Results 141 to 150 of about 22,958,501 (389)

Discovery of Natural Compound α‐Hederin via Large‐Scale Screening as a Targeted JAK/STAT3 Inhibitor for Ovarian Cancer Therapy

open access: yesAdvanced Science, EarlyView.
This study identifies α‐Hederin as a potent dual JAK1/JAK2 inhibitor that blocks STAT3 activation in ovarian cancer. By disrupting STAT3‐driven transcriptional programs, α‐Hederin suppresses tumor proliferation, invasion, and EMT, while enhancing cisplatin efficacy and overcoming chemoresistance.
Jiayu Wang   +9 more
wiley   +1 more source

Identification and characterization of an irreversible inhibitor of CDK2 [PDF]

open access: yes, 2015
Irreversible inhibitors that modify cysteine or lysine residues within a protein kinase ATP binding site offer, through their distinctive mode of action, an alternative to ATP-competitive agents.
Anscombe, Elizabeth   +16 more
core   +1 more source

Irisin Attenuates Pulmonary Vascular Remodeling in Pulmonary Arterial Hypertension via Ubiquitin‐Mediated Regulation of ENO1

open access: yesAdvanced Science, EarlyView.
Irisin is a crucial plasma biomarker and promising therapeutic target that reflects disease severity, pulmonary vascular remodeling status and clinical outcome in patients with pulmonary arterial hypertension (PAH). As a novel protective factor, irisin is downregulated in PAH. By ubiquitination, irisin promotes Enolase 1 degradation and suppresses cell
Na Sun   +15 more
wiley   +1 more source

SCF Fbx4/alphaB-crystallin cyclin D1 ubiquitin ligase: a license to destroy

open access: yesCell Division, 2007
Cyclin D1 is an allosteric regulator for cyclin-dependent kinases 4 and 6 (CDK4/6). The cyclin D/CDK4 kinase promotes G1/S transition through the posttranslational modification and the subsequent inactivation of the retinoblastoma (Rb) protein and ...
Lin Douglas I   +2 more
doaj   +1 more source

The Molecular Perspective: Cyclins

open access: yesSTEM CELLS, 2004
Abstract Learning Objective After completing this course, the reader will be able to: Describe the role of cyclins and cyclin-dependent kinases in cancer. Access and take the CME test online and receive 1 hour of AMA PRA category 1 credit at CME.TheOncologist.com
openaire   +4 more sources

PTf‐SRiApt Targeting SCAF4‐POLR2A Interaction Suppresses Tumor Growth and Promotes Antitumor Immunity in Triple‐Negative Breast Cancer

open access: yesAdvanced Science, EarlyView.
A phosphorothioate‐modified aptamer PTf‐SRiApt capable of disrupting “undruggable” transcription factor SCAF4‐POLR2A interaction with high inhibitory activity and biological stability is presented here. Through this inhibition, PTf‐SRiApt successfully arrested cell cycle progression, induced cell death, and elevated immune recruitment in SCAF4‐POLR2A ...
Liyan Fei   +13 more
wiley   +1 more source

Histone deacetylase inhibitor, Trichostatin A induces ubiquitin-dependent cyclin D1 degradation in MCF-7 breast cancer cells

open access: yesMolecular Cancer, 2006
Background Cyclin D1 is an important regulator of G1-S phase cell cycle transition and has been shown to be important for breast cancer development.
Charles Coombes R   +4 more
doaj   +1 more source

Bromodomain analysis of Brd2-dependent transcriptional activation of cyclin A.

open access: yesBiochemical Journal, 2005
Cyclin A is regulated primarily through transcription control during the mammalian cell cycle. A dual mechanism of cyclin A transcriptional repression involves, on the one hand, promoter-bound inhibitory complexes of E2F transcription factors and RB ...
A. Sinha, D. Faller, G. Denis
semanticscholar   +1 more source

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