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Drug: Tamoxifen
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Small Change - Big Consequence: The Impact of C15-C16 Double Bond in a D ‑ring of Estrone on Estrogen Receptor Activity
In conclusion, the combination of computational and experimental methods shown here represents a rapid approach to determine the activity of compounds towards ER. Our data will not only contribute to research focused on the regulation of ER activity but may also be useful for the further development of novel steroid receptor-targeted drugs applicable in clinical practice.PMID:37468002 | DOI:10.1016/j.jsbmb.2023.106365
Source: Mol Biol Cell - July 19, 2023 Category: Molecular Biology Authors: Petr Vonka Lucie Rarova Vaclav Bazgier Vlastimil Tichy Tamara Kolarova Jitka Holcakova Karel Berka Miroslav Kvasnica Jana Oklestkova Eva Kudova Miroslav Strnad Roman Hrstka Source Type: research
LncRNA AGPG confers endocrine resistance in breast cancer by promoting E2F1 activity
Cancer Res. 2023 Jul 18:CAN-23-0015. doi: 10.1158/0008-5472.CAN-23-0015. Online ahead of print.ABSTRACTResistance to endocrine therapy represents a major concern for patients with estrogen receptor α positive (ERα+) breast cancer. Endocrine therapy resistance is commonly mediated by activated E2F signaling. A better understanding of the mechanisms governing E2F1 activity in resistant cells could reveal strategies for overcoming resistance. Here, we identified the long non-coding RNA (lncRNA) actin gamma 1 pseudogene 25 (AGPG) as a regulator of E2F1 activity in endocrine resistant breast cancer. Expression of EGPG was inc...
Source: Cell Research - July 18, 2023 Category: Cytology Authors: Shiyi Yu Ying Wang Xue Gong Zhehao Fan Zheng Wang Zhengyan Liang Rui Wu Binjie Cao Ning Wang Caili Bi Dan Lv Haibo Sun Source Type: research
Design, synthesis and biological evaluation of a novel bioactive indane scaffold 2-(diphenylmethylene)c-2,3-dihydro-1H-inden-1-one with potential anticancer activity
Eur J Pharm Sci. 2023 Jul 17;188:106529. doi: 10.1016/j.ejps.2023.106529. Online ahead of print.ABSTRACTOver the past decades, designing of privileged structures has emerged as a useful approach to the discovery and optimisation of novel biologically active molecules, and many have been successfully exploited across and within different target families. Examples include indole, quinolone, isoquinoline, benzofuran and chromone, etc. In the current study, we focus on synthesising a novel hybrid scaffold constituting naturally occurring benzophenone (14) and indanone (22) ring systems, leading to a general structure of 2-(dip...
Source: European Journal of Pharmaceutical Sciences - July 17, 2023 Category: Drugs & Pharmacology Authors: Tao Zhang Vilmar Bandero Claire Corcoran Ismael Obaidi Manuel Ruether John O'Brien Lorraine O'Driscoll Neil Frankish Helen Sheridan Source Type: research
Nuclear PRMT5 is a biomarker of sensitivity to tamoxifen in ER α < sup > + < /sup > breast cancer
EMBO Mol Med. 2023 Jul 17:e17248. doi: 10.15252/emmm.202217248. Online ahead of print.ABSTRACTEndocrine therapies targeting estrogen signaling, such as tamoxifen, have significantly improved management of estrogen receptor alpha (ERα)-positive breast cancers. However, their efficacy is limited by intrinsic and acquired resistance to treatment, and there is currently no predictive marker of response to these anti-estrogens to guide treatment decision. Here, using two independent cohorts of breast cancer patients, we identified nuclear PRMT5 expression as an independent predictive marker of sensitivity to tamoxifen. Mechani...
