Article
Oncology
G. R. Hancock, K. S. Young, D. J. Hosfield, C. Joiner, E. A. Sullivan, Y. Yildiz, M. Laine, G. L. Greene, S. W. Fanning
Summary: This study identified chemically unconventional antagonists of estrogen receptor alpha (ERα) that have moderate effects on the transcriptional activities of breast cancer cells, exhibit anti-proliferative properties, and engage transcriptional pathways similar to selective estrogen receptor degraders.
Article
Oncology
Irina Jilishitz, Jason Luis Quinones, Priyank Patel, Grace Chen, Jared Pasetsky, Allison VanInwegen, Scott Schoninger, Manasi P. Jogalekar, Vladislav Tsiperson, Lingyue Yan, Yun Wu, Susan R. S. Gottesman, Jonathan Somma, Stacy W. Blain
Summary: Using NP-ALT as a therapeutic approach can effectively inhibit CDK4/6 and CDK2 by targeting the tyrosine phosphorylation of p27Kip1. This treatment shows efficacy in HR+ breast cancer cells, CDK4i-resistant cells, and can induce necroptosis, particularly in cells with an ER gain of function mutation.
MOLECULAR CANCER RESEARCH
(2021)
Article
Chemistry, Medicinal
Jiawang Liu, Nirmal Rajasekaran, Ahamed Hossain, Changde Zhang, Shanchun Guo, Borui Kang, Hunsoon Jung, Hongjoong Kim, Guangdi Wang
Summary: Fulvestrant-3-boronic acid (ZB716), an oral selective estrogen receptor degrader (SERD) under clinical development, has been investigated in ADME studies to characterize its absorption, metabolism, and pharmacokinetics. ZB716 exhibits high plasma protein binding and low intestinal mucosal permeability, with high clearance in hepatocytes and metabolism primarily by CYP2D6 and CYP3A. In enzyme activity assays, ZB716 induces certain cytochrome P450 enzymes in a concentration-dependent manner. Pharmacokinetic studies in rats and dogs demonstrate oral bioavailability and dose-proportional drug exposure, with drug accumulation as measured by maximum concentration and area under the concentration-time curve (AUC).
Article
Oncology
Gary Schwartz, Kevin Shee, Bianca Romo, Jonathan Marotti, Alexei Kisselev, Lionel Lewis, Todd Miller
Summary: A single-center phase Ib study showed that the combination of fulvestrant and the proteasome inhibitor ixazomib has a favorable safety profile and antitumor activity in patients with fulvestrant-resistant advanced ER+ breast cancer, warranting further testing.
Article
Oncology
Qian Liu, Yutao Shen, Yujia Xiong, Jiwei Bai, Yazhuo Zhang, Chuzhong Li
Summary: A study on gonadotropin-type pituitary adenoma tissue specimens and transcriptome-sequencing data revealed that low-level ESR1 expression was associated with longer progression-free survival in patients. The ErbB signaling pathway and STAT5B gene were found to be related to ESR1. The ER inhibitors AZD9496 and fulvestrant showed significant inhibitory effects on pituitary adenoma growth in vitro and in vivo, potentially through blocking the JAK2/STAT5B pathway.
Article
Medicine, General & Internal
Engin Kut, Serkan Menekse
Summary: This study retrospectively analyzed mHRPBC patients receiving fulvestrant in our center to evaluate its efficacy and clinical outcomes, and identify factors affecting its efficacy and clinical outcomes. The results showed that fulvestrant is effective in mHRPBC, particularly in patients with BMI under 30, without brain metastasis, without prior chemotherapy, under 65 years of age, and using fulvestrant in the early treatment line. The efficacy of fulvestrant may vary according to age and BMI.
CUREUS JOURNAL OF MEDICAL SCIENCE
(2023)
Article
Oncology
Kenichi Watanabe, Naoki Niikura, Yuichiro Kikawa, Mari Oba, Kokoro Kobayashi, Hiroshi Tada, Shinji Ozaki, Uhi Toh, Yutaka Yamamoto, Michiko Tsuneizumi, Toshitaka Okuno, Nobutaka Iwakuma, Takashi Takeshita, Takayuki Iwamoto, Hiroshi Ishiguro, Norikazu Masuda, Shigehira Saji
Summary: The combination of fulvestrant and palbociclib is a potentially safe and effective treatment option for patients with hormone receptor-positive/human epidermal growth factor receptor 2-negative metastatic breast cancer.
