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Topic Review
Biography
Topic Review
1-C Metabolism in AML
One-carbon (1-C) metabolism is essential for numerous cancer cell functions, including protein and nucleic acid synthesis and maintaining cellular redox balance, and inhibition of the 1-C pathway has yielded several highly active drugs, such as methotrexate and 5-FU.
617
07 Jul 2021
Topic Review
1,2,4-Triazoles
Compounds containing the 1,2,4-triazole ring in their structure are characterised by multidirectional biological activity.
1.7K
23 Aug 2021
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.
328
21 Mar 2022
Topic Review
4D Printing Technology
4D printing (4DP) is an evolution of 3DP where additive manufacturing printing techniques are employed. In other words, adapting 3DP processes for 4DP of shape memory polymers (SMPs) or smart materials requires minor adjustments. In order to produce the desired shape-changing materials as per estimation or for optimal application, an air circulation system may be incorporated into 3DP’s traditional fused deposition method (FDM) technology. This would cool the SMP below its Tg and, after these small alterations, previous 3DP methods such as stereolithography apparatus (SLA), digital laser writing and inkjet printing can also be employed.
391
05 Jan 2023
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.
386
30 May 2023
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.
468
18 Mar 2021
Topic Review
Peer Reviewed
A Journey to Hear: The Evolution of Cochlear Implants
Cochlear implants (CIs), a revolutionary breakthrough in auditory technology, have profoundly impacted the lives of individuals with severe hearing impairment. Surgically implanted behind the ear and within the delicate cochlea, these devices represent a direct pathway to restoring the sense of hearing. Implanting hope alongside innovation, their captivating history unfolds through pivotal dates and transformative milestones. From the first human implantation by Drs. William House and John Doyle in 1961 to FDA approval in 1984, each step in their evolution mirrors a triumph of human ingenuity. The 1990s witnessed significant miniaturization, enhancing accessibility, while the 21st century brought about improvements in speech processing and electrode technology. These strides have elevated CIs beyond functional devices to life-changing instruments, enriching both auditory experiences and communication skills. This entry delves into the captivating history of CIs, spotlighting key dates that paint a vivid picture of challenges overcome and remarkable progress achieved. It explores the people and moments that defined their development, ultimately shaping these implants into indispensable tools that continually redefine the landscape of hearing assistance.
623
12 Jan 2024
Topic Review
A Novel, Pan-PDE Inhibitor From the Group of 7,8-Disubstituted Purine-2,6-Dione Derivatives
Phosphodiesterases (PDEs) inhibitors are currently a widespread and extensively studied group of anti-inflammatory and anti-fibrotic compounds which may find use in the treatment of numerous lung diseases, including asthma and chronic obstructive pulmonary disease. Several PDE inhibitors are currently in clinical development, and some of them, e.g. roflumilast, are already recommended for clinical use. Due to numerous reports indicating that elevated intracellular adenosine 3’,5’-cyclic monophosphate (cAMP) levels may contribute to alleviation of inflammation and airway fibrosis, new and effective PDE inhibitors are constantly being sought. Recently, a group of 7,8-disubstituted purine-2,6-dione derivatives, representing novel and prominent pan-PDE inhibitors has been synthesized. Some of them were reported to modulate transient receptor potential ankyrin 1 (TRPA1) ion channels as well. Compound 145 (4-(8-butoxy-1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(5-(tert-butyl)-2-hydroxyphenyl)butanamide) – a pan-PDE inhibitor and a weak TRPA1 modulator inhibited fibroblast to myofibroblasts transition (FMT) as well as MRC-5 human lung fibroblasts proliferation, migration, and contraction. The effect of this compound appeared to depend mainly on its strong PDE inhibitory properties, and not on its effects on TRPA1 modulation. The strong anti-remodelling effects of 145 required activation of the cAMP/protein kinase A/CREB pathway leading to inhibition of transforming growth factor type β1 (TGF-β1) and Smad-dependent signalling in MRC-5 cells.
608
09 Sep 2021
Topic Review
A2B Adenosine Receptors
Adenosine is a signalling molecule which, by activating specific membrane receptors, acts as an important player during brain insults such as ischemia. or demyelinating injuries. Here we review data in the literature describing A2B receptor-mediated effects in preclinical in vitro and in vivo models of cerebral ischemia and myelination that point to A2B receptor ligands as putative therapeutic targets for the still unmet treatment of stroke or demyelinating diseases.
601
14 Apr 2021
Topic Review
Accum™ Technology
Compromised activity is a common impediment for biologics requiring endosome trafficking into target cells. In cancer cells, antibody-drug conjugates (ADCs) are trapped in endosomes or subsequently pumped extracellularly, leading to a reduction in intracellular accumulation. In subsets of dendritic cells (DCs), endosome-engulfed antigens face non-specific proteolysis and collateral damage to epitope immunogenicity before proteasomal processing and subsequent surface presentation. Accum™ is a novel biotechnology exemplifying, in its initial concept, the need to circumvent the biological challenges of ADCs.
340
29 Jul 2022
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