Source: Molecular Medicine - July 17, 2023 Category: Molecular Biology Authors: Coralie Poulard Thuy Ha Pham Youenn Drouet Julien Jacquemetton Ausra Surmielova Loay Kassem Benoite Mery Christine Lasset Jonathan Reboulet Isabelle Treilleux Elisabetta Marangoni Olivier Tr édan Muriel Le Romancer Source Type: research
Design, Synthesis and Biological Evaluation of a Novel Bioactive Indane Scaffold 2-(diphenylmethylene)c-2,3-dihydro-1H-inden-1-one with Potential Anticancer Activity
Eur J Pharm Sci. 2023 Jul 15:106529. doi: 10.1016/j.ejps.2023.106529. Online ahead of print.ABSTRACTOver the past decades, designing of privileged structures has emerged as a useful approach to the discovery and optimisation of novel biologically active molecules, and many have been successfully exploited across and within different target families. Examples include indole, quinolone, isoquinoline, benzofuran and chromone, etc. In the current study, we focus on synthesising a novel hybrid scaffold constituting naturally occurring benzophenone (14) and indanone (22) ring systems, leading to a general structure of 2-(dipheny...
Source: European Journal of Pharmaceutical Sciences - July 17, 2023 Category: Drugs & Pharmacology Authors: Tao Zhang Vilmar Bandero Claire Corcoran Ismael Obaidi Manuel Ruether John O'Brien Lorraine O'Driscoll Neil Frankish Helen Sheridan Source Type: research
Nuclear PRMT5 is a biomarker of sensitivity to tamoxifen in ER α < sup > + < /sup > breast cancer
EMBO Mol Med. 2023 Jul 17:e17248. doi: 10.15252/emmm.202217248. Online ahead of print.ABSTRACTEndocrine therapies targeting estrogen signaling, such as tamoxifen, have significantly improved management of estrogen receptor alpha (ERα)-positive breast cancers. However, their efficacy is limited by intrinsic and acquired resistance to treatment, and there is currently no predictive marker of response to these anti-estrogens to guide treatment decision. Here, using two independent cohorts of breast cancer patients, we identified nuclear PRMT5 expression as an independent predictive marker of sensitivity to tamoxifen. Mechani...
Source: Molecular Medicine - July 17, 2023 Category: Molecular Biology Authors: Coralie Poulard Thuy Ha Pham Youenn Drouet Julien Jacquemetton Ausra Surmielova Loay Kassem Benoite Mery Christine Lasset Jonathan Reboulet Isabelle Treilleux Elisabetta Marangoni Olivier Tr édan Muriel Le Romancer Source Type: research
Comparative anticancer effects of Annona muricata Linn (Annonaceae) leaves and fruits on DMBA-induced breast cancer in female rats
CONCLUSION: These results confirm the anti-breast cancer effect of A. muricata, however, the aqueous fruit extract was more potent than the ethanolic leaves extract.PMID:37454062 | DOI:10.1186/s12906-023-04073-x
Source: Cancer Control - July 15, 2023 Category: Cancer & Oncology Authors: Kevine Kamga Silihe William Defo Mbou Judith Christiane Ngo Pambe Larissa Vanelle Kenmogne Laure Fotso Maptouom Marius Tr ésor Kemegne Sipping St éphane Zingue Dieudonn é Njamen Source Type: research
Smarca2 genetic ablation is phenotypically benign in a safety assessment of tamoxifen-inducible conditional knockout rats
Toxicol Appl Pharmacol. 2023 Jul 13:116627. doi: 10.1016/j.taap.2023.116627. Online ahead of print.ABSTRACTSMARCA2 and SMARCA4 are the ATPases of the SWI/SNF chromatin remodeling complex, which play a significant role in regulating transcriptional activity and DNA repair in cells. SMARCA2 has become an appealing synthetic-lethal, therapeutic target in oncology, as mutational loss of SMARCA4 in many cancers leads to a functional dependency on residual SMARCA2 activity. Thus, for therapeutic development, an important step is understanding any potential safety target-associated liabilities of SMARCA2 inhibition. To best mimic...
Source: Toxicology and Applied Pharmacology - July 15, 2023 Category: Toxicology Authors: Jonathan Maher Nicola Stagg Gary Cain Roxanne Andaya Paula Katavolos Fermin Gallardo-Chang Anna Pham Xiaofen Ye Tom Januario Tuija Alcantar Roger Caothien Merone Roose-Girma Donglu Zhang Ruina Li Shu Chen Robert L Yauch Source Type: research
