Results 111 to 120 of about 4,906,436 (344)
Application of a macrocyclization strategy in kinase inhibitor development
Acta Materia MedicaKinases have a pivotal role in phosphorylation and kinase dysregulation has been implicated in the occurrence and progression of various diseases. By mid-2024 the Food and Drug Administration had approved 81 small-molecule kinase inhibitors targeting ...
Kun Xing +5 more
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Molecules, 2016 The success of the first approved kinase inhibitor imatinib has spurred great interest in the development of type II inhibitors targeting the inactive DFG-out conformation, wherein the Phe of the DFG motif at the start of the activation loop points into ...
Qingwen Zhang, Xuejin Zhang, Qidong You
doaj +1 more source
7-Azaindole: A Versatile Scaffold for Developing Kinase Inhibitors.
Chemical and pharmaceutical bulletin, 2018 The majority of kinase inhibitors have been developed as ATP competitors to interact with a hinge region in ATP binding sites of kinases. 7-Azaindole has been found as an excellent hinge binding motif by making two hydrogen bonds with the kinase hinge ...
T. Irie, M. Sawa
semanticscholar +1 more source
Updates on Kinase Inhibitors in Allergy
The Journal of Allergy and Clinical Immunology: In PracticeKinase inhibitors are emerging as transformative therapeutic agents in allergy. Advances in drug design have produced highly selective inhibitors with improved safety and efficacy, extending their clinical use beyond oncologic indications to the treatment of immune-mediated and hypersensitivity disorders. Bruton's tyrosine kinase inhibitors offer rapid,
Melanie C. Dispenza, Brian S. Kim
openaire +2 more sources
Molecular Oncology, EarlyView.Combining PTEN protein assessment and transcriptomic profiling of prostate tumors, we uncovered a network enriched in senescence and extracellular matrix (ECM) programs associated with PTEN loss and conserved in a mouse model. We show that PTEN‐deficient cells trigger paracrine remodeling of the surrounding stroma and this information could help ...
Ivana Rondon‐Lorefice +16 more
wiley +1 more source
Targeting kinases with anilinopyrimidines: Discovery of N-phenyl-N'-[4-(pyrimidin-4-ylamino)phenyl]urea derivatives as selective inhibitors of class III receptor tyrosine kinase subfamily [PDF]
, 2015 Kinase inhibitors are attractive drugs/drug candidates for the treatment of cancer. The most recent literature has highlighted the importance of multi target kinase inhibitors, although a correct balance between specificity and non-specificity is ...
Chilin, Adriana +5 more
core +2 more sources
PLoS ONEBackgroundThe role of upfront cytoreductive nephrectomy remains debatable in the present era of tyrosine kinase inhibitors and immune checkpoint inhibitors.
Gu-Shun Lai +8 more
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FDA-approved small-molecule kinase inhibitors.
TIPS - Trends in Pharmacological Sciences, 2015 Kinases have emerged as one of the most intensively pursued targets in current pharmacological research, especially for cancer, due to their critical roles in cellular signaling.
Peng Wu, T. Nielsen, M. Clausen
semanticscholar +1 more source
Potential therapeutic targeting of BKCa channels in glioblastoma treatment
Molecular Oncology, EarlyView.This review summarizes current insights into the role of BKCa and mitoBKCa channels in glioblastoma biology, their potential classification as oncochannels, and the emerging pharmacological strategies targeting these channels, emphasizing the translational challenges in developing BKCa‐directed therapies for glioblastoma treatment.
Kamila Maliszewska‐Olejniczak +4 more
wiley +1 more source
Chinese Journal of Lung Cancer, 2017 At present the treatment of advanced non-small cell lung cancer enters a targeted era and develops rapidly. New drugs appear constantly. Small molecular tyrosine kinase inhibitors have occupied the biggest piece of the territory, which commonly have a ...
Guowei ZHANG, Huijuan WANG, Zhiyong MA
doaj +1 more source