Artificial transmembrane ion transporters as potential therapeutics

Coronavirus disease 2019 (COVID-19) is a new infectious respiratory disease that has caused the ongoing global pandemic. The primary purpose of this article is to describe evolving clinical epidemiology of COVID-19, including 1) infection and testing, 2) clinical spectrum including classification of clinical type, asymptomatic cases, severe cases and comorbidity, and clinical and immunological response, 3) regional variation in clinical presentation, 4) population distribution by age, sex, and occupation, and finally, 5) case-fatality. This content may provide important information on detailed clinical type and presentation of the disease, in which appropriate clinical outcomes can be derived for developing prevention strategies and clinical studies or trials that aim to test potential therapeutics or products for different patient populations.

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Synthesis of Acetogenin Analogs as Potential Therapeutics for Treating Prostate Cancer

10.21236/ada407206 ◽

2002 ◽

Author(s):

Brian L. Pagenkopf

Keyword(s):

Prostate Cancer ◽

Potential Therapeutics

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Click Reactions in Chemistry of Triterpenes - Advances Towards Development of Potential Therapeutics

Current Medicinal Chemistry ◽

10.2174/0929867324666171009122612 ◽

2018 ◽

Vol 25 (5) ◽

pp. 636-658 ◽

Cited By ~ 22

Author(s):

Jan Pokorny ◽

Lucie Borkova ◽

Milan Urban

Keyword(s):

Biological Activities ◽

Synthetic Approach ◽

Clinical Use ◽

New Approach ◽

Click Reactions ◽

Drug Candidates ◽

The Past ◽

Low Toxicity ◽

New Compounds ◽

Potential Therapeutics

Triterpenoids are natural compounds with a large variety of biological activities such as anticancer, antiviral, antibacterial, antifungal, antiparazitic, antiinflammatory and others. Despite their low toxicity and simple availability from the natural resources, their clinical use is still severely limited by their higher IC50 and worse pharmacological properties than in the currently used therapeutics. This fact encouraged a number of researchers to develop new terpenic derivatives more suitable for the potential clinical use. This review summarizes a new approach to improve both, the activity and ADME-Tox properties by connecting active terpenes to another modifying molecules using click reactions. Within the past few years, this synthetic approach was well explored yielding a lot of great improvements of the parent compounds along with some less successful attempts. A large quantity of the new compounds presented here are superior in both activity and ADME-Tox properties to their parents. This review should serve the researchers who need to promote their hit triterpenic structures towards their clinical use and it is intended as a guide for the chemical synthesis of better drug candidates.

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Microbial Genetic Screens for Monitoring Protein Misfolding Associated with Neurodegeneration: Tools for Identifying Disease-Relevant Genes and for Screening Synthetic and Natural Compound Libraries for the Discovery of Potential Therapeutics

Current Pharmaceutical Design ◽

10.2174/1381612824666180515143752 ◽

2018 ◽

Vol 24 (19) ◽

pp. 2055-2075 ◽

Cited By ~ 3

Author(s):

Kalliopi Kostelidou ◽

Ilias Matis ◽

Georgios Skretas

Keyword(s):

Protein Misfolding ◽

Socioeconomic Impact ◽

Genetic Screens ◽

Subsequent Formation ◽

The Past ◽

Compound Libraries ◽

Selection Systems ◽

Cellular Factors ◽

Effective Drugs ◽

Potential Therapeutics

Neurodegenerative Diseases (ND) are a major threat to the aging population and the lack of a single preventive or disease-modifying agent only serves to increase their impact. In the past few years, protein misfolding and the subsequent formation of neurotoxic oligomeric/aggregated protein species have emerged as a unifying theme underlying the pathology of these complex diseases. Recently developed microbial genetic screens and selection systems for monitoring ND-associated protein misfolding have allowed the establishment of highthroughput assays for the identification of cellular factors and processes that are important mediators of NDassociated proteotoxicities. In addition, such systems have facilitated the discovery of synthetic and natural compounds with the ability to rescue the misfolding and the associated pathogenic effects of aggregation-prone proteins associated with NDs. This review outlines such available systems in bacteria and yeast, whose usage will likely accelerate the pre-clinical discovery process for effective drugs against a variety of NDs with high socioeconomic impact.

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