EDITORIAL: Protein Activation in Drug Discovery - Part-II

Author(s): Qi Chen, Junliang , Hao.

Journal Name: Current Topics in Medicinal Chemistry

Volume 19 , Issue 26 , 2019

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VOLUME: 19
ISSUE: 26
Year: 2019
Page: [2377 - 2377]
Pages: 1
DOI: 10.2174/156802661926191114102544



Marine Actinomycetes-derived Natural Products

(E-pub Abstract Ahead of Print)

Author(s): Chengfang Yang, Rui Qian, Yao Xu, Junxi Yi, Yiwen Gu, Xiaoyu Liu, Haobing Yu, Binghua Jiao, Xiaoling Lu, Wei Zhang*.

Journal Name: Current Topics in Medicinal Chemistry

Abstract:

Actinomycetes is an abundant resource for discovering a large number of lead compounds, which play an important role in the microbial drug discovery. Compared to terrestrial microorganisms, marine actinomycetes have unique metabolic pathways because of their special living environment, which has the potential to produce a variety of bioactive substances. In this paper, secondary metabolites isolated from marine actinomycetes are reviewed (2013-2018), most of which exhibited cytotoxic, antibacterial and antiviral biological activities.

Keywords: Marine Actinomycetes, Secondary Metabolites, Antibacterial Activity, Antiviral Activity, Cytotoxic Activity, Lead Compound

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(E-pub Abstract Ahead of Print)
DOI: 10.2174/1568026619666191114102359
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Perspectives on Anti-Candida Drug Development

Author(s): Ashok K. Dubey*, Rajeev K. Singla.

Journal Name: Current Topics in Medicinal Chemistry

Volume 19 , Issue 26 , 2019

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VOLUME: 19
ISSUE: 26
Year: 2019
Page: [2375 - 2376]
Pages: 2
DOI: 10.2174/156802661926191114102349



Meet Our Executive Guest Editor

Author(s): Qi Chen.

Journal Name: Current Topics in Medicinal Chemistry

Volume 19 , Issue 26 , 2019

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VOLUME: 19
ISSUE: 26
Year: 2019
Page: [2371 - 2372]
Pages: 2
DOI: 10.2174/156802661926191114102039



Mechanism and Development of Modern General Anesthetics

(E-pub Abstract Ahead of Print)

Author(s): Xiaoxuan Yang, Anita Luethy, Honghai Zhang, Yan Luo, Qingsheng Xue, Buwei Yu, Han Lu*.

Journal Name: Current Topics in Medicinal Chemistry

Abstract:

Background: Before October of 1846, surgery and pain were synonymous but not thereafter. Conquering pain must be one of the very few that has potentially affected every human being in the world of all milestones in medicine.

Methods: This review article describes how various general anesthetics were discovered historically and how they work in the brain to induce sedative, hypnosis and immobility. Their advantages and disadvantages will also be discussed.

Results: Anesthesia is a relatively young field but is rapidly evolving. Currently used general anesthetics are almost invariably effective, but nagging side effects, both short (e.g., cardiac depression) and long (e.g., neurotoxicity) term, have reawakened the call for new drugs.

Conclusion: Based on the deepening understanding of historical development and molecular targets and actions of modern anesthetics, novel general anesthetics are being investigated as potentially improved sedative-hypnotics or a key to understand the mechanism of anesthesia.

Keywords: General Anesthetics, Development, Mechanism, GABAA Receptors

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(E-pub Abstract Ahead of Print)
DOI