Fatty Acid Biosynthesis: An Updated Review on KAS Inhibitors.

Since the early twentieth century, with the isolation of penicillin and streptomycin in the 1940s, the modern era of anti-infective drug development has gained momentum. Due to the enormous success of early drug discovery, many infectious diseases were successfully prevented and eradicated. However, this initial hope was wrongheaded, and pathogens evolved as a significant threat to human health.

Potential of triazines in Alzheimer's disease: A versatile privileged scaffold.

Triazines are six-membered privileged scaffolds that have been explored in drug discovery programs owing to their stability in biological media and robust reactivity. Their unique chemical properties have led to the exploration of the triazine-containing molecules for multifaceted disorders like Alzheimer's disease (AD). The pathology of AD involves the interplay of multiple biochemical events such as amyloid beta-aggregation, formation of reactive oxygen species, cholinergic degradation, and metal ion dysregulation.

Emerging topical drug delivery approaches for the treatment of Atopic dermatitis.

Background: Atopic dermatitis is a chronic, relapsing skin inflammation disease that generally affects 20% of children and 1-3% of adults. It is characterized by pruritus, inflammatory skin lesions, and skin barrier defect. The pillar treatment is topical therapies that have shown great adherence and incredible results in alleviating symptoms of atopic dermatitis.

The Wnt/β-catenin pathway in breast cancer therapy: a pre-clinical perspective of its targeting for clinical translation.

Introduction: Despite various treatments available, there is still a high mortality rate in breast cancer patients. Thus, there exists an unmet need for new therapeutic interventions. Studies show that the Wnt/β-catenin signaling pathway is involved in breast cancer metastasis because of its transcriptional control on epithelial to mesenchymal transition.

2 Receptor Specific Ligand Conjugated Nanocarriers: An Effective Strategy for Targeted Therapy of Tuberculosis.

Tuberculosis (TB) is an ancient chronic disease caused by the bacillus Mycobacterium tuberculosis, which has affected mankind for more than 4,000 years. Compliance with the standard conventional treatment can assure recovery from tuberculosis, but the emergence of drug-resistant strains poses a great challenge for the effective management of tuberculosis. The process of discovery and development of new therapeutic entities with better specificity and efficacy is unpredictable and time-consuming.

Pyrimidine: An elite heterocyclic leitmotif in drug discovery-synthesis and biological activity.

Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. Heterocycles possessing a pyrimidine scaffold have piqued tremendous interest of organic and medicinal chemists owing to their privileged bioactivities. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.

SIRT1-FOXOs activity regulates diabetic complications.

The prevalence of diabetes is continuously increasing in the recent decades. Persistent hyperglycemia, hyperinsulinemia and the subsequent oxidative stress result in diabetic complications, primarily categorized as microvascular (nephropathy, retinopathy and neuropathy) and macrovascular (cardiomyopathy) complications. The complications are prevalent in both type 1 and type 2 diabetic patients.

Caveolin-1: A Promising Therapeutic Target for Diverse Diseases.

The plasma membrane of eukaryotic cells contains small flask-shaped invaginations known as caveolae that are involved in the regulation of cellular signaling. Caveolin-1 is a 21-24k- Da protein localized in the caveolar membrane. Caveolin-1 (Cav-1) has been considered as a master regulator among the various signaling molecules.

Cellulosic Polymers for Enhancing Drug Bioavailability in Ocular Drug Delivery Systems.

One of the major impediments to drug development is low aqueous solubility and thus poor bioavailability, which leads to insufficient clinical utility. Around 70-80% of drugs in the discovery pipeline are suffering from poor aqueous solubility and poor bioavailability, which is a major challenge when one has to develop an ocular drug delivery system. The outer lipid layer, pre-corneal, dynamic, and static ocular barriers limit drug availability to the targeted ocular tissues.

Identification of potential antileishmanial 1,3-disubstituted-4-hydroxy-6-methylpyridin-2(1H)-ones, in vitro metabolic stability, cytotoxicity and molecular modeling studies.

We report the synthesis and in vitro evaluation of 1,3-disubstituted-4-hydroxy-6-methylpyridin-2(1H)-one derivatives against Leishmania donovani. Amongst the compound library synthesized, molecules 3d, 3f, 3h, 3i, 3l, and 3m demonstrated substantial dose-dependent killing of the promastigotes. Their IC values range from 55.

The pleiotropic peroxisome proliferator activated receptors: Regulation and therapeutics.

The Peroxisome proliferator-activated receptors (PPARs) are key regulators of metabolic events in our body. Owing to their implication in maintenance of homeostasis, both PPAR agonists and antagonists assume therapeutic significance. Understanding the molecular mechanisms of each of the PPAR isotypes in the healthy body and during disease is crucial to exploiting their full therapeutic potential.

Emerging Role of Interleukins for the Assessment and Treatment of Liver Diseases.

Background: The most common liver diseases are fibrosis, alcoholic liver disease, nonalcoholic fatty disease, viral hepatitis, and hepatocellular carcinoma. These liver diseases account for approximately 2 million deaths per year worldwide, with cirrhosis accounting for 2.1% of the worldwide burden.

Deubiquitylating enzymes: potential target in autoimmune diseases.

The ubiquitin-proteasome pathway is responsible for the turnover of different cellular proteins, such as transport proteins, presentation of antigens to the immune system, control of the cell cycle, and activities that promote cancer. The enzymes which remove ubiquitin, deubiquitylating enzymes (DUBs), play a critical role in central and peripheral immune tolerance to prevent the development of autoimmune diseases and thus present a potential therapeutic target for the treatment of autoimmune diseases. DUBs function by removing ubiquitin(s) from target protein and block ubiquitin chain elongation.

