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Topic Review
Microbiota
The human gut microflora comprises over 1000 species and more than 7000 strains, representing 1013–1014 bacterial cells, which is ten times more numerous than other cells. Healthy gut microbiota is mainly composed of the phyla Firmicutes and Bacteroidetes, representing around 90% of the human gut flora, followed by Actinobacteria, Verrucomicrobia, and Proteobacteria.
  • 1.7K
  • 18 Jan 2022
Topic Review
Biological Drug Approvals by the FDA in 2015–2021
Despite belonging to a relatively new class of pharmaceuticals, biological drugs have been used since the 1980s, when they brought about a breakthrough in the treatment of chronic diseases, especially cancer. They conquered a large space in the pipeline of the pharmaceutical industry and boosted the innovation portfolio and arsenal of therapeutic compounds available. From 2015 to 2021, the number of drugs included in this class grew over this period, totaling 90 approvals, with an average of 13 authorizations per year.
  • 1.7K
  • 30 Sep 2022
Topic Review
Chemical Exchange Saturation Transfer MRI
Recently, Chemical Exchange Saturation Transfer (CEST) MRI is emerging as an attractive approach with the capability of directly using low concentration, exchangeable protons-containing agents for generating quantitative MRI contrast. The ability to utilize diamagnetic compounds has been extensively exploited to detect many clinical compounds, such as FDA approved drugs, X-ray/CT contrast agents, nutrients, supplements, and biopolymers. The ability to directly off-label use clinical compounds permits CEST MRI to be rapidly translated to clinical settings.
  • 1.7K
  • 12 Jan 2021
Topic Review
Tackling Pandemics through Computer-Aided Drug Discovery Approaches
Since its outbreak in December 2019, the COVID-19 pandemic has caused the death of more than 6.5 million people around the world. The high transmissibility of its causative agent, the SARS-CoV-2 virus, coupled with its potentially lethal outcome, provoked a profound global economic and social crisis. The urgency of finding suitable pharmacological tools to tame the pandemic shed light on the ever-increasing importance of computer simulations in rationalizing and speeding up the design of new drugs, further stressing the need for developing quick and reliable methods to identify novel active molecules and characterize their mechanism of action. 
  • 1.7K
  • 08 Mar 2023
Topic Review
Phenothiazines Modified with Pyridine Ring
Azaphenothiazines are the largest and most perspective group of modified phenothiazines, and they exhibit variety of biological activities. The review sums up the current knowledge on the anticancer activity of isomeric pyridobenzothiazines and dipyridothiazines, which are modified azaphenothiazines with one and two pyridine rings, respectively, against 10 types of cancer cell lines. Some 10-substituted dipyridothiazines and even 10-unsubstituted parent compounds, such as 10H-1,9-diazaphenothiazine and 10H-3,6-diazaphenothiazine, exhibited very potent action with the IC50 values less than 1 µg/mL and 1 µM against selected cancer cell lines. The strength of the anticancer action depends both on the tricyclic ring scaffolds and the substituents at the thiazine nitrogen atom.
  • 1.7K
  • 18 Mar 2021
Topic Review
Development of Trichosanthin
Tian Hua Fen, a herbal powder extract that contains trichosanthin (TCS), was used as an abortifacient in traditional Chinese medicine. In 1972, TCS was purified to alleviate the side effects. Because of its clinical applications, TCS became one of the most active research areas in the 1960s to the 1980s in China. These include obtaining the sequence information in the 1980s and the crystal structure in 1995. The replication block of TCS on human immunodeficiency virus in lymphocytes and macrophages was found in 1989 and started a new chapter of its development.
  • 1.7K
  • 21 Mar 2022
Topic Review
Phosphodiesterase 5 Inhibitors
Phosphodiesterase 5 (PDE5) inhibitors presented themselves as important players in the nitric oxide/cGMP pathway, thus exerting a profound impact on various physiological and pathological processes. Beyond their well-known efficacy in treating male erectile dysfunction (ED) and pulmonary arterial hypertension (PAH), a plethora of studies have unveiled their significance in the treatment of a myriad of other diseases, including cognitive functions, heart failure, multiple drug resistance in cancer therapy, immune diseases, systemic sclerosis and others.
