scholarly journals Protein-protein interactions among signaling pathways may become new therapeutic targets in liver cancer (Review)

2015 ◽  
Vol 35 (2) ◽  
pp. 625-638 ◽  
Author(s):  
XIAO ZHANG ◽  
YULAN WANG ◽  
JIAYI WANG ◽  
FENYONG SUN
Keyword(s):  
Liver Cancer ◽  
Signaling Pathways ◽  
Protein Interactions ◽  
Therapeutic Targets ◽  
Protein Protein Interactions ◽  
Cancer Review ◽  
New Therapeutic Targets

scholarly journals Targeted disruption of PKC from AKAP Signaling Complexes

2021 ◽  
Author(s):  
Ameya J. Limaye ◽  
George N. Bendzunas ◽  
Eileen Kennedy
Keyword(s):  
Protein Kinase C ◽  
Protein Kinase ◽  
Signaling Pathways ◽  
Protein Interactions ◽  
Protein Protein Interactions ◽  
Targeted Disruption ◽  
Physiological Processes ◽  
Kinase C ◽  
P Protein

Protein Kinase C (PKC) is a member of the AGC subfamily of kinases and regulates a wide array of signaling pathways and physiological processes. Protein-protein interactions involving PKC and its...

Inositide-dependent signaling pathways as new therapeutic targets in myelodysplastic syndromes

2015 ◽  
Vol 20 (6) ◽  
pp. 677-687 ◽  
Author(s):  
Sara Mongiorgi ◽  
Carlo Finelli ◽  
Yong Ryoul Yang ◽  
Cristina Clissa ◽  
James A. McCubrey ◽  
...  
Keyword(s):  
Signaling Pathways ◽  
Myelodysplastic Syndromes ◽  
Therapeutic Targets ◽  
New Therapeutic Targets

scholarly journals Developing drugs for the ‘undruggable’

BioTechniques ◽  
2020 ◽  
Vol 69 (4) ◽  
pp. 239-241
Author(s):  
Abigail Sawyer
Keyword(s):  
Protein Interactions ◽  
Therapeutic Targets ◽  
Protein Protein Interactions ◽  
Human Interactome ◽  
Novel Therapeutic

There are up to 650,000 ‘undruggable’ protein-protein interactions (PPIs) in the human interactome that can be potentially considered as novel therapeutic targets. How does the ‘undruggable’ become ‘druggable’?

scholarly journals Discovery of cell active macrocyclic peptides with on-target inhibition of KRAS signaling

2021 ◽  
Author(s):  
Shuhui Lim ◽  
Nicolas Boyer ◽  
Nicole Boo ◽  
Chunhui Huang ◽  
Gireedhar Venkatachalam ◽  
...  
Keyword(s):  
Small Molecules ◽  
Protein Interactions ◽  
Therapeutic Targets ◽  
Protein Protein Interactions ◽  
Intracellular Protein ◽  
Macrocyclic Peptides

Macrocyclic peptides have the potential to address intracellular protein-protein interactions (PPIs) of high value therapeutic targets that have proven largely intractable to small molecules. Here, we report broadly applicable lessons...

scholarly journals Latest update on chemokine receptors as therapeutic targets

2021 ◽  
Author(s):  
Wing Yee Lai ◽  
Anja Mueller
Keyword(s):  
Protein Interactions ◽  
Chemokine Receptors ◽  
Inflammatory Diseases ◽  
Specific Binding ◽  
Therapeutic Targets ◽  
Cell Types ◽  
Fine Tuning ◽  
Protein Protein Interactions ◽  
Diverse Range ◽  
Chemokine Ligand

The chemokine system plays a fundamental role in a diverse range of physiological processes, such as homeostasis and immune responses. Dysregulation in the chemokine system has been linked to inflammatory diseases and cancer, which renders chemokine receptors to be considered as therapeutic targets. In the past two decades, around 45 drugs targeting chemokine receptors have been developed, yet only three are clinically approved. The challenging factors include the limited understanding of aberrant chemokine signalling in malignant diseases, high redundancy of the chemokine system, differences between cell types and non-specific binding of the chemokine receptor antagonists due to the broad ligand-binding pockets. In recent years, emerging studies attempt to characterise the chemokine ligand–receptor interactions and the downstream signalling protein–protein interactions, aiming to fine tuning to the promiscuous interplay of the chemokine system for the development of precision medicine. This review will outline the updates on the mechanistic insights in the chemokine system and propose some potential strategies in the future development of targeted therapy.

scholarly journals Chimeric GPCRs mimic distinct signaling pathways and modulate microglia responses

2021 ◽  
Author(s):  
Rouven Schulz ◽  
Medina Korkut-Demirbaş ◽  
Gloria Colombo ◽  
Sandra Siegert
Keyword(s):  
Signaling Pathways ◽  
Protein Interactions ◽  
Immune Cell ◽  
Signal Transmission ◽  
The Body ◽  
Cell Type ◽  
Protein Protein Interactions ◽  
Β2 Adrenergic Receptor ◽  
Neuronal Signal ◽  
And Function

G protein-coupled receptors (GPCRs) regulate multiple processes ranging from cell growth and immune responses to neuronal signal transmission. However, ligands for many GPCRs remain unknown, suffer from off-target effects or have poor bioavailability. Additional challenges exist to dissect cell type-specific responses when the same GPCR is expressed on different cells within the body. Here, we overcome these limitations by engineering DREADD-based GPCR chimeras that selectively bind their agonist clozapine-N-oxide (CNO) and mimic a GPCR-of-interest. We show that the chimeric DREADD-β2-adrenergic receptor (β2AR/ADRB2) triggers comparable responses to levalbuterol on second messenger and kinase activity, post-translational modifications, and protein-protein interactions. Moreover, we successfully recapitulate β2AR-mediated filopodia formation in microglia, a β2AR-expressing immune cell that can drive inflammation in the nervous system. To further dissect microglial inflammation, we compared DREADD-β2AR with two additionally designed DREADD-based chimeras mimicking GPR65 and GPR109A/HCAR2, both enriched in microglia. DREADD-β2AR and DREADD-GPR65 modulate the inflammatory response with a similar profile as endogenously expressed β2AR, while DREADD-GPR109A had no impact. Our DREADD-based approach allows investigation of cell type-dependent signaling pathways and function without known endogenous ligands.

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