Uterine leiomyomas (fibroids) are a major public health problem. Current medical treatments with GnRH analogs do not provide long-term benefit. Thus, permanent shrinkage or inhibition of fibroid growth via medical means remains a challenge. The AKT pathway is a major growth and survival pathway for fibroids. We propose that AKT inhibition results in a transient regulation of specific mechanisms that ultimately drive cells into cellular senescence or cell death. In this study, we investigated specific mechanisms of AKT inhibition that resulted in senescence. We observed that administration of MK-2206, an allosteric AKT inhibitor, increased levels of reactive oxygen species, up-regulated the microRNA miR-182 and several senescence-associated genes (including p16, p53, p21, and β-galactosidase), and drove leiomyoma cells into stress-induced premature senescence (SIPS). Moreover, induction of SIPS was mediated by HMGA2, which colocalized to senescence-associated heterochromatin foci. This study provides a conceivable molecular mechanism of SIPS by AKT inhibition in fibroids.
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http://dx.doi.org/10.1210/en.2013-1929 | DOI Listing |
Mol Divers
December 2024
Small-Molecule Drug Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai, 201203, People's Republic of China.
Overexpressed AXL kinase is involved in various human malignancies, which incurs tumor progression, poor prognosis, and drug resistance. Suppression of the aberrant AXL axis with genetic tools or small-molecule inhibitors has achieved valid antitumor efficacies in both preclinical studies and clinical antitumor campaigns. Herein we will report the design, synthesis, and structure-activity relationship (SAR) exploration of a series of anilinopyrimidine type II AXL inhibitors.
View Article and Find Full Text PDFJ Biomol Struct Dyn
December 2024
School of Pharmacy and Life Sciences, Centurion University of Technology and Management, Bhubaneswar, India.
Glimepiride (GLM) is one of the potential antidiabetic drugs used in clinics for a long time. It is currently used in combination with metformin along with other drugs, but has shown various complications in patients from long-term use. Thus, the hypothesis is to use a lower dose of GLM with a non-toxic class of flavonoid, naringin (NARN), for better therapy with minimal side-effects.
View Article and Find Full Text PDFJ Med Food
December 2024
Division of Food and Nutrition and Human Ecology Research Institute, Chonnam National University, Gwangju, Republic of Korea.
Here, we investigated whether a mixture of and (1:3, KGC01CE) could suppress muscle atrophy in HO-induced C2C12 cells and dexamethasone-injected mice. Our results revealed that KGC01CE effectively safeguarded against HO-induced muscle atrophy in C2C12 cells compared with the same mixture at other ratios. We demonstrated that dexamethasone elicited oxidative stress in muscle tissue and decreased the grip strength and cross-sectional areas of muscle fibers; however, oral administration of KGC01CE (1:3) suppressed these dexamethasone-induced changes.
View Article and Find Full Text PDFLipids Health Dis
December 2024
Department of Hepatobiliary Surgery, The Fifth Affiliated Hospital of Sun Yat-sen University, Zhuhai, Guangdong, 519000, People's Republic of China.
Background: There is still no reliable therapeutic targets and effective pharmacotherapy for metabolic dysfunction-associated steatotic liver disease (MASLD). RASD1 is short for Ras-related dexamethasone-induced 1, a pivotal factor in various metabolism processes of Human. However, the role of RASD1 remains poorly illustrated in MASLD.
View Article and Find Full Text PDFSci Rep
December 2024
School of Medicine, Cardiff University, Henry Wellcome Building, Cardiff, CF14 4XN, UK.
Most pancreatic cancer patients are diagnosed at advanced stages, with poor survival rates and drug resistance making pancreatic cancer one of the highest causes of cancer death in the UK. Understanding the underlying mechanism behind its carcinogenesis, metastasis and drug resistance has become an essential task for researchers. We have discovered that a well-established tumour suppressor, EPLIN, has an oncogenic rather than suppressive role in pancreatic cancer.
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