Crizotinib-induced antitumour activity in human alveolar rhabdomyosarcoma cells is not solely dependent on ALK and MET inhibition [PDF]
BACKGROUND: Rhabdomyosarcoma (RMS) is the most commonly diagnosed malignant soft tissue tumour in children and adolescents. Aberrant expression of Anaplastic Lymphoma Kinase (ALK) and MET gene has been implicated in the malignant progression of RMS ...
CAMERO, SIMONA+11 more
core +1 more source
Computer-aided drug discovery/design (CADD) techniques allow the identification of natural products that are capable of modulating protein functions in pathogenesis-related pathways, constituting one of the most promising lines followed in drug discovery.
Laura Llorach-Pares+3 more
doaj +1 more source
Cdc2-like kinases: structure, biological function and therapeutic targets for diseases
The CLKs (Cdc2-like kinases) belong to the dual-specificity protein kinase family and play crucial roles in regulating transcript splicing via the phosphorylation of SR proteins (SRSF1–12), catalyzing spliceosome molecular machinery, and modulating the ...
Mengqiu Song+5 more
doaj +1 more source
Ca2+ triggers premature inactivation of the cdc2 protein kinase in permeabilized sea urchin embryos.
Exit from mitosis requires inactivation of the cyclin B-p34cdc2 protein kinase complex. Since increased cytosolic Ca2+ has been implicated as a potential trigger of mitotic progression, we directly tested the possibility that Ca2+ triggers the pathway ...
F. Suprynowicz, C. Prusmack, T. Whalley
semanticscholar +1 more source
Neuronal Cdc2-like Kinase (Nclk) Binds and Phosphorylates the Retinoblastoma Protein [PDF]
The tumor suppressor retinoblastoma protein (RB) plays a central role in cellular growth regulation, differentiation, and apoptosis. Phosphorylation of RB results in a consequent loss of its ability to inhibit cell cycle progression. However, how RB phosphorylation might be regulated in apoptotic or postmitotic cells, such as neurons, remains unclear ...
Caren C. Helbing+5 more
openaire +4 more sources
High throughput screens yield small molecule inhibitors of Leishmania CRK3:CYC6 cyclin-dependent kinase. [PDF]
Leishmania species are parasitic protozoa that have a tightly controlled cell cycle, regulated by cyclin-dependent kinases (CDKs). Cdc2-related kinase 3 (CRK3), an essential CDK in Leishmania and functional orthologue of human CDK1, can form an active ...
Roderick G Walker+9 more
doaj +1 more source
Billion-years old proteins show the importance of N-lobe orientation in Imatinib-kinase selectivity [PDF]
The molecular origins of proteins' functions are a combinatorial search problem in the proteins' sequence space, which requires enormous resources to solve. However, evolution has already solved this optimization problem for us, leaving behind suboptimal solutions along the way. Comparing suboptimal proteins along the evolutionary pathway, or ancestors,
arxiv
Functional characterization of the diatom cyclin-dependent kinase A2 as a mitotic regulator reveals plant-like properties in a non-green lineage [PDF]
Background: Cyclin-dependent kinases (CDKs) are crucial regulators of cell cycle progression in eukaryotes. The diatom CDKA2 was originally assigned to the classical A-type CDKs, but its cell cycle phase-specific transcription at the G2-to-M phase ...
Bowler, Chris+4 more
core +2 more sources
A three-state kinetic mechanism for scaffold mediated signal transduction [PDF]
Signaling events in eukaryotic cells are often guided by a scaffolding protein. Scaffold proteins assemble multiple proteins in a spatially localized signaling complex and exert numerous physical effects on signaling pathways. To study these effects, we consider a minimal, three-state kinetic model of scaffold mediated kinase activation.
arxiv +1 more source
The Immune Microenvironment: New Therapeutic Implications in Organ Fibrosis
This review summarizes recent advances in understanding the immune microenvironment's role in fibrosis, focusing on phenotypic/functional alterations of immune cells and their dynamic interactions with other cellular constituents within tissues. The authors further explore therapeutic opportunities and challenges in targeting immune microenvironment ...
Xiangqi Chen+6 more
wiley +1 more source