Cellulose nanocrystals: Fundamentals and biomedical applications.

The present review explores the recent developments of cellulose nanocrystals, a class of captivating nanomaterials in variety of applications. CNCs are made by acid hydrolysing cellulosic materials like wood, cotton, tunicate, flax fibers by sonochemistry. It has many desirable properties, including a high tensile strength, wide surface area, stiffness, exceptional colloidal stability, and the ability to be modified.

Advances in Pyrazole Based Scaffold as Cyclin-dependent Kinase 2 Inhibitors for the Treatment of Cancer.

The transformation of a normal cell into a tumor cell is one of the initial steps in cell cycle deregulation. The cell cycle is regulated by cyclin-dependent kinases (CDKs) that belong to the protein kinase family. CDK2 is an enchanting target for specific genotype tumors since cyclin E is selective for CDK2 and the deregulation of specific cancer types.

An insight into cytotoxic activity of flavonoids and sesquiterpenoids from selected plants of Asteraceae species.

Cancer continues to be a disease that is difficult to cure and the current therapeutic regimen is associated with severe side effects and the issue of emerging drug resistance. According to the World Health Organization fact sheet 2017, cancer is the second major cause of morbidity and death and a 70% rise in new cases is expected over the next 20 years. The quest for new anticancer chemical entities is a thrust area identified by many government agencies and industry research and development groups.

Recent advancements in cellulose-based biomaterials for management of infected wounds.

Introduction: Chronic wounds are a substantial burden on the healthcare system. Their treatment requires advanced dressings, which can provide a moist wound environment, prevent bacterial infiltration, and act as a drug carrier. Cellulose is biocompatible, biodegradable, and can be functionalized according to specific requirements, which makes it a highly versatile biomaterial.

Bromodomains: A novel target for the anticancer therapy.

Bromodomains are a group of structurally diverse proteins characterized as readers of post-translational modifications. They bear unique structural topology and are known to have diverse cellular functions. As epigenetic readers of histone acetylation, bromodomains appear to have both physiological and pathological implications.

Synthetic Strategies of Pyrimidine-Based Scaffolds as Aurora Kinase and Polo-like Kinase Inhibitors.

The past few decades have witnessed significant progress in anticancer drug discovery. Small molecules containing heterocyclic moieties have attracted considerable interest for designing new antitumor agents. Of these, the pyrimidine ring system is found in multitude of drug structures, and being the building unit of DNA and RNA makes it an attractive scaffold for the design and development of anticancer drugs.

Design and Encapsulation of Immunomodulators onto Gold Nanoparticles in Cancer Immunotherapy.

The aim of cancer immunotherapy is to reactivate autoimmune responses to combat cancer cells. To stimulate the immune system, immunomodulators, such as adjuvants, cytokines, vaccines, and checkpoint inhibitors, are extensively designed and studied. Immunomodulators have several drawbacks, such as drug instability, limited half-life, rapid drug clearance, and uncontrolled immune responses when used directly in cancer immunotherapy.

Nano intervention in topical delivery of corticosteroid for psoriasis and atopic dermatitis-a systematic review.

Atopic dermatitis (AD) and psoriasis are highly prevalent, complex, chronic inflammatory skin diseases that immensly affect the patient's quality of life. While there is no definitive cure for these conditions, suppressive medications aim at managing the symptoms of these diseases. The application of emollients accompanied by symptomatic anti-inflammatory therapy consisting of topical corticosteroids (TCS) is extensively employed for controlling the symptoms among general practitioners making this therapeutic class an indispensable pillar of dermatotherapeutics.

Topical nanocarriers for management of Rheumatoid Arthritis: A review.

Rheumatoid arthritis (RA) is a systemic autoimmune disease manifested by chronic joint inflammation leading to severe disability and premature mortality. With a global prevalence of about 0.3%-1% RA is 3-5 times more prevalent in women than in men.

Therapeutic benefits of natural oils along with permeation enhancing activity.

The skin is the largest organ of the integumentary system with a multifunctional purpose to protect the body from heat and microbes, regulate body temperature, and act as a sensory organ. A topical dosage form applied on the skin will have to cross the stratum corneum, which would then allow the dosage form to traverse the subsequent layers of the skin. The drug with poor solubility and short half-life would serve as an ideal candidate for its delivery via the transdermal route.

Emerging epigenetic targets in rheumatoid arthritis.

Rheumatoid arthritis is a complex disorder that is characterized by irreversible and progressive destructions of joints, but its exact etiology remains mainly unknown. The occurrence and the progression of the disease entirely depend on environmental and genetic factors. In recent years, various epigenetic changes involving DNA methylation, histone modification, miRNA, X-chromosome inactivation, bromodomain, sirtuin, and many others were identified that were found to be linked to the activation and the aggressive phenotype in rheumatoid arthritis.

Therapeutic potential of ferulic acid and its derivatives in Alzheimer's disease-A systematic review.

Alzheimer's disease (AD) is a progressive neurodegenerative disorder primarily caused by accumulation of amyloid-beta (Aβ) peptide extracellularly and neurofibrillary tangles intracellularly. Recently, it has been shown that oxidative stress and mitochondrial dysregulation play an important role in pathology of AD. Therefore, modulating various targets such as Aβ aggregation, neuro-inflammation, and oxidative stress, genetic factors such as Apolipoprotein E gene (ApoE) are some of the ways to manage AD.