BREAST CANCER RESEARCH AND TREATMENT
(2023)
Article
Biochemistry & Molecular Biology
Dinh Nam Tran, Seon-Mi Park, Eui-Man Jung, Eui-Bae Jeung
Summary: Research has shown that offspring of mice exposed to D4 during pregnancy exhibited cognitive dysfunction and neurodevelopmental defects, possibly due to the effects of D4 on the cell cycle of neuronal progenitor cells.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Oncology
Tufia C. Haddad, Vera J. Suman, Antonino B. D'Assoro, Jodi M. Carter, Karthik V. Giridhar, Brendan P. McMenomy, Katelyn Santo, Erica L. Mayer, Meghan S. Karuturi, Aki Morikawa, P. Kelly Marcom, Claudine J. Isaacs, Sun Young Oh, Amy S. Clark, Ingrid A. Mayer, Khandan Keyomarsi, Timothy J. Hobday, Prema P. Peethambaram, Ciara C. O'Sullivan, Roberto A. Leon-Ferre, Minetta C. Liu, James N. Ingle, Matthew P. Goetz
Summary: This randomized clinical trial found that adding fulvestrant to treatment with alisertib did not increase objective tumor response rates (ORRs) or progression-free survival (PFS) in endocrine-resistant metastatic breast cancer (MBC).
Review
Endocrinology & Metabolism
Kaoru Sato, Ken-ichi Takayama, Satoshi Inoue
Summary: Estrogens play an important role in the female reproductive system and also regulate physiological processes associated with learning and memory in the brain. They have neuroprotective effects in the pathogenesis of Alzheimer's disease (AD), which has a higher incidence in older and postmenopausal women. Estrogens bind to estrogen receptors (ERs) and activate transcriptional machineries, and also stimulate signal transduction through membrane ERs (mERs). Estrogen-related receptors (ERRs), which lack estrogen-binding capabilities, are expressed in the human brain and implicated in AD pathogenesis.
FRONTIERS IN ENDOCRINOLOGY
(2023)
Review
Endocrinology & Metabolism
Xue-Ling Xu, Zheng-Yuan Huang, Kun Yu, Jun Li, Xiang-Wei Fu, Shou-Long Deng
Summary: This review focuses on the role of ER alpha and ER beta in polycystic ovary syndrome (PCOS), ovarian cancer, and premature ovarian failure (POF), as well as the major challenges of existing therapies. It provides a reference for the treatment of estrogen target tissue ovarian diseases.
FRONTIERS IN ENDOCRINOLOGY
(2022)
Review
Biochemistry & Molecular Biology
Kenta Yoh, Kazuhiro Ikeda, Kuniko Horie, Satoshi Inoue
Summary: Estrogen is an essential hormone that primarily functions in the female reproductive system and has pleiotropic effects in various tissues and organs. Low estrogen levels, such as in postmenopausal women, can lead to disorders like cardiovascular disease, dementia, metabolic syndrome, osteoporosis, sarcopenia, and frailty. Estrogen receptors (ERs) and estrogen-related receptors (ERRs) play crucial roles in muscle physiology, including muscle mass maintenance, exercise physiology, and regeneration, particularly in relation to mitochondrial function and metabolism.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Oncology
Kamrunnahar Shanta, Kentaro Nakayama, Mohammad Mahmud Hossain, Sultana Razia, Tomoka Ishibashi, Masako Ishikawa, Hitomi Yamashita, Kosuke Kanno, Seiya Sato, Satoru Nakayama, Yoshiro Otsuki, Satoru Kyo
Summary: This study investigated the hormone receptor expression and hormonal inhibition efficacy in low-grade serous ovarian carcinomas (LGSOCs). The results showed higher expression of estrogen receptor (ER) in LGSOCs and serous borderline tumors (SBTs). PIK3CA mutation was positively correlated with ER expression in LGSOCs. MPSC1 cell experiments demonstrated low ER expression and significant inhibition of cell proliferation by fulvestrant. ER downregulation and combination therapy with PI3K inhibitors may be a novel treatment approach for LGSOCs.
