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Topic Review
5-Aminolevulinic Acid Photodynamic Therapy in Cancer Treatment
5-aminolevulinic acid-photodynamic therapy (5-ALA-PDT) is a therapeutic option for a variety of cutaneous and internal malignancies. PDT uses a photosensitizer that, activated by light in the presence of molecule oxygen, forms ROS, which are responsible for the apoptotic activity of the malignant tissues. 5-ALA is usually used as an endogenous pro-photosensitizer because it is converted to Protoporphyrin IX (PpIX), which enters into the process of heme synthesis and contextually becomes a photosensitizer, radiating a red fluorescent light. PDT has the benefit of being administered before or after chemotherapy, radiation, or surgery, without impairing the efficacy of these treatment techniques. Furthermore, sensitivity to PDT is unaffected by the negative effects of chemotherapy or radiation. 
  • 522
  • 30 May 2023
Topic Review
5-Aminolevulinic Acid Priming to Enhance Plant Tolerance
Priming is an adaptive strategy that improves plant defenses against biotic and abiotic stresses. Stimuli from chemicals, abiotic cues, and pathogens can trigger the establishment of priming state. Priming with 5-aminolevulinic acid (ALA), a potential plant growth regulator, can enhance plant tolerance to the subsequent abiotic stresses, including salinity, drought, heat, cold, and UV-B. However, the molecular mechanisms underlying the remarkable effects of ALA priming on plant physiology remain to be elucidated.
  • 602
  • 26 Jan 2022
Topic Review
5-Arylidenerhodanines as P-gp Modulators
Multidrug resistance (MDR) is considered one of the major mechanisms responsible for the failure of numerous anticancer and antiviral chemotherapies. Various strategies to overcome the MDR phenomenon have been developed, and one of the most attractive research directions is focused on the inhibition of MDR transporters, membrane proteins that extrude cytotoxic drugs from living cells. 
  • 346
  • 14 Apr 2023
Topic Review
5-Azacitidine Treatment in Myelodysplastic Syndrome Patients
This entry focused on the impact of the treatment with the hypomethylating agent 5-azacitidine on the redox status and inflammation in 24 MDS patients. Globally, MDS patients showed less redox status in terms of a reduction in the GSSG/GSH ratio and in the LPO levels, as well as increased CAT activity compared with healthy subjects, with no changes in SOD, GPx, and GRd activities, or  AOPP levels. When analyzing the evolution from early to advanced stages of the disease, we found that the GPx activity, GSSG/GSH ratio, LPO, and AOPP increased, with a reduction in CAT. GPx changes were related to the presence of risk factors such as high-risk IPSS-R or mutational score. Moreover, there was an increase in IL-2, IL-6, IL-8, and TNF-α plasma levels, with a further increase of IL-2 and IL-10 from early to advanced stages of the disease. However, we did not observe any association between inflammation and oxidative stress.
  • 398
  • 29 Mar 2022
Topic Review
5-Bromo-2′-deoxyuridine
The thymidine analogue 5-bromo-2′-deoxyuridine (BrdU) is a pyrimidine 2′-deoxyribonucleoside compound having 5-bromouracil as the nucleobase. This agent is permanently incorporated into the DNA during the synthetic phase of the cell cycle. It has been argued that gene duplication, DNA repair or apoptotic cellular events might contribute to BrdU labeling in vivo.
  • 640
  • 12 Oct 2021
Topic Review
5-HT2A Receptor Ligands Against Depression
According to the World Health Organization, depression is a multifactorial disorder that affects around 350 million people worldwide. The most widespread monoamine of the CNS-serotonin (5-HT) is believed to play a vital role in the pathomechanism of this condition, and the importance of the neurotransmitter is elevated by the "serotonin hypothesis", linking the presence of the depression-like symptoms with diminished 5-HT concentration in certain brain regions. Serotonin acts its biological effects via numerous receptors. Out of all seven types of serotonin receptors, the serotonin 2A receptor has been identified as a most promising molecular target valuable for the treatment of mood disorders. Recent medicinal chemistry findings on the structure and function of the serotonin 2A (5-HT2A) receptor facilitated design and discovery of novel anti-depressants. 
