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Topic Review
3-Iodothyronamine and 3-Iodothyroacetic Acid
3-iodothyronamine (T1AM) and 3-iodothyroacetic acid (TA1) are thyroid-hormone-related compounds endowed with pharmacological activity through mechanisms that remain elusive. Some evidence suggests that they may have redox features.
  • 725
  • 21 Mar 2022
Topic Review
Synthetic Cathinones and Synthetic Cannabinoids
Novel psychoactive substances (NPS) are compounds of natural and synthetic origin, similar to traditional drugs of abuse. NPS are involved in a contemporary trend whose origin lies in a thinner balance between legitimate therapeutic drug research and legislative control. The contemporary NPS trend resulted from the replacement of MDMA by synthetic cathinones in ‘ecstasy’ during the 2000s. The most common NPS are synthetic cannabinoids and synthetic cathinones. Interestingly, during the last 50 years, these two classes of NPS have been the object of scientific research for a set of health conditions. 
  • 725
  • 06 May 2022
Topic Review
Main Metabolic Pathways with Respect to Alzheimer’s Disease
Alzheimer’s disease (AD) is an aging-related neurodegenerative disease, leading to the progressive loss of memory and other cognitive functions. Metabolomics allows the study of biochemical alterations in pathological processes which may be involved in AD progression and to discover new therapeutic targets. Metabolites are substrates, intermediates, and products of metabolic body processes, which typically are small molecules with a molecular weight of less than ~1.5 kDa. Since low molecular weight metabolites are intermediates or end products of cellular metabolism, metabolomics, or the study of metabolism can be considered one of the core disciplines of systems biology. It can help in improving our understanding of changes in biochemical pathways, revealing crucial information that is closely related to human disease or therapeutic status.
  • 725
  • 21 Mar 2023
Topic Review
Nanoparticles in Neuro-Oncology Theranostics
The rapid growth of nanotechnology and the development of novel nanomaterials with unique physicochemical characteristics provides potential for the utility of nanomaterials in theranostics, including neuroimaging, for identifying neurodegenerative changes or central nervous system malignancy. 
  • 724
  • 02 Jul 2021
Topic Review
Pyroptosis and Cancer
Pyroptosis is a programmed cell death characterized by the rupture of the plasma membranes and release of cellular content leading to inflammatory reaction. Four cellular mechanisms inducing pyroptosis have been reported, including the (i) caspase 1-mediated canonical, (ii) caspase 4/5/11-mediated non-canonical, (iii) caspase 3/8-mediated and (iv) caspase-independent pathways. Although discovered as a defense mechanism protecting cells from infections of intracellular pathogens, pyroptosis plays roles in tumor initiation, progression and metastasis of tumors, as well as in treatment response to antitumor drugs and, consequently, patient outcome. Pyroptosis induction following antitumor therapies has been reported in several tumor types, including lung, colorectal and gastric cancer, hepatocellular carcinoma and melanoma.
  • 723
  • 29 Jan 2023
Topic Review
BMVs for Drug Delivery Applications
Numerous factors need to be considered to develop a nanodrug delivery system that is biocompatible, non-toxic, easy to synthesize, cost-effective, and feasible for scale up over and above their therapeutic efficacy. With regards to this, worldwide, exosomes, which are nano-sized vesicles obtained from mammalian cells, are being explored as a biomimetic drug delivery system that has superior biocompatibility and high translational capability. However, the economics of undertaking large-scale mammalian culture to derive exosomal vesicles for translation seems to be challenging and unfeasible. Recently, Bacterial Membrane Vesicles (BMVs) derived from bacteria are being explored as a viable alternative as biomimetic drug delivery systems that can be manufactured relatively easily at much lower costs at a large scale. Until now, BMVs have been investigated extensively as successful immunomodulating agents, but their capability as drug delivery systems remains to be explored in detail. 
