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Topic Review Video
Allosteric Antagonism of the Pregnane X Receptor
The pregnane X receptor (PXR, NR1I2) is a xenobiotic-activated transcription factor with high levels of expression in the liver. It not only plays a key role in drug metabolism and elimination, but also promotes tumor growth, drug resistance, and metabolic diseases. It has been proposed as a therapeutic target for type II diabetes, metabolic syndrome, and inflammatory bowel disease, and PXR antagonists have recently been considered as a therapy for colon cancer. The identified allosteric sites of the PXR provide new insights into the development of safe and efficient allosteric modulators of the PXR receptor. Researchers therefore propose that novel PXR allosteric sites might be promising targets for treating chronic metabolic diseases and some cancers. 
  • 484
  • 13 Oct 2022
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. 
  • 616
  • 29 Mar 2022
Topic Review
Alpha-2 Agonists for Attention Deficit Hyperactivity Disorder
Attention Deficit Hyperactivity Disorder (ADHD) is one of the most common neurodevelopmental disorders, characterized by the Diagnostic and Statistical Manual of Mental Disorders, Fifth Edition (DSM-5), which is marked by symptoms such as inappropriate levels of inattention, hyperactivity, and impulsivity that can affect academic, social, and personal functioning in children and adolescents.
  • 261
  • 01 Jun 2023
Topic Review
Alpha-Amylase Inhibitory Metabolites from Pericarps of Garcinia mangostana
Two new benzophenones and five known metabolites were purified from Garcinia mangostana ((GM) pericarps. They were characterized by various spectral techniques. Compounds 6 and 7 displayed AAI activity. They also exhibited highly negative docking scores, when complexed with 5TD4. Their complexes with the α-amylase were found to be stable over the course of 50 ns. These results supported the previous reports that GM can potentially represent an appealing treatment of diabetes and its related disorders.
  • 407
  • 29 Mar 2022
Topic Review
Alpha-Lipoic Acid
Alpha-lipoic acid (LA) is a powerful endogenous and exogenous antioxidant. It is a disulfide compound soluble in both water and oil.
  • 1.0K
  • 30 Aug 2021
Topic Review
American Ginseng Berry and its Mental Health Applications
Despite the popularity of the ginseng (Panax) root in health research and on the market, the ginseng berry’s potential remains relatively unexplored. Implementing ginseng berry cultivations and designing berry-derived products could improve the accessibility to mental health-promoting nutraceuticals.
  • 463
  • 30 Jun 2022
Topic Review
Amorphization of Poorly Water-Soluble Drugs
Amorphization technology has been the subject of continuous attention in the pharmaceutical industry, as a means to enhance the solubility of poorly water-soluble drugs. Being in a high energy state, amorphous formulations generally display significantly increased apparent solubility as compared to their crystalline counterparts, which may allow them to generate a supersaturated state in the gastrointestinal tract and in turn, improve the bioavailability. Conventionally, hydrophilic polymers have been used as carriers, in which the amorphous drugs were dispersed and stabilized to form polymeric amorphous solid dispersions. However, the technique had its limitations, some of which include the need for a large number of carriers, the tendency to recrystallize during storage, and the possibility of thermal decomposition of the drug during preparation. Therefore, emerging amorphization technologies have focused on the investigation of novel amorphous-stabilizing carriers and preparation methods that can improve the drug loading and the degree of amorphization. 
  • 1.3K
  • 08 Sep 2021
Topic Review
Analytical Assessment of Biosimilars
The analytical assessment includes testing physicochemical and functional attributes to establish a claim of biosimilarity. How closely a biosimilar candidate should match the reference product will remain questionable since a reference product is approved based on whatever quality attributes it presents; a biosimilar candidate, on the other hand, must match these quality attributes, even if the reference product’s attributes are not the most desirable.
  • 1.5K
  • 27 Apr 2022
Topic Review
Anastasios Lymperopoulos
My laboratory for the Study of Neurohormonal Control of the Circulation studies the molecular pharmacology, physiology, and biology of the G protein-coupled receptors (GPCRs) that regulate cardiac function and systemic circulation in general. Particular emphasis is given to autonomic nervous system`s (specifically adrenergic) receptors and to angiotensin II receptors. The general focus is on studying mechanisms underlying abnormal signaling/function of these GPCRs that contribute to heart failure pathophysiology, aiming at discovering and validating novel molecular targets for cardiovascular disease therapy. Our lab`s studies also include novel molecular effects of beta-blockers and angiotensin receptor blockers, two very important drug classes acting through cardiovascular adrenergic and angiotensin receptors, respectively.
  • 742
  • 29 Oct 2020
Topic Review
Angiotensin II Type 2 Receptor
Preclinical evidence, accumulated over the past decade, indicates that the angiotensin II type 2 receptor (AT2R) stimulation exerts significant neuroprotective effects in various animal models of neuronal injury, notably in the central nervous system.   Studies of brain AT2R distribution and function are outshining the recent findings about AT2R in peripheral sensoryneurons and pain modulation. While AT2R, as an atypical G protein-coupled receptor, and its related signaling are still under investigation, pharmacological studies have shown that stimulation of AT2R leads to neuritogenesis in vitro and in vivo. This review aims to report the evidence of potential neuroprotective and neuroregenerative roles of AT2R in the peripheral nervous system (PNS).
  • 1.0K
  • 10 Mar 2021
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