Article
Oncology
Taronish D. Dubash, Aditya Bardia, Brian Chirn, Brittany A. Reeves, Joseph A. LiCausi, Risa Burr, Ben S. Wittner, Sumit Rai, Hitisha Patel, Teeru Bihani, Heike Arlt, Francois-Clement Bidard, Virginia G. Kaklamani, Philippe Aftimos, Javier Cortes, Simona Scartoni, Alessio Fiascarelli, Monica Binaschi, Nassir Habboubi, A. John Iafrate, Mehmet Toner, Daniel A. Haber, Shyamala Maheswaran
Summary: This study compared the clinical outcomes of HR+ breast cancer patients who had received fulvestrant treatment with elacestrant and endocrine therapy. The results indicated that elacestrant had better efficacy than fulvestrant in patients with advanced cancers and diverse treatment histories. Patient-derived models were used to validate the sensitivity of elacestrant.
BREAST CANCER RESEARCH AND TREATMENT
(2023)
Review
Endocrinology & Metabolism
Kun Yu, Zheng-Yuan Huang, Xue-Ling Xu, Jun Li, Xiang-Wei Fu, Shou-Long Deng
Summary: This article discusses the role of estrogen in the female endometrium and its regulatory role through nuclear and membrane-associated receptors. The importance of ERs in maintaining endometrial function is emphasized, and references for treating endometrial diseases are provided.
FRONTIERS IN ENDOCRINOLOGY
(2022)
Article
Oncology
Su-Hyung Lee, Jun-Won Park, Du-Min Go, Hark Kyun Kim, Hyo-Jung Kwon, Sang-Uk Han, Dae-Yong Kim
Article
Medicine, Research & Experimental
Jun Won Park, Su Hyung Lee, Du Min Go, Hark Kyun Kim, Hyo-Jung Kwon, Dae-Yong Kim
LABORATORY INVESTIGATION
(2015)
Article
Pharmacology & Pharmacy
Ji-Won Song, Chang-Seob Seo, Tae-In Kim, Og-Sung Moon, Young-Suk Won, Hwa-Young Son, Jong-Keun Son, Hyo-Jung Kwon
BIOLOGICAL & PHARMACEUTICAL BULLETIN
(2016)
Article
Immunology
Ji-Won Song, Chang-Seob Seo, Eun-Sang Cho, Tae-In Kim, Young-Suk Won, Hyo-Jung Kwon, Jong-Keun Son, Hwa-Young Son
INTERNATIONAL IMMUNOPHARMACOLOGY
(2016)
Article
Pharmacology & Pharmacy
Young-Suk Won, Ji-Won Song, Jong-Hwan Lim, Mee-Young Lee, Og-Sung Moon, Hyoung-Chin Kim, Hwa-Young Son, Hyo-Jung Kwon
TOXICOLOGY AND APPLIED PHARMACOLOGY
(2016)
Article
Oncology
Su-Hyung Lee, Jun-Won Park, Sang-Ho Woo, Du-Min Go, Hyo-Jung Kwon, Ja-June Jang, Dae-Yong Kim
Article
Immunology
Charith U. B. Wijerathne, Chang-Seob Seo, Ji-Won Song, Hee-Seon Park, Og-Sung Moon, Young-Suk Won, Hyo-Jung Kwon, Hwa-Young Son
INTERNATIONAL IMMUNOPHARMACOLOGY
(2017)
Article
Fisheries
H. P. S. U. Chandrarathna, Chamilani Nikapitiya, S. H. S. Dananjaya, C. U. B. Wijerathne, S. H. M. P. Wimalasena, Hyo Jung Kwun, Gang-Joon Heo, Jehee Lee, Mahanama De Zoysa
FISH & SHELLFISH IMMUNOLOGY
(2018)
Article
Plant Sciences
Hee-Seon Park, Charith U. B. Wijerathne, Hye-Yun Jeong, Chang-Seob Seo, Hyekyung Ha, Hyo-Jung Kwun
JOURNAL OF ETHNOPHARMACOLOGY
(2018)
Article
Gastroenterology & Hepatology
Hyo-Jung Kwon, Young-Suk Won, Ogyi Park, Binxia Chang, Michael J. Duryee, Geoffrey E. Thiele, Akiko Matsumoto, Surendra Singh, Mohamed A. Abdelmegeed, Byoung-Joon Song, Toshihiro Kawamoto, Vasilis Vasiliou, Geoffrey M. Thiele, Bin Gao
Article
Pharmacology & Pharmacy
Hee-Seon Park, Chang-Seob Seo, Charith U. B. Wijerathne, Hye-Yun Jeong, Og-Sung Moon, Young-Won Seo, Young-Suk Won, Hwa-Young Son, Jong-Hwan Lim, Hyo-Jung Kwun
BIOLOGICAL & PHARMACEUTICAL BULLETIN
(2019)
Article
Plant Sciences
No Soo Kim, Sarah Shin, Hee-Seon Park, Hyo-Jung Kwon, Hwa-Young Son, Ok-Sun Bang
JOURNAL OF ETHNOPHARMACOLOGY
(2019)
Article
Plant Sciences
Jinhyung Rho, Chang-Seob Seo, Hee-Seon Park, Charith U. B. Wijerathne, Hye-Yun Jeong, Og-Sung Moon, Young-Won Seo, Hwa-Young Son, Young-Suk Won, Hyo-Jung Kwun
JOURNAL OF ETHNOPHARMACOLOGY
(2019)
Article
Pharmacology & Pharmacy
