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Janus kinase inhibitors are potential therapeutics for amyotrophic lateral sclerosis
Amyotrophic lateral sclerosis (ALS) is a poorly treated multifactorial neurodegenerative disease associated with multiple cell types and subcellular...
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The role of mitochondria in the resistance of melanoma to PD-1 inhibitors
Malignant melanoma is one of the most common tumours and has the highest mortality rate of all types of skin cancers worldwide. Traditional and novel...
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Computational Modeling of Phosphodiesterase Inhibitors as Anti-Alzheimer Agents
Neurodegenerative diseases are pathological disorders inducing a gradual loss of neuronal functionality presenting a multifactorial character. Among...
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Cyclin-dependent kinase 7 (CDK7) inhibitors as a novel therapeutic strategy for different molecular types of breast cancer
BACKGROUNDCyclin-dependent kinase (CDK) 7 is aberrantly overexpressed in many types of cancer and is an attractive target for cancer therapy due to...
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PDE5 inhibitors and gastric mucosa: implications for the management of peptic ulcer disease
Peptic ulcer disease (PUD) continues to be a cause of significant morbidity and mortality worldwide. Almost two-thirds of PUD cases are asymptomatic....
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Screening method toward ClbP-specific inhibitors
BackgroundColibactin is a genotoxin produced by Escherichia coli and other Enterobacteriaceae that is believed to increase the risk of colorectal...
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Structure-based optimization of aminothiadiazole inhibitors of AKT
We report here the discovery and structure-guided optimization of a novel series of AKT kinase inhibitors. Based on docking studies for the predicted...
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Potential role for protein kinase D inhibitors in prostate cancer
Protein kinase D (PrKD), a novel serine-threonine kinase, belongs to a family of calcium calmodulin kinases that consists of three isoforms: PrKD1,...
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Immune checkpoint inhibitors in gastrointestinal malignancies: an Umbrella review
In the Modern era, immune checkpoint inhibitors (ICIs) have been the cornerstone of success in the treatment of several malignancies. Despite...
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Acinetobacter baumannii Virulence Factors and Biofilm Components: Synthesis, Structure, Function, and Inhibitors
Acinetobacter baumannii (A. baumannii) is a Gram-negative opportunistic human pathogen, and the drastic dissemination of multidrug resistance in A....
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Novel potent and highly selective DDR1 inhibitors from integrated lead finding
Discoidin domain receptor 1 (DDR1) is a collagen-activated receptor tyrosine kinase and an attractive anti-fibrotic target. To identify novel DDR1...
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CNS-Active p38α MAPK Inhibitors for the Management of Neuroinflammatory Diseases: Medicinal Chemical Properties and Therapeutic Capabilities
During the last two decades, many p38α mitogen-activated protein kinase (p38α MAPK) inhibitors have been developed and tested in preclinical/clinical...
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Dipeptidyl-peptidase-4 inhibitors have anti-inflammatory effects in patients with type 2 diabetes
AimsSystematic low-grade inflammation is considered to be an important factor leading to the development of T2DM and the progression of its...
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Adenine derivatives as inhibitors of the casein kinase CK1delta enzyme
Overexpression of CK1δ has been associated to the development of cancer and neurodegenerative disorders, making ligands of this protein very...
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SUMOylation inhibitors activate anti-tumor immunity by resha** the immune microenvironment in a preclinical model of hepatocellular carcinoma
PurposeHigh levels of heterogeneity and immunosuppression characterize the HCC immune microenvironment (TME). Unfortunately, the majority of...
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Nitric Oxide-cGMP-PKG Signaling in the Cardioprotective Effects of Phosphodiesterase 5 Inhibitors
Phosphodiesterase 5 (PDE5) is an enzyme that catalyzes the degradation of cGMP to its inactive form, 5′-GMP. The inhibition of PDE5 leads to the...
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Medicinal chemistry insights into non-hydroxamate HDAC6 selective inhibitors
HDAC6 is predominantly found in the cytoplasm and is mainly responsible for deacetylation of non-histone proteins including α-tubulin in...
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Meta-analysis and systematic review of vesicular monoamine transporter (VMAT-2) inhibitors in schizophrenia and psychosis
RationaleDopamine antagonists induce dopamine receptor supersensitivity. This may manifest in late-appearing movement disorders (tardive dyskinesia...
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Pharmaceutical aspects of novel CGRP inhibitors used in the prophylaxis and treatment of migraine
Migraine is one of the most prevalent neurological disorders known to have an immense adverse socio-economic impact. Neurogenic inflammation is...
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Role of natural secondary metabolites as HIF-1 inhibitors in cancer therapy
Hypoxia-inducible Factor 1 (HIF-1) is a transcriptional activator that intervenes in versatile reactions to hypoxia. Natural drugs, widely...
