Topic Review
Progress of Natural Product Databases
Natural products (NPs) are a rich source of structurally novel molecules, and the chemical space they encompass is far from being fully explored. NPs have represented a significant source of bioactive molecules and have served as a source of inspiration for developing many drugs on the market. Computer-aided drug design (CADD) has contributed to drug discovery research, mitigating costs and time. In this sense, compound databases represent a fundamental element of CADD. 
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  • 30 Sep 2022
Topic Review
Metal Ions and Bioactive Glasses
Bioactive glasses (BGs) are of great interest in the field of medical implants due to their osteoinductive, osteoproductive, osteoconductive, and antimicrobial properties. Metal ions with bactericidal action can be incorporated into the glass structure in order to improve the antibiofilm activity of the BGs.
  • 20
  • 30 Sep 2022
Topic Review
Proteolysis-targeting Chimeras for Drug Targeted Protein Research
Proteolysis-targeting chimera (PROTAC) is a heterobifunctional molecule. Typically, PROTAC consists of two terminals which are the ligand of the protein of interest (POI) and the specific ligand of E3 ubiquitin ligase, respectively, via a suitable linker. PROTAC degradation of the target protein is performed through the ubiquitin–proteasome system (UPS).
  • 69
  • 26 Sep 2022
Topic Review
HDAC8 in Different Diseases
Histone deacetylases (HDACs), also known as lysine deacetylases (KDACs), belong to the class of zinc (Zn2+)-dependent or nicotinamide adenine dinucleotide (NAD+)-dependent proteolytic enzymes. HDACs participate in transcriptional repression and chromatin condensation mechanisms by removing the acetyl moiety from the acetylated ε-amino group of histone lysines and other non-histone proteins. These enzymes play a pivotal role in the modulation of several cellular pathways such as cell proliferation, apoptosis, neurogenesis and epigenetic regulations. In some cases, HDACs are involved in the occurrence and progression of numerous pathophysiological conditions as well as diseases such as neurological disorders, fibrosis, cancer, metabolic dysfunctions and parasitic infections.
  • 39
  • 23 Sep 2022
Topic Review
Biological Effects of Natural Acylated Flavonoids
Acylated flavonoids are widely distributed natural metabolites in medicinal plants and foods with several health attributes. Flavonoids are secondary metabolites that are widely distributed in planta, and they are well recognized for their health benefits, viz., anticancer, antioxidant, anti-inflammatory, antiviral, and as neuro- and cardio-protective effects. Flavonoids are phytochemicals comprising a benzopyrone ring bearing a phenolic or poly-phenolic group at different positions, classified based on their chemical structure, degree of unsaturation, and oxidation of carbon ring, viz., anthoxanthins (flavanone and flavanol), flavanones, flavanonols, flavans, chalcones, anthocyanidins, and isoflavonoids.
  • 36
  • 14 Sep 2022
Gottfried Heinisch
On 19 September 2019, the Pharmaceutical Science community in Austria lost a distinguished luminary, O. Univ.-Prof.i.R. Dr. Dr.h.c. Mag. pharm. Gottfried Heinisch, at the age of eighty after a long, severe illness. Born in 1938 to a Lower-Austrian Pharmacist’s family, Gottfried Heinisch studied pharmaceutical sciences at the University of Vienna, initially with the perspective of becoming a P
  • 35
  • 13 Sep 2022
Topic Review
Tumor Polyamine-Suppressing Strategy
Several tumor polyamine-suppressing strategies have been developed, as follows. (1) Ornithine decarboxylase (ODC) and S-adenosylmethionine decarboxylase 1 (AMD1) are important for polyamine synthesis. The α-difluoromethylornithine (DFMO), which acts as an irreversible suicide inhibitor of ODC, has been used to prevent and treat multiple cancers, such as pancreatic cancer, gastric cancer, lung carcinoma, neuroblastoma, endometrial cancer, and osteosarcoma. (2) Highly regulated catabolic pathways are utilized to control the intracellular polyamine pool. The modulation of the polyamine catabolic enzyme produces decreasing polyamine content and induces the generation of toxic compounds. (3) Some inhibitors targeting the polyamine transport system (PTS) can hinder polyamine import and antagonize polyamine uptake. (4) Synthetic polyamines, including polyamine analogs and polyamine conjugates, possess anticancer activity against tumor cells.
  • 61
  • 01 Sep 2022
Topic Review
Novel Agent with the Terminal Phenoxy Group
The terminal phenoxy group is a moiety of many drugs in use today. Numerous literature reports indicated its crucial importance for biological activity; thus, it is a privileged scaffold in medicinal chemistry. Most often, the presence of the phenoxy moiety provided the chances for the compound to match the target, ensuring selectivity, the π–π interaction, or increase the ability to form the hydrogen bonds by the oxygen ether atom.
  • 46
  • 01 Sep 2022
Topic Review
An Overview of PDE4 Inhibitors in Clinical Trials
Since the early 1980s, phosphodiesterase 4 (PDE4) has been an attractive target for the treatment of inflammation-based diseases. Several scientific advancements, by both academia and pharmaceutical companies, have enabled the identification of many synthetic ligands for this target, along with the acquisition of precise information on biological requirements and linked therapeutic opportunities. The transition from pre-clinical to clinical phase was not easy for the majority of these compounds, mainly due to their significant side effects, and it took almost thirty years for a PDE4 inhibitor to become a drug i.e., Roflumilast, used in the clinics for the treatment of chronic obstructive pulmonary disease. Three additional compounds have reached the market: Crisaborole for atopic dermatitis, Apremilast for psoriatic arthritis and Ibudilast for Krabbe disease. 
  • 33
  • 31 Aug 2022
Topic Review
Volatilomics in Prostate Cancer
The lack of highly specific and sensitive biomarkers for the early detection of prostate cancer (PCa) is a major barrier to its management. Volatilomics emerged as a non-invasive, simple, inexpensive, and easy-to-use approach for cancer screening, characterization of disease progression, and follow-up of the treatment’s success.
  • 99
  • 24 Aug 2022
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