  • 722
  • 24 Sep 2021
Topic Review
Mechanistically Coupled PK (MCPK) Model of Dabrafenib Metabolism
Dabrafenib inhibits the cell proliferation of metastatic melanoma with the oncogenic BRAF(V600)-mutation. However, dabrafenib monotherapy is associated with pERK reactivation, drug resistance, and consequential relapse. A clinical drug-dose determination study shows increased pERK levels upon daily administration of more than 300 mg dabrafenib. To clarify whether such elevated drug concentrations could be reached by long-term drug accumulation, the pharmacokinetics (MCPK) of dabrafenib and its metabolites were mechanistically coupled. The MCPK model is qualitatively based on in vitro and quantitatively on clinical data to describe occupancy-dependent CYP3A4 enzyme induction, accumulation, and drug–drug interaction mechanisms. The prediction suggests an eight-fold increase in the steady-state concentration of potent desmethyl-dabrafenib and its inactive precursor carboxy-dabrafenib within four weeks upon 150 mg b.d. dabrafenib. While it is generally assumed that a higher dose is not critical, it was found experimentally that a high physiological dabrafenib concentration fails to induce cell death in embedded 451LU melanoma spheroids.
  • 718
  • 29 Jan 2022
Topic Review
Neuropeptides Inhibitors for Colorectal Cancer
Neuropeptides are mainly secreted from the human central and peripheral nervous systems. Neuropeptides bind to its cognate rhodopsin-like G-protein coupled receptor (GPCR) and perform various physiological functions. Conventional cancer treatments in clinical practice still present many drawbacks due to the lack of selectivity toward the target cell, drug-resistance, and side-effects, thus pushing for the development of new therapeutic agents and therapies. Recent research suggests that neuropeptides influence cancer cell proliferation, invasion, metastasis, and angiogenesis and, therefore, they could be exploited as a target for novel anticancer therapies. Very recently, targeted approaches that inhibit neuropeptides and their associated receptors are being developed in cancer treatment. 
  • 718
  • 29 Sep 2022
Topic Review
Curcumin Inorganic Nanoparticles and its Anti-cancer Potential
Curcumin is a natural compound that has been widely investigated thanks to its various biological properties, including antiproliferative. This molecule acts on different cancers such as lung, breast, pancreatic, colorectal, etc. However, the bioactive actions of curcumin have limitations when its physicochemical properties compromise its pharmacological potential. As a therapeutic strategy against cancer, curcumin has been associated with inorganic nanoparticles. These nanocarriers are capable of delivering curcumin and offering physicochemical properties that synergistically enhance anticancer properties. 
  • 715
  • 31 Jan 2024
Topic Review
TRPA1 Role in Inflammatory Disorders
The transient receptor potential ankyrin 1 (TRPA1), a member of the TRP superfamily of channels, is primarily localized in a subpopulation of primary sensory neurons of the trigeminal, vagal, and dorsal root ganglia, where its activation mediates neurogenic inflammatory responses. The TRPA1 pathway could be a protective mechanism to detect and respond to harmful agents in various pathological conditions, including several inflammatory diseases.
  • 714
  • 09 May 2022
Topic Review
Disrupting GPCR Complexes with Smart Drug-like Peptides
G protein-coupled receptors (GPCRs) are a superfamily of proteins classically described as monomeric transmembrane (TM) receptors. However, increasing evidence indicates that many GPCRs form higher-order assemblies made up of monomers pertaining to identical (homo) or to various (hetero) receptors. The formation and structure of these oligomers, their physiological role and possible therapeutic applications raise a variety of issues that are currently being actively explored. In this context, synthetic peptides derived from TM domains stand out as powerful tools that can be predictably targeted to disrupt GPCR oligomers, especially at the interface level, eventually impairing their action.
  • 713
  • 10 Feb 2022
Topic Review
Intrathecal Pseudodelivery of Drugs for Neurodegenerative Diseases
Intrathecal pseudodelivery of drugs is a novel route to administer medications to treat neurodegenerative diseases based on the cerebrospinal fluid (CSF)-sink therapeutic strategy by means of implantable devices. 
  • 713
  • 10 Mar 2023
Topic Review
Dipeptidyl Peptidase 4 Inhibitors
Information on absorption, metabolism and excretion of drugs is necessary to support the studies on their pharmacokinetics and potential drug–drug interactions. Moreover, the knowledge on drug metabolism is one of the crucial factors used to assess their pharmacokinetic profile in patients with some dysfunctions. It is especially important in diabetic patients with higher incidence of chronic liver and kidney problems.