  • 1.7K
  • 19 Oct 2023
Topic Review
GABAAR-Mediated Currents
Propofol or barbiturate application at low concentrations increases desensitization and slows deactivation of GABA-induced current and propofol/barbiturate at high concentrations directly elicits after-responses upon their washout in hippocampal or sensory neurons. It is postulated that the generation of such after-responses is caused by removal of the blockade by anesthetic agents as partial antagonists. However, the increased desensitization was invariably followed by slowdown of deactivation of GABA-induced current, and the after-response may arise as a consequence of extreme slowdown of deactivation following strong desensitization. It is thus possible that propofol and barbiturate can facilitate resensitization of GABA responses. Propofol and barbiturate are useful to treat the alcohol/benzodiazepine withdrawal syndrome. Considering that the slowdown of deactivation following desensitization and the after-response induced by propofol or barbiturate application, the regulatory mechanisms of desensitization/resensitization of GABAAR-mediated currents might be important for understanding the treatment of the alcohol/benzodiazepine withdrawal syndrome.
  • 1.6K
  • 29 Oct 2020
Topic Review
Periodontitis and Systemic Disorder
Periodontitis, a major oral disease, affects a vast majority of the population but has been often ignored without realizing its long-fetched effects on overall human health. A realization in recent years of its association with severe diseases such as carditis, low birth weight babies, and preeclampsia has instigated dedicated research in this area. In the arena of periodontal medicines, the studies of past decades suggest a link between human periodontal afflictions and certain systemic disorders such as cardiovascular diseases, diabetes mellitus, respiratory disorders, preterm birth, autoimmune disorders, and cancer. Although, the disease appears as a locoregional infection, the periodontal pathogens, in addition their metabolic products and systemic mediators, receive access to the bloodstream, thereby contributing to the development of systemic disorders. Mechanism-based insights into the disease pathogenesis and association are highly relevant and shall be useful in avoiding any systemic complications.
  • 1.6K
  • 30 Sep 2021
Topic Review
Lipid-Based Nanoparticles as a Versatile Drug Delivery System
Liposomes, nanoemulsions, solid lipid nanoparticles, nanostructured lipid nanocarriers, and lipid–polymer hybrid nanoparticles are developed for cancer treatment which is well confirmed and documented. cancer nanotechnology that overcomes the drawbacks of conventional drug delivery systems starting from small-scale barricades such as intracellular trafficking and site-specific targeting to large-scale barriers such as biodistribution.
  • 1.6K
  • 27 Sep 2022
Topic Review
Overcoming Multidrug Resistance of Antibiotics via Nanodelivery Systems
Antibiotic resistance has become a threat to microbial therapies nowadays. The conventional approaches possess several limitations to combat microbial infections. Therefore, to overcome such complications, novel drug delivery systems have gained pharmaceutical scientists’ interest. Significant findings have validated the effectiveness of novel drug delivery systems such as polymeric nanoparticles, liposomes, metallic nanoparticles, dendrimers, and lipid-based nanoparticles against severe microbial infections and combating antimicrobial resistance. 
  • 1.6K
  • 18 Mar 2022
Topic Review
Micro- and Nanosized Carriers for Nose-to-Brain Drug Delivery
The intranasal route of drug administration offers numerous advantages, such as bypassing the intestine, avoiding first-pass metabolism, and reducing systemic side effects. Moreover, it circumvents the BBB, providing direct entrance to the brain through the olfactory and trigeminal nerve pathways.  Micro- and nanotechnological approaches were widely used to overcome these limitations and enhance the availability of drugs in the brain tissue. Micro- and nanoparticulate carriers are composed of natural or synthetic materials that interact with biological structures at the molecular level and lead the treatment of NDs into a new direction. They may induce interaction between target sites, thus minimizing the side effects.
  • 1.6K
  • 22 Aug 2022
Topic Review
Exosomal-based Drug Delivery
Exosomes are membrane-bound nanovesicles that are typically 30–150 nm in size with various bioactive molecules. They are typically generated by first endocytosing various transmembrane proteins into endosomes within the cell, which are then sorted and form intraluminal vesicles. These vesicles are then released as the endosome merges with the cell membrane and releases its contents outside of the cell. Tetraspanins (CD9, CD63, CD81) are one of the most common proteins expressed on the surface of exosomes and are often used as exosome-specific markers. These proteins have been shown to interact with different proteins such as integrins and major histocompatibility complexes (MHC). Exosomes commonly act as carriers of genetic and proteomic information, and are therefore vital in intercellular communication. In its role as a cellular messenger, exosomes have been implicated in promoting cancer; because of this, they are also being investigated as potential therapeutic targets and delivery vehicles. 
