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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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Are mGluR2/3 Inhibitors Potential Compounds for Novel Antidepressants?
Depression is the most common mental illness characterized by anhedonia, avolition and loss of appetite and motivation. The majority of conventional...
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Impact of HIF prolyl hydroxylase inhibitors in heart failure patients with renal anemia
ObjectiveHypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitors are a new class of anti-anemia agents. We retrospectively evaluated the...
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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...
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Recent Advances in FDA-Approved Kinase Inhibitors Targeting Lung Cancer
Lung cancer is a chronic deadly disease and is implicated with highest mortality rate among all cancers since years. Kinase are the...
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Design and Applications of Genetically-Encoded Voltage-Dependent Calcium Channel Inhibitors
Ca2+ influx through high-voltage-gated Ca2+ channels (HVGCCs; CaV1/CaV2) is an exceptionally powerful and versatile signal that controls numerous...
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SGLT2 inhibitors prevent LPS-induced M1 macrophage polarization and alleviate inflammatory bowel disease by downregulating NHE1 expression
BackgroundClassically activated M1 macrophages, characterized by aberrant glycolysis and secretion of inflammatory cytokines, play pivotal roles in...
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Vital residues-orientated rational design of butenolide inhibitors targeting Of ChtI
An effective approach for discovering small molecular inhibitors is the residues-oriented strategy based on enzyme analysis. In this study, we...
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Progress in discovery and development of natural inhibitors of histone deacetylases (HDACs) as anti-cancer agents
The study of epigenetic translational modifications had drawn great interest for the last few decades. These processes play a vital role in many...
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Discovery of potent maternal embryonic leucine zipper kinase (MELK) inhibitors of novel chemotypes using structure-based pharmacophores
Maternal embryonic leucine zipper kinase (MELK) is a serine-threonine kinase. Several studies have revealed its role as a regulator in the...
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Development of convenient crystallization inhibition assays for structure-activity relationship studies in the discovery of crystallization inhibitors
Kidney stone diseases are increasing globally in prevalence and recurrence rates, indicating an urgent medical need for develo** new therapies that...
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Small-Molecule HIV Entry Inhibitors Targeting gp120 and gp41
Interrupting early events in the virus life cycle, such as those prior to the formation of provirus, could effectively prevent HIV-1 infection. HIV-1...
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Systematical Evaluation of the Structure-Cardiotoxicity Relationship of 7-Azaindazole-based PI3K Inhibitors Designed by Bioisosteric Approach
A growing concern of cardiotoxicity induced by PI3K inhibitors has raised the requirements to evaluate the structure-cardiotoxicity relationship...
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Rheumatoid arthritis—recent advances in pathogenesis and the anti-inflammatory effect of plant-derived COX inhibitors
The majority of people with autoimmune disorders, including those with rheumatoid arthritis, osteoarthritis, and tendonitis report pain, stiffness,...
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Histone Deacetylase Inhibitors: Design, Synthesis, and Biological Evaluation
Alzheimer’s disease (AD), a neurodegenerative disease, is a chronic form of dementia. AD is mostly prevalent in the elderly and is characterised by...
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High-content analysis identified synergistic drug interactions between INK128, an mTOR inhibitor, and HDAC inhibitors in a non-small cell lung cancer cell line
BackgroundThe development of drug resistance is a major cause of cancer therapy failures. To inhibit drug resistance, multiple drugs are often...
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Impact of low serum iron on treatment outcome of PD-1 inhibitors in advanced gastric cancer
BackgroundThe aim of this study was to investigate the influence of serum iron levels in advanced gastric cancer (GC) patients treated with...
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Hit-to-lead optimization of amino-carboxamide benzothiazoles as LSD1 inhibitors
The lysine-specific demethylase enzyme (LSD1) is a potential therapeutic target in cancer, which has a significant role in oncogenic processes such...
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Design, synthesis and antitumor activity evaluation of novel benzamide HDAC inhibitors
In recent years, histone deacetylase (HDAC) has become one of the hottest and most effective targets for the treatment of cancer. In this work, we...
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Tumor immune checkpoints and their associated inhibitors
Immunological evasion is one of the defining characteristics of cancers, as the immune modification of an immune checkpoint (IC) confers immune...