Aromatase is an enzyme that plays a crucial role in the biosynthesis of estrogens, which are hormones that contribute to the growth of certain types of breast cancer. In particular, aromatase catalyzes the conversion of androgens (male hormones) into estrogens (female hormones) in various tissues, including the adrenal glands, ovaries, and adipose tissue. Given the role of estrogen in promoting the growth of hormone-receptor-positive breast cancers, aromatase has become an important molecular target for the development of anticancer agents. Aromatase inhibitors can be classified into two main groups based on their chemical structure: steroidal and non-steroidal inhibitors. This work presents a review of the literature from the last ten years regarding the search for new aromatase inhibitors. We present the directions of search, taking into account the impact of structure modifications on anticancer activity.
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http://dx.doi.org/10.3390/molecules29020346 | DOI Listing |
Contemp Clin Trials
December 2024
Department of Medical Social Sciences, Northwestern University Feinberg School of Medicine, Chicago, IL, United States of America; Robert H. Lurie Comprehensive Cancer Center of Northwestern University, Chicago, IL, United States of America. Electronic address:
Background: Aromatase inhibitors (AIs) are a cornerstone of adjuvant systemic therapy for postmenopausal patients with hormone-receptor positive (HR+) breast cancer. Although AIs decrease cancer recurrence rates and improve survival rates, approximately 50 % of patients experience arthralgia-persistent pain related to worse patient outcomes and poor AI adherence. Current medical interventions for AI-associated arthralgia have limited efficacy and side effects that restrict their use among older patients.
View Article and Find Full Text PDFZhongguo Zhong Yao Za Zhi
October 2024
School of Pharmacy, Shandong University of Traditional Chinese Medicine Ji'nan 250355, China State Key Laboratory of Integration and Innovation of Classic Formula and Modern Chinese Medicine, Lunan Pharmaceutical Group Co., Ltd. Linyi 273400, China.
This study aims to explore the therapeutic effect of Yuzhi Zhixue Granules on polycystic ovary syndrome(PCOS) in rats and explain the underlying mechanism by metabolomics. Rats were randomized into normal, model, low-, medium-, and high-dose(0.5, 1.
View Article and Find Full Text PDFBMC Pediatr
December 2024
Jinhua Maternity and Child Health Care Hospital, Jinhua Women and Children's Hospital, Jinhua, 322199, China.
Whether the addition of aromatase inhibitors (AIs) to recombinant human growth hormone (rhGH) could yield additional benefit for short stature is controversial. We aimed to assess the effects of combined AIs and rhGH versus those of rhGH alone for short stature using a meta-analytic approach. The PubMed, Embase, and the Cochrane library electronic databases were searched systematically for eligible randomized controlled trials (RCTs) from inception until December 2021.
View Article and Find Full Text PDFJ Clin Oncol
December 2024
Massachusetts General Hospital, Harvard University, Boston, MA, USA.
Purpose: Cyclin-dependent kinase 4/6 inhibitors (CDK4/6i) combined with endocrine therapy (ET) are the standard first-line treatment for hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced breast cancer (ABC); however, disease progression occurs in almost all patients and additional treatment options are needed. Herein we report outcomes of the postMONARCH trial investigating a switch in ET with/without CDK4/6 inhibition with abemaciclib after disease progression on CDK4/6i.
Methods: This double-blind, randomized Phase III study enrolled patients with disease progression on prior CDK4/6i plus aromatase inhibitor as initial therapy for advanced disease or recurrence on/after adjuvant CDK4/6i+ET.
J Cachexia Sarcopenia Muscle
December 2024
Department of Internal Medicine, Division of Medical Oncology, Yonsei Cancer Center, Yonsei University College of Medicine, Seoul, South Korea.
Background: Recent evidence indicates that a dysregulated host metabolism influences treatment outcomes in patients with breast cancer. We investigated the association of computed tomography (CT)-derived body composition indices with therapeutic responses in patients with hormone receptor-positive, HER2-negative advanced breast cancer (ABC) on endocrine plus CDK4/6 inhibitor (CDK4/6i) treatment.
Methods: The study involved a retrospective cohort of patients with ABC at the Yonsei Cancer Center who received CDK4/6i and aromatase inhibitors as first-line therapy between January 2017 and October 2020.
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