Charith U. B. Wijerathne, Hee-Seon Park, Hye-Yun Jeong, Ji-Won Song, Og-Sung Moon, Young-Won Seo, Young-Suk Won, Hwa-Young Son, Jong-Hwan Lim, Sung -Hum Yeon, Hyo-Jung Kwun
BIOLOGICAL & PHARMACEUTICAL BULLETIN
(2017)
Article
Biochemistry & Molecular Biology
Soojung Hahn, Gyuri Kim, Sang-Man Jin, Jae Hyeon Kim
Summary: This study utilized three-dimensional intestinal organoids to investigate the effects of metformin on inflammatory bowel disease (IBD) and found that metformin can enhance intestinal barrier function and reduce levels of inflammatory cytokines.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
V. V. Sudarev, M. S. Gette, S. V. Bazhenov, O. M. Tilinova, E. V. Zinovev, I. V. Manukhov, A. I. Kuklin, Yu. L. Ryzhykau, A. V. Vlasov
Summary: This study investigated the self-assembly processes of ferritin-based protein complexes and obtained structurally characterized oligomeric states. These results provide new potential and opportunities for the application of ferritin in various fields.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Yalda Sabaghi, Farnaz Pourfarzad, Leila Zolghadr, Azita Bahrami, Tahereh Shojazadeh, Alireza Farasat, Nematollah Gheibi
Summary: p-Coumaric acid (p-CA) is a plant compound with anti-cancer activities. This study designed a nano-liposomal carrier containing p-CA to enhance its effectiveness against melanoma cells. The findings showed that the liposomal form of p-CA had a greater impact on the cells. Kinetic modeling indicated that the best fitting model was zero-order.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
M. D. Nazmul Hasan, Md Mahfuzur Rahman, Al Asmaul Husna, Nobuhiro Nozaki, Osamu Yamato, Naoki Miura
Summary: This study investigated the expression of ncRNAs other than miRNAs in different histologic subtypes of canine mammary gland tumors (MGT). Three aberrantly expressed ncRNAs were identified as potential biomarkers for differentiating MGT subtypes. YRNA and tRFs expression levels were found to be decreased in metastatic compared to primary MGT cell lines.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Seine A. Shintani
Summary: In this study, the researchers used signal analysis to study the instantaneous amplitude and phase of sarcomeric oscillations in skeletal muscle. They identified two types of oscillations, sarcomeric oscillations and sarcosynced oscillations, and visualized their behavior during propagating waves. The researchers discovered the presence of sarcomeric defect holes and sarcomeric collision holes, which are important indicators for understanding the oscillation properties of sarcomeres. This finding has important implications for improving our understanding of muscle function and its regulatory mechanisms.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Shuanglin Zhang, Yuzhong Jia, Guolan Ma, Yanyan Yang, Zhenzhen Cao, Antao Luo, Zefu Zhang, Shihan Li, Jie Wen, Hanfeng Liu, Jihua Ma
Summary: Bupleurum is an antiarrhythmic agent that may exert its effects by inhibiting L-type calcium channels.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Tomotaka Ohkubo, Yasuhiko Matsumoto, Hiroaki Sasaki, Kaoru Kinoshita, Yuki Ogasawara, Takashi Sugita
Summary: This study found that Citrobacter koseri inhibits the growth of Staphylococcus epidermidis, disrupting the balance between S. epidermidis and Staphylococcus aureus, and exacerbating inflammation in atopic dermatitis.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Toshifumi Asano, Philipp Sasse, Takao Nakata
Summary: A Cre recombination-based fluorescent reporter system was developed to monitor cell-cell fusion. The system successfully detected the formation of multinuclear myotubes and placental syncytiotrophoblast. This tool could facilitate the study of cell-to-cell fusion.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Ke Shi, Yunlong Shan, Xiao Sun, Kuida Chen, Qiong Luo, Qiang Xu
