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Ferrozoles: Ferrocenyl derivatives of letrozole with dual effects as potent aromatase inhibitors and cytostatic agents
In the treatment of hormone-dependent cancers, aromatase inhibitors (AI) are receiving increased attention due to some undesirable effects such as...
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SERPINA3-ANKRD11-HDAC3 pathway induced aromatase inhibitor resistance in breast cancer can be reversed by HDAC3 inhibition
Endocrine resistance is a major challenge for breast cancer therapy. To identify the genes pivotal for endocrine-resistance progression, we screened...
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Real-World Effectiveness of Denosumab and Bisphosphonates on Risk of Vertebral Fractures in Women with Breast Cancer Undergoing Treatment with Aromatase Inhibitors
Bone-active drugs are recommended to protect the skeleton from detrimental actions of aromatase inhibitors (AIs). However, most of literature data...
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Regulation of aromatase in cancer
The regulation of aromatase, an enzyme involved in the biosynthesis of estrogen in normal and cancer cells, has been associated with growth factor...
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Type I IFN stimulates IFI16-mediated aromatase expression in adipocytes that promotes E2-dependent growth of ER-positive breast cancer
Although type I interferons (IFNs) play multifaceted roles during tumorigenesis and cancer treatment, the interplay between type I IFNs and estrogen...
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FSIP1 enhances the therapeutic sensitivity to CDK4/6 inhibitors in triple-negative breast cancer patients by activating the Nanog pathway
CDK4/6 inhibitors are routinely recommended agents for the treatment of advanced HR + HER2 − breast cancer. However, their therapeutic effectiveness in...
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Virtual screening for potential discoidin domain receptor 1 (DDR1) inhibitors based on structural assessment
Discoidin domain receptor 1 (DDR1) (EC Number 2.7.10.1) has recently been considered as a promising therapeutic target for idiopathic pulmonary...
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Aging is associated with sex-specific alteration in the expression of genes encoding for neuroestradiol synthesis and signaling proteins in the mouse trigeminal somatosensory input
Pain perception is influenced by sex and aging, with previous studies indicating the involvement of aromatase, the estradiol synthase enzyme, in...
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Anti-masculinization induced by aromatase inhibitors in adult female zebrafish
BackgroundEarly sex differentiation genes of zebrafish remain an unsolved mystery due to the difficulty to distinguish the sex of juvenile zebrafish....
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In silico analysis of nsSNPs in CYP19A1 gene affecting breast cancer associated aromatase enzyme
The human aromatase protein encoded by CYP19A1 gene is the principle enzyme involved in the biogenesis of oestrogen in adipose tissues. An excessive...
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Alterations in PTEN and ESR1 promote clinical resistance to alpelisib plus aromatase inhibitors
Alpelisib is a selective inhibitor of phosphoinositide 3-kinase (PI3K)α, shown to improve outcomes for PIK3CA -mutant, hormone receptor–positive...
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Identification of bicyclic compounds that act as dual inhibitors of Bcl-2 and Mcl-1
Elevated expression of anti-apoptotic proteins, such as Bcl-2 and Mcl-1 contributes to poor prognosis and resistance to current treatment modalities...
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An in-silico scaffold- hop** approach to design novel inhibitors against gp130: A potential therapeutic application in cancer and Covid-19
An upregulation of the gp130-signalling cascade has been reported in multiple cancers, making gp130 an attractive target for the development of...
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The present and future of PI3K inhibitors for cancer therapy
Phosphoinositide 3-kinase (PI3K) signaling regulates cellular proliferation, survival and metabolism, and its aberrant activation is one of the most...
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Single-cell morphological and transcriptome analysis unveil inhibitors of polyploid giant breast cancer cells in vitro
Considerable evidence suggests that breast cancer therapeutic resistance and relapse can be driven by polyploid giant cancer cells (PGCCs). The...
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Steroidal ferrocenes as potential enzyme inhibitors of the estrogen biosynthesis
The potential inhibitory effect of diverse triazolyl-ferrocene steroids on key enzymes of the estrogen biosynthesis was investigated. Test compounds...
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Fungal aromatic-bisabolane sesquiterpenoids—possible peptidylprolyl cis/trans isomerase (Pin1) inhibitors for cancer
Marine fungi have been proven as potential sources of natural metabolites with significant bioactivities that have not been sufficiently explored....
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Diacylhydrazine Derivatives of 2-(5-(Pyridin-3-yl)-2H-Tetrazol-2-yl)Acetohydrazide and 2-(5-(Pyridin-4-yl)-2H-Tetrazol-2-yl)Acetohydrazide as Potential Inhibitors of Nucleotide Pyrophosphatase
AbstractNucleotide Pyrophosphatases (NPPs) i.e. NPP1 and 3 are responsible for maintaining the extracellular level of nucleotides and nucleosides and...
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Mechanisms of resistance to cyclin-dependent kinase 4/6 inhibitors
Cyclin-dependent kinase (CDK) 4/6 inhibitors have emerged in the treatment of metastatic hormone receptor (HR)-positive and human epidermal growth...
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ATAC-seq and RNA-seq analysis unravel the mechanism of sex differentiation and infertility in sex reversal chicken
BackgroundSex determination and differentiation are complex and delicate processes. In female chickens, the process of sex differentiation is...
