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Topic Review
Clinical Application of Hypoxia-Inducible Factor-1α Inhibitors
Hypoxia is a common phenomenon amongst physiological and pathological conditions, and is a strong stressor for cells and organisms, which can lead to metabolic disorders, and even cause cell death. Hypoxia-inducible factor-1α (HIF-1α) is the only transcription factor that has been found to be active under hypoxia, and is also the main nuclear transcription factor that mediates the adaptive response to hypoxia in mammals. It is closely related to the growth and development of organisms and the pathogenesis of some diseases. HIF-1α has low expression in the human brain, lung, placenta, heart, skeletal muscle, kidney, and pancreas under normoxia, but there is an exponentially large increase of HIF-1α in the brain, lung, kidney, heart, and other tissues under hypoxia. HIF-1α inhibitors can be widely used in the treatment of various diseases related to HIF-1 overexpression, such as tumors; leukemia; diabetes and its complications; ischemic, cardiovascular and brain diseases; and inflammatory diseases, etc.
  • 220
  • 20 Jul 2023
Biography
Carlos M. Villalón
Carlos M. Villalón was born in Mexico City on November 2, 1959. He completed his studies in Chemistry & Pharmacy (Pharmacist) in 1983 at the National School of Biological Sciences (IPN), and his postgraduate studies at the Department of Pharmacology and Toxicology of Cinvestav (M.Sc. in 1986 and Ph.D. in 1988). Between 1988 and 1991 he did a postdoctoral stay at the Erasmus Universiteit Rotterd
  • 483
  • 18 Jul 2023
Topic Review
Drugs of the Kallikrein–Kinin System
The kallikrein–kinin system consists of the two kininogen substrates present in the blood plasma, and two serine proteases: the plasma and tissue kallikreins. The action of the latter on kininogens produces small peptides, the kinins, short-lived, but endowed by powerful pharmacologic actions on blood vessels and other tissues. Several classes of drugs alter kinin formation or action at their receptors for a therapeutic benefit.
  • 489
  • 17 Jul 2023
Topic Review
Prejunctional 5-HT Receptors/Mechanisms and Modulation of Neurovascular Transmission
5-Hydroxytryptamine (5-HT), or serotonin, plays a crucial role as a neuromodulator and/or neurotransmitter of several nervous system functions. Its actions are complex, and depend on multiple factors, including the type of effector or receptor activated. Briefly, 5-HT can activate: (i) metabotropic (G-protein-coupled) receptors to promote inhibition (5-HT1, 5-HT5) or activation (5-HT4, 5-HT6, 5-HT7) of adenylate cyclase, as well as activation (5-HT2) of phospholipase C; and (ii) ionotropic receptor (5-HT3), a ligand-gated Na+/K+ channel. Regarding blood pressure regulation (and beyond the intricacy of central 5-HT effects), this monoamine also exerts direct postjunctional (on vascular smooth muscle and endothelium) or indirect prejunctional (on autonomic and sensory perivascular nerves) effects. At the prejunctional level, 5-HT can facilitate or preclude the release of autonomic (e.g., noradrenaline and acetylcholine) or sensory (e.g., calcitonin gene-related peptide) neurotransmitters facilitating hypertensive or hypotensive effects. Hence, we cannot formulate a specific impact of 5-HT on blood pressure level, since an increase or decrease in neurotransmitter release would be favoured, depending on the type of prejunctional receptor involved.
  • 401
  • 14 Jul 2023
Topic Review
SARS-CoV-2 Peptide Vaccines
Several times during the past two decades, epidemic viral diseases created global challenges. Although many solutions have been proposed to deal with this tight spot, it is still believed that public vaccination represents the most effective strategy to handle it. So far, various kinds of vaccines including protein subunits, virus-like particles, inactivated, live attenuated, viral vectors, RNA, and DNA vaccines have been used in the prevention of COVID-19. Among the various categories of vaccines, peptide vaccines have created a new hope for quick and trustworthy access due to the development of proteomics equipment.
  • 305
  • 14 Jul 2023
Topic Review
Biological Activities of Asteltoxins
Asteltoxins belong to a group of polyene pyrone mycotoxins that are known to be potent inhibitors of mitochondrial ATP synthesis and ATP hydrolysis. Asteltoxin A was first isolated from the toxic maize cultures of Aspergillus stellatus. Several attempts have been made to synthesize asteltoxin A, starting with the synthesis of a bis(tetrahydrofuran) moiety that has been demonstrated previously in biosynthetic studies. 
  • 428
  • 14 Jul 2023
Topic Review
Docking Studies of Recently Synthesized MAO-B Inhibitors
With the significant growth of patients suffering from neurodegenerative diseases (NDs), novel classes of compounds targeting monoamine oxidase type B (MAO-B) are promptly emerging as distinguished structures for the treatment of the latter. As a promising function of computer-aided drug design (CADD), structure-based virtual screening (SBVS) is being heavily applied in processes of drug discovery and development. The utilization of molecular docking, as a helping tool for SBVS, is providing essential data about the poses and the occurring interactions between ligands and target molecules. 
  • 314
  • 13 Jul 2023
Topic Review
Steroidal (Glyco)Alkaloids: Classification
Steroidal (glycol)alkaloids S(G)As are secondary metabolites made of a nitrogen-containing steroidal skeleton linked to a (poly)saccharide, naturally occurring in the members of the Solanaceae and Liliaceae plant families. The genus Solanum is familiar to all of us as a food source (tomato, potato, eggplant), but a few populations have also made it part of their ethnobotany for their medicinal properties. The recent development of the isolation, purification and analysis techniques have shed light on the structural diversity among the SGAs family, thus attracting scientists to investigate their various pharmacological properties. 
  • 379
  • 11 Jul 2023
Topic Review
Phytochemicals and Parkinson’s Disease
Complementary therapies and phytonutrients derived from plant sources have been proposed as treatments for Parkinson’s disease. Numerous natural phytochemicals have emerged as therapeutically interesting compounds, drug entities, and phytochemicals for the treatment of inflammatory disorders. Additionally, numerous pharmacological studies have shown that phytochemicals are useful in treating neurodegenerative diseases (NDDs), depression, and dementia.
  • 247
  • 10 Jul 2023
Topic Review
Metastasis Suppression through Primary Tumour Targeting with Nanoparticles
Nanotechnology’s use has expanded, demonstrating its efficacy in enhancing fields such as cancer treatment, radiation therapy, diagnostics, and imaging. Applications for nanomaterials are diverse, ranging from enhanced radiation adjuvants to more sensitive early detection instruments. Cancer, particularly when it has spread beyond the original site of cancer, is notoriously tough to combat. Many people die from metastatic cancer, which is why it remains a huge issue. Cancer cells go through a sequence of events known as the “metastatic cascade” throughout metastasis, which may be used to build anti-metastatic therapeutic techniques. Conventional treatments and diagnostics for metastasis have their drawbacks and hurdles that must be overcome. 
  • 218
  • 10 Jul 2023
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