  • 1.2K
  • 14 Feb 2022
Topic Review
5-HT2B Receptor in Fibrosing ILD
Interstitial lung disease (ILD) encompasses a heterogeneous group of more than 200 conditions, of which primarily idiopathic pulmonary fibrosis (IPF), idiopathic nonspecific interstitial pneumonia, hypersensitivity pneumonitis, ILD associated with autoimmune diseases and sarcoidosis may present a progressive fibrosing (PF) phenotype. Despite different aetiology and histopathological patterns, the PF-ILDs have similarities regarding disease mechanisms with self-sustaining fibrosis, which suggests that the diseases may share common pathogenetic pathways. Previous studies show an enhanced activation of serotonergic signaling in pulmonary fibrosis, and the serotonin (5-HT)2 receptors have been implicated to have important roles in observed profibrotic actions.
  • 512
  • 19 Jan 2021
Topic Review
5-Hydroxymethylfurfural (HMF)
HMF, an indispensable member of the furan-based platform compound, known as the “sleeping giant”, is a bridge between renewable biomass and industrial bulk chemicals. In recent years, the catalytic transformation of biomass to HMF has been widely studied and envisaged to be hopeful in achieving sustainable biorefineries. The synthesis of HMF from biomass requires the acid hydrolysis of biomass to hexose, and then dehydration of hexose, to obtain HMF. In the second step of dehydration, starting from ketohexose (fructose) is more efficient than starting from aldohexose (glucose).
  • 1.4K
  • 11 Oct 2021
Topic Review
5-Hydroxytryptamine 2B Receptor
Since the first characterization of the 5-hydroxytryptamine 2B receptor (5-HT2BR) in 1992, significant progress has been made in understanding the biological function, the structure, and small-molecule pharmaceutical ligands of the 5-HT2BR. Emerging evidence has suggested that the 5-HT2BR is implicated in the regulation of the cardiovascular system, fibrosis disorders, cancer, gastrointestinal (GI) tract, and nervous system. Eight crystal complex structures of the 5-HT2BR bound with different ligands provided great insights into ligand recognition, activation mechanism, and biased signaling. Numerous 5-HT2BR antagonists have been discovered and developed, and several of them have been advanced to clinical trials. It is expected that the novel 5-HT2BR antagonists with high potency and selectivity will lead to first-in-class drugs in various therapeutic areas.
  • 533
  • 18 Mar 2021
Topic Review
5-Hydroxytryptamine and Gut
Serotonin, also known as 5-hydroxytryptamine (5-HT), is a metabolite of tryptophan and is reported to modulate the development and neurogenesis of the enteric nervous system, gut motility, secretion, inflammation, sensation, and epithelial development. Approximately 95% of 5-HT in the body is synthesized and secreted by enterochromaffin (EC) cells, the most common type of neuroendocrine cells in the gastrointestinal (GI) tract, through sensing signals from the intestinal lumen and the circulatory system. Gut microbiota, nutrients, and hormones are the main factors that play a vital role in regulating 5-HT secretion by EC cells. Apart from being an important neurotransmitter and a paracrine signaling molecule in the gut, gut-derived 5-HT was also shown to exert other biological functions (in autism and depression) far beyond the gut. Moreover, studies conducted on the regulation of 5-HT in the immune system demonstrated that 5-HT exerts anti-inflammatory and proinflammatory effects on the gut by binding to different receptors under intestinal inflammatory conditions. Understanding the regulatory mechanisms through which 5-HT participates in cell metabolism and physiology can provide potential therapeutic strategies for treating intestinal diseases. Herein, we review recent evidence to recapitulate the mechanisms of synthesis, secretion, regulation, and biofunction of 5-HT to improve the nutrition and health of humans.
  • 861
  • 17 Aug 2021
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