A new structural type of kinase inhibitor, containing a benzocarbazole nucleus, has been identified. Members of the series are selective for inhibition of the cyclin dependent kinase family of enzymes. Although the cdks are highly homologous, representatives of the series showed intra-cdk selectivities, especially for cdk4. SAR studies elucidated the important features of the molecules for inhibition.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/s0960-894x(01)00416-4 | DOI Listing |
Proc Natl Acad Sci U S A
January 2025
Beijing Key Laboratory of Growth and Developmental Regulation for Protected Vegetable Crops, College of Horticulture, China Agricultural University, Beijing 100193, China.
Light serves as an energy source for cell division and expansion during fruit development. Cell expansion significantly influences fruit size and is closely linked to endoreduplication, a unique cell cycle variation characterized by DNA replication without cytokinesis. Paradoxically, under conditions of ample photosynthates, light signaling suppresses cell expansion.
View Article and Find Full Text PDFMol Divers
January 2025
School of Applied Material Sciences, Central University of Gujarat, Gandhinagar, Gujarat, India.
Cancer, a leading global cause of death, presents considerable treatment challenges due to resistance to conventional therapies like chemotherapy and radiotherapy. Cyclin-dependent kinase 11 (CDK11), which plays a pivotal role in cell cycle regulation and transcription, is overexpressed in various cancers and is linked to poor prognosis. This study focused on identifying potential inhibitors of CDK11 using computational drug discovery methods.
View Article and Find Full Text PDFExp Dermatol
January 2025
Department of Dermatology, Ajou University School of Medicine; Suwon, Suwon, Korea.
Senescent melanocytes have been suggested to play a role in the development of ageing-associated pigmentary changes and skin ageing. Here, we assessed the senolytic capacity of recognised senolytic chemicals and natural compounds in UV-irradiated senescent melanocytes. Among the tested agents, only ABT-737 and ABT-263 showed a significant reduction in the number of SA-β-Gal-positive senescent melanocytes and in the expressions of p16 and p21.
View Article and Find Full Text PDFJ Oncol Pharm Pract
January 2025
Department of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, 576104, Karnataka, India.
Introduction: The utilization of CDK4/6 inhibitors has led to compromised survival rates for breast cancer patients. Consequently, certain treatment aspects, involving adherence and drug-to-drug interactions, are gaining prominence. To develop chemotherapy regimens that are both effective and efficient, our main objective was to thoroughly characterize the drug-drug interactions that occur between cyclin-dependent kinase inhibitors and concurrently prescribed medications in hospitalized breast cancer patients.
View Article and Find Full Text PDFZool Res
January 2025
State Key Laboratory of Reproductive Regulation and Breeding of Grassland Livestock (R2BGL), Inner Mongolia University, Hohhot, Inner Mongolia 010070, China.
Somatic cell nuclear transfer (SCNT) has been successfully employed across various mammalian species, yet cloned animals consistently exhibit low pregnancy rates, primarily due to placental abnormalities such as hyperplasia and hypertrophy. This study investigated the involvement of the Hippo signaling pathway in aberrant placental development in SCNT-induced bovine pregnancies. SCNT-derived cattle exhibited placental hypertrophy, including enlarged abdominal circumference and altered placental cotyledon morphology.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!