Summary: This study found that low expression of TP53INP2 is associated with poor survival in colorectal cancer (CRC) patients. As the malignancy of CRC progresses, TP53INP2 expression gradually decreases. Knockdown of TP53INP2 promotes CRC cell proliferation and tumor growth. Mechanistically, TP53INP2 deficiency decreases phosphorylation of beta-catenin, leading to increased accumulation and enhanced nuclear translocation and transcriptional activity. Additionally, TP53INP2 sequesters TIM50, inhibiting its activation of beta-catenin. In conclusion, downregulation of TP53INP2 promotes CRC progression by activating beta-catenin.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Martina Rossi, Fabio Tomaselli, Alejandro Hochkoeppler
Summary: Oligomeric enzymes are known for their higher catalytic rates compared to monomeric enzymes, but the extent of additivity in their activity is still not well understood. This study used tetrameric rabbit lactate dehydrogenase as a model to examine the kinetics of its catalytic action. Surprisingly, when the concentration of the limiting reactant exceeded that of a single subunit, there was a significant slowdown in the enzyme's conformational rearrangements.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Amin Sahraei, Mohammad Javad Shamsoddini, Fakhrossadat Mohammadi, Leila Hassani
Summary: This study explored the inhibitory effects of gallium curcumin, indium curcumin, and vanadyl curcumin on the amyloid fibrillation of hen egg white lysozyme, as well as the binding interactions of these metal complexes with the enzyme. The results showed that indium curcumin and vanadyl curcumin exhibited higher binding affinities and stronger inhibitory effects on amyloid fibrillation compared to gallium curcumin.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Takahiro Sasaki, Yoshiki Kuse, Shinsuke Nakamura, Masamitsu Shimazawa
Summary: PGRN deficiency plays a significant role in cardiac remodeling and arrhythmias post-myocardial infarction (MI), potentially by promoting metabolic abnormalities in macrophages.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Hongwei Zhao, Yiqiang Li, Yibo Zhang, Chi Zhang
Summary: Electrical brain stimulation technology is commonly used to treat brain neurological disorders, but it can cause side effects. This study investigated the impact of electric fields on nerve fibers and revealed the possible origin of side effects. The findings provide guidance for selecting electrical parameters in clinical stimulation therapy.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Julia S. Scott, Lake-Ee Quek, Andrew J. Hoy, Johannes V. Swinnen, Zeyad D. Nassar, Lisa M. Butler
Summary: The fatty acid elongation enzyme ELOVL5 plays a critical role in promoting metastasis in prostate cancer. Knocking down ELOVL5 leads to the accumulation of malonyl-CoA, which inhibits fatty acid oxidation in mitochondria. This study highlights the importance of fatty acid elongation in regulating cell viability and provides a potential target for prostate cancer treatment.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Zan Zhou, Wen-jun Jiang, Li Li, Jun-qiang Si
Summary: This study investigates the effect of noise exposure on cognitive function in mice and explores the underlying molecular mechanisms. The findings suggest that noise exposure leads to increased inflammation, increased phosphorylation of Tau protein, and decreased levels of postsynaptic density protein, resulting in cognitive impairment.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)