Results 71 to 80 of about 27,930 (225)

Synthesis and Antitumor Activity of Staurosporine Derivatives

open access: yesNatural Product Communications, 2022
Twenty-four derivatives of staurosporine were synthesized by modification at the 3′- N , 3- and 7-positions. Of these compounds, 16 were synthesized for the first time and their structures were determined by NMR spectroscopy, ECD, and HRESIMS.
Gang Li   +6 more
doaj   +1 more source

PANoptosis in the pathogenesis of myelodysplastic syndromes

open access: yesMolecular Oncology, Volume 20, Issue 11, Page 2584-2610, November 2026.
PANoptosis, a combination of three types of programmed cell death, is mediated by a large protein complex called a PANoptosome. In healthy bone marrow hematopoietic cells, PANoptosis is restricted by inhibitory signaling. In MDS, bone marrow cells become sensitive to the PANoptotic stimuli due to the aberrant inactivation of inhibitory signaling or ...
Rohit Thalla   +4 more
wiley   +1 more source

Staurosporine mobilizes Ca2+ from secretory granules by inhibiting protein kinase C in rat submandibular acinar cells

open access: yes, 2002
Staurosporine was previously shown to mobilize Ca2+ from the thapsigargin-insensitive Ca2+ store in rat submandibular acinar cells. However, the nature of the store is not yet known.
신동민, 이승일, 서정택
core   +1 more source

Defining the conformational landscape of glycogen synthase kinase 3 beta (GSK3β)

open access: yesActa Crystallographica Section D, Volume 82, Issue 11, Page 1285-1297, November 2026.
This article presents a systematic structural curation of all deposited GSK3β crystal structures to map its conformational ensemble, revealing eight distinct conformational states.Glycogen synthase kinase 3 beta (GSK3β) is a serine/threonine kinase implicated in Alzheimer's disease, type 2 diabetes, oncology and bipolar disorder, and represents an ...
Akanksha Gurtu, Fernanda Laezza
wiley   +1 more source

Alkylation of staurosporine to derive a kinase probe for fluorescence applications [PDF]

open access: yes, 2016
The natural product staurosporine is a high-affinity inhibitor of nearly all mammalian protein kinases.The labelling of staurosporine has proven effective as a means of generating protein kinase research tools. Most tools have been generated by acylation
Alexander J. M. Disney   +5 more
core   +1 more source

Computational POM and DFT Evaluation of Experimental in-vitro Cancer Inhibition of Staurosporine-Ruthenium(II) Complexes: The Power Force of Organometallics in Drug Design

open access: yesActa Chimica Slovenica, 2015
A computational Petra/Osiris/Molinspiration/DFT(POM/DFT) based model has been developed for the identification of physic-chemical parameters governing the bioactivity of  Ruthenium-Staurosporine complexes 2-4 containing an antitumoral-Kinase (TK ...
Taibi Ben Hadda   +9 more
doaj   +1 more source

Decoding neuronal vulnerability: Multidimensional analysis of D1R‐ and D2R‐ medium‐sized spiny neurons in Huntington's disease

open access: yesBrain Pathology, Volume 36, Issue 6, November 2026.
D1R and D2R MSNs show distinct responses to Huntington's pathology. G&T‐sequencing of pre‐symptomatic MSNs reveals global LINE‐1 downregulation. While D1R‐MSNs display early transcriptomic changes (OXPHOS/translation upregulation) and reduced mutant huntingtin aggregation, D2R‐MSNs exhibit higher nuclear mHTT accumulation and greater CAG somatic ...
Guendalina Bergonzoni   +22 more
wiley   +1 more source

Activation of GSK3 Prevents Termination of TNF-Induced Signaling

open access: yesJournal of Inflammation Research, 2021
Bastian Welz,* Rolf Bikker,* Leonie Hoffmeister, Mareike Diekmann, Martin Christmann, Korbinian Brand,* René Huber* Institute of Clinical Chemistry, Hannover Medical School, Hannover, 30625, Germany*These authors contributed equally to this ...
Welz B   +6 more
doaj  

Staurosporine Increases Lentiviral Vector Transduction Efficiency of Human Hematopoietic Stem and Progenitor Cells

open access: yesMolecular Therapy: Methods & Clinical Development, 2018
Lentiviral vector (LVV)-mediated transduction of human CD34+ hematopoietic stem and progenitor cells (HSPCs) holds tremendous promise for the treatment of monogenic hematological diseases.
Gretchen Lewis   +10 more
doaj   +1 more source

Thermodynamic characterisation of covalent ligand binding

open access: yesBritish Journal of Pharmacology, Volume 183, Issue 22, Page 6704-6717, November 2026.
Background and Purpose Differential scanning fluorimetry (DSF) is a common and straightforward method to evaluate the thermal stability of proteins and has been heavily used for ligand binding characterisation as well as for screening. One class of compounds that is less typically evaluated by DSF are covalent binders.
Rebecca Hertzman   +4 more
wiley   +1 more source

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