC microdroplet based biosensor for naked eye detection of SK-BR3 human breast cancer cells. The herceptin antibody-conjugated LC microdroplets were fabricated using 4-cyano-4'-pentyl biphenyl (5CB) as the liquid crystalline
Adamantyl Antiestrogens with Novel Side Chains Reveal a Spectrum of Activities in Suppressing Estrogen Receptor Mediated Activities in Breast Cancer Cells.
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To search for new antiestrogens more effective in treating breast cancers, we explored alternatives to the acrylic acid side chain used in many antiestrogens. To facilitate our search, we used a simple adamantyl ligand core that by avoiding stereochemical issues enabled rapid synthesis of acrylate
Oral administration of highly bright Cr3+ doped ZnGa2O4 nanocrystals for in vivo targeted imaging of orthotopic breast cancer.
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Near-infrared (NIR) long lasting persistent luminescence nanoparticles (PLNPs) have attracted considerable attention in the area of in vivo bioimaging, due to their background-free luminescence characteristics and deep tissue penetration. However, the low fluorescence quantum yield and short
Novel poly(ethylene-co-acrylic acid) nanofibrous biomaterials for peptide synthesis and biomedical applications.
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Poly(ethylene-co-acrylic acid) (PE-co-AA) fibers in sizes of 200-500 nm were prepared by using a novel melt-extrusion-extraction fabrication process. The thermoplastic nanofibers could be controllably dispersed and reassembled by a novel solvent exchange filtration method. The dispersed PE-co-AA
Nanopatterned polystyrene-b-poly(acrylic acid) surfaces to modulate cell-material interaction.
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In this work we explore the effect of surface nanoarchitecture of polystyrene (PS) and polystyrene-b-poly(acrylic acid) (PS-b-PAA) diblock copolymer films on cell viability. PS and PS-b-PAA have been nanopatterned at temperatures of 110, 120 and 140°C using nanoporous aluminium oxide membranes (AAO)
Estrone decorated poly-ion complex micelles for targeted melittin delivery to hormone responsive breast cancer cells.
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Tumor targeting has revolutionized cancer research, especially active cellular targeting of nanoparticles where they are specifically homed to pathological site to deliver the therapeutics. This strategy which involves the utilization of affinity ligands on the surface of the nano-carriers minimizes
Anti-breast cancer potential of SS5020, a novel benzopyran antiestrogen.
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Treatment with tamoxifen (TAM) increases the risk of developing endometrial cancer in women. The carcinogenic effect is thought to involve initiation and/or promotion resulting from DNA damage induced by TAM as well as its estrogenic action. To minimize this serious side-effect while increasing the
Anti-breast cancer potential of SS1020, a novel antiestrogen lacking estrogenic and genotoxic actions.
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Long-term treatment with tamoxifen (TAM) increases the risk of developing endometrial cancer in women. Several antiestrogens developed in last decades have been discontinued from clinical testing because of their undesirable effects on the uterus. To avoid such serious side-effect while increasing
Chemotherapy of Breast Cancer Cells Using Novel pH-Responsive Cellulose-Based Nanocomposites.
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Purpose: The objective of the current study was to compare the anticancer efficacy of doxorubicin-loaded cellulose based magnetic (Fe3O4), zinc oxide (ZnO) nanoparticles on and free doxorubicin (DOX) on MCF-7 breast cancer cells. Methods: Novel pH-sensitive
Sensitizing basal-like breast cancer to chemotherapy using nanoparticles conjugated with interference peptide.
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Basal-like breast cancers are highly aggressive malignancies associated with very poor prognosis. Although these cancers may initially respond to first-line treatment, they become highly resistant to standard chemotherapy in the metastatic setting. Chemotherapy resistance in basal-like breast
Modeling a pH-sensitive Zein-co-acrylic acid hybrid hydrogels loaded 5-fluorouracil and rutin for enhanced anticancer efficacy by oral delivery.
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The combination of natural and synthetic polymeric materials grafted hydrogels offer great potential as oral therapeutic systems because of its intrinsic biocompatibility, biodegradability, protect labile drugs from metabolism and controlled release properties. Hence, in the present study, we aimed
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.
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The discovery of an orally bioavailable selective estrogen receptor downregulator (SERD) with equivalent potency and preclinical pharmacology to the intramuscular SERD fulvestrant is described. A directed screen identified the 1-aryl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole motif as a novel,
Additive Polyplexes to Undertake siRNA Therapy against CDC20 and Survivin in Breast Cancer Cells.
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Small interfering RNA (siRNA) delivered to silence overexpressed genes associated with malignancies is a promising targeted therapy to decrease the uncontrolled growth of malignant cells. To create potent delivery agents for siRNA, here we formulated additive polyplexes of siRNA using linoleic
Characterization of molecular and structural determinants of selective estrogen receptor downregulators.
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Antiestrogens used for breast cancer therapy can be categorized into two classes that differ in their effect on estrogen receptor (ER) alpha stability. The selective estrogen receptor modulators (SERMs) stabilize ER alpha and the selective estrogen receptor downregulators (SERDs) cause a decrease in
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