Results 91 to 100 of about 16,673,842 (253)

Insight into Janus kinases specificity: From molecular architecture to cancer therapeutics

MedComm – Oncology
Janus Kinases (JAKs) play a crucial role as therapeutic targets for various cancers. However, the current JAK inhibitors (JAKi) available have limited therapeutic benefits due to their lack of selectivity.
Tian‐Hua Wei, Meng‐Yi Lu, Si‐Hui Yao, Yu‐Qi Hong, Jin Yang, Meng‐Yuan Zhang, Yu‐Qi Yin, Yu‐Jie Han, Qing‐Qing Li, Zi‐Xuan Wang, Yi‐Bo Wang, Zhen‐Jiang Tong, Yun Zhou, Wei‐Chen Dai, Yan‐Cheng Yu, Shan‐Liang Sun, Ye Yang, Nian‐Guang Li, Zhi‐Hao Shi   +18 more
doaj   +1 more source

Novel indole-based synthetic molecules in cancer treatment: Synthetic strategies and structure-activity relationship

Medicine in Drug Discovery
Indole is one of the naturally occurring nitrogen-containing bicyclic heterocyclic ring systems where benzene and pyrrole rings are fused. It has been demonstrated to exhibit versatile biological activities.
Biplab Debnath, Bikram Nandi, Samiran Paul, Swarup Manna, Arindam Maity, Krishnalekha Bandyopadhyay, Shambo Panda, Shah Alam Khan, Rajarshi Nath, Md Jawaid Akhtar   +9 more
doaj   +1 more source

Epigenetic reprogramming of lineage switching in cancer

FEBS Letters, EarlyView.
Cancer cells rarely commit to a single identity. Epigenetic mechanisms and tumor microenvironment cues push epithelial cells toward flexible, hybrid states that can shift into mesenchymal, neuroendocrine, or stem‐like fates, driving metastasis, drug resistance, and tumor heterogeneity. Targeting the epigenetic regulators behind these transitions, using
Ezgi Boyvatlı, Burcu Akman, Ezgi Bağırsakçı, Nese Atabey, Serap Erkek‐Ozhan   +4 more
wiley   +1 more source

Synthesis and activity of novel indole derivatives as inhibitors of CD38

Acta Pharmaceutica Sinica B, 2013
CD38 is a multifunctional enzyme/receptor expressed in a variety of mammalian tissues, regulating a wide range of physiological functions. Beginning with the previously reported compound 1, an inhibitor of human CD38 NADase, we synthesized a series of ...
Dongying Wu, Kaiyiu Ting, Yaokai Duan, Na Li, Jianguo Li, Liangren Zhang, Honcheung Lee, Lihe Zhang   +7 more
doaj   +1 more source

Structure-activity relationship of karrikin germination stimulants

, 2010
Karrikins (2H-furo[2,3-c]pyran-2-ones) are potent smoke-derived germination promoters for a diverse range of plant species but, to date, their mode of action remains unknown.
R. Stick (23419942), L. Commander (23318893), G. Flematti (23315989), E. Goddard-Borger (23419939), E. Ghisalberti (23315992), Kingsley Dixon (23304052), C. Heath (23326114), A. Scaffidi (23316619), D. Nelson (7350899), S. Smith (2840546)   +9 more
core  

Autophagy and mitophagy in pancreatic β‐cell homeostasis and their involvement in diabetes pathophysiology

FEBS Letters, EarlyView.
This review focuses on the role of autophagy and mitophagy in maintaining pancreatic β‐cell function and homeostasis. We discuss how genetic defects affecting these pathways contribute to the development of type 1, type 2, monogenic, and gestational diabetes. We further explore their potential as therapeutic targets. Created in BioRender.
Yunkyeong Lee, Mingming Tong, Anna L. Gloyn   +2 more
wiley   +1 more source

Ligand‐dependent transcriptional heterogeneity in cell cycle gene expression delays G1/S entry

FEBS Letters, EarlyView.
EGF and HRG induce distinct G1/S progression programs in ErbB2‐amplified BT474 breast cancer cells. Despite activating the potent ErbB2–ErbB3 heterodimer, HRG does not accelerate cell‐cycle entry. Instead, EGF promotes earlier restriction‐point passage via ERK–FOS signaling, whereas HRG activates the AKT–MYC axis, driving transcriptional heterogeneity ...
Ririn Rahmala Febri, Ayaka Nagasato‐Ichikawa, Keita Iida, Shuhei Kimura, Akira Imamoto, Mariko Okada   +5 more
wiley   +1 more source

Synthesis, Biological Evaluation and Structure–Activity Relationship of Juglone Derived Naphthoquinones as Potential Antipsoriatic Agents

Biomolecules
Psoriasis is a chronic, immune-mediated inflammatory skin disease for which the development of structurally novel and accessible small-molecule candidates remains of considerable interest. In this study, a series of juglone-derived naphthoquinone analogs
Tong Bu, Zile Gong, Yudong Ma, Lixia Dai, Yuchao Ma, Xiaoyan Yu, Xiaorong Yang, Xiaolou Miao, Xiaofei Shang   +8 more
doaj   +1 more source

Structure-Activity and Lipophilicity Relationships of Selected Antibacterial Natural Flavones and Flavanones of Chilean Flora

Molecules, 2017
In this study, we tested eight naturally-occurring flavonoids—three flavanones and five flavones—for their possible antibacterial properties against four Gram-positive and four Gram-negative bacteria.
Javier Echeverría, Julia Opazo, Leonora Mendoza, Alejandro Urzúa, Marcela Wilkens   +4 more
doaj   +1 more source

Structure-activity relationships of the fluoroquinolones [PDF]

Antimicrobial Agents and Chemotherapy, 1989
D T, Chu, P B, Fernandes
openaire   +2 more sources