  • 1.6K
  • 06 Jun 2021
Topic Review
Allosteric Modulation of Adenosine A2A Receptors
Adenosine is a naturally occurring purine nucleoside that regulates various physiologic functions, including inflammation and wound healing, cardiac contraction, blood vessel formation, vasodilation, learning, memory, sleep, and arousal. Adenosine is released by neurons and glial cells. Extracellular adenosine modulates neuronal excitability, synaptic plasticity, and the release and reuptake of several neurotransmitters. The effects of extracellular adenosine are modulated via four subtypes of G-protein coupled adenosine receptors (GPCRs), denoted A1, A2A, A2B, and A3. Adenosine A2A receptors (A2ARs) are broadly expressed in the brain, cardiovascular system, blood vessels, spleen, thymus, leukocytes, and lung, making them an important drug target. The therapeutic potential of targeting adenosine A2ARs is immense due to their broad expression in the body and central nervous system. The role of A2ARs in cardiovascular function, inflammation, sleep/wake behaviors, cognition, and other primary nervous system functions has been extensively studied. 
  • 1.6K
  • 29 Mar 2022
Topic Review
Paracetamol
Paracetamol (acetaminophen) is one of the most commonly prescribed drugs worldwide. Synthetized over 150 years ago, paracetamol is highly efficient as analgesic and antipyretic and is on the list of the World Health Organization’s essential medicines. Paracetamol is also a hypothermic agent.
  • 1.6K
  • 28 Apr 2022
Topic Review
Clinical Trials of Parkinson’s Disease
Parkinson’s disease (PD) is a progressive neurodegenerative disorder that currently has no cure, but treatments are available to improve PD symptoms and maintain quality of life.
  • 1.6K
  • 03 Aug 2021
Topic Review
MiRNA-7
MicroRNAs (miRNAs, miRs) are small non-coding RNA (ncRNA) molecules capable of regulating post-transcriptional gene expression. Imbalances in the miRNA network have been associated with the development of many pathological conditions and diseases, including cancer. Recently, miRNAs have also been linked to the phenomenon of multidrug resistance (MDR). MiR-7 is one of the extensively studied miRNAs and its role in cancer progression and MDR modulation has been highlighted. MiR-7 is engaged in multiple cellular pathways and acts as a tumor suppressor in the majority of human neoplasia. Its depletion limits the effectiveness of anti-cancer therapies, while its restoration sensitizes cells to the administered drugs.
  • 1.6K
  • 25 Feb 2021
Topic Review
Lipid-Based Nanocarriers
Nanoparticle-based drug delivery has demonstrated promising results for topical ophthalmic nanotherapies in the treatment of intraocular diseases. Studies have revealed that nanocarriers enhance the intraocular half-life and bioavailability of several therapies including proteins, peptides and genetic material. Amongst the array of nanoparticles available nowadays, lipid-based nanosystems have shown an increased efficiency and feasibility in topical formulations, making them an important target for constant and thorough research in both preclinical and clinical practice.
  • 1.6K
  • 19 Jun 2021
Topic Review
Promising Anticancer and Neuroprotective Compounds
Flavonoids derived from citrus plants are favored by phytomedicinal researchers due to their wide range of biological activities, and relevant studies have been sustained (since the first paper published in 1955). The modern pharmacological effects of citrus flavonoids are primarily focused on their anticancer activities (such as breast cancer, gastric cancer, lung cancer, and liver cancer), neuroprotective effects (such as anti-Alzheimer’s disease, Parkinson’s disease), and metabolic diseases.
  • 1.6K
  • 22 Mar 2023
Topic Review
AhR, inflammation and breast cancer
AhR, an environmentally sensitive transcription factor, is one of the more evolutionary conserved molecules in living cells.
  • 1.6K
  • 21 Feb 2022
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