  • 712
  • 27 Jul 2023
Topic Review
Renoprotective Mechanisms of Medicinal Plants
Diabetic nephropathy (DN), also recognized as diabetic kidney disease, is a kidney malfunction caused by diabetes mellitus. A possible contributing factor to the onset of DN is hyperglycemia. Poorly regulated hyperglycemia can damage blood vessel clusters in the kidneys, leading to kidney damage. Its treatment is difficult and expensive because its causes are extremely complex and poorly understood. Extracts from medicinal plants can be an alternative treatment for DN. The bioactive content in medicinal plants inhibits the progression of DN.
  • 710
  • 13 Mar 2023
Topic Review
Antidiabetic Properties of Plant Secondary Metabolites
Plants with a general tonic effect, plants containing insulin-like substances, plant purifiers, and plants rich in vitamins, organic acids, and other nutrients have been shown to play an important role in the treatment and prevention of type 2 diabetes mellitus and its complications.
  • 709
  • 19 Jun 2023
Topic Review
Treatment of  Rheumatoid Arthritis
Rheumatoid arthritis refers to joint diseases of unclear etiology whose final stages can lead to unbearable pain and complete immobility of the affected joints. Modern treatment with anti-inflammatory drugs, including janus kinase (JAK) inhibitors, monoclonal antibodies, and botanicals (polyphenols, glycosides, alkaloids, etc.) has achieved some success and hope for improving the course of the disease. 
  • 708
  • 30 Oct 2023
Topic Review
Cannabis for Potential Therapeutic Uses
Cannabis sativa has been utilized as a medicine and for recreational and spiritual purposes. Phytocannabinoids are a family of compounds that are found in the cannabis plant, which is known for its psychotogenic and euphoric effects; the main psychotropic constituent of cannabis is Δ9-tetrahydrocannabinol (Δ9-THC). The pharmacological effects of cannabinoids are a result of interactions between those compounds and cannabinoid receptors, CB1 and CB2, located in many parts of the human body. Cannabis is used as a therapeutic agent for treating pain and emesis. Some cannabinoids are clinically applied for treating chronic pain, particularly cancer and multiple sclerosis-associated pain, for appetite stimulation and anti-emesis in HIV/AIDS and cancer patients, and for spasticity treatment in multiple sclerosis and epilepsy patients. Medical cannabis varies from recreational cannabis in the chemical content of THC and cannabidiol (CBD), modes of administration, and safety. Despite the therapeutic effects of cannabis, exposure to high concentrations of THC, the main compound that is responsible for most of the intoxicating effects experienced by users, could lead to psychological events and adverse effects that affect almost all body systems, such as neurological (dizziness, drowsiness, seizures, coma, and others), ophthalmological (mydriasis and conjunctival hyperemia), cardiovascular (tachycardia and arterial hypertension), and gastrointestinal (nausea, vomiting, and thirst), mainly associated with recreational use. Cannabis toxicity in children is more concerning and can cause serious adverse effects such as acute neurological symptoms (stupor), lethargy, seizures, and even coma. 
  • 708
  • 29 Feb 2024
Topic Review
Hemorphins
Hemorphins are endogenous peptides that are also known as “non-classical” or “atypical” opioid peptides. They are produced under physiologicalor pathological(inflammation) states by hemoglobin proteolysis. They can be released from almost any of the hemoglobin chains (beta-, kappa-, delta-, or epsilon-chain) except the alpha chain.
  • 706
  • 09 Jul 2021
Topic Review
Pharmacogenomics Variability of Lipid-Lowering Therapies
The exponential expansion of genomic data coupled with the lack of appropriate clinical categorization of the variants is posing a major challenge to conventional medications for many common and rare diseases. To narrow this gap and achieve the goals of personalized medicine, a collaborative effort should be made to characterize the genomic variants functionally and clinically with a massive global genomic sequencing of “healthy” subjects from several ethnicities. Familial-based clustered diseases with homogenous genetic backgrounds are amongst the most beneficial tools to help address this challenge
  • 706
  • 11 Oct 2021
Topic Review
Pharmacists and Medication Regimen Complexity
Medication regimen complexity (MRC) may influence health outcomes, such as hospitalisation, hospital readmission and medication adherence. Pharmacists have been referred to as health professionals with the opportunity to act on MRC reduction.
  • 705
  • 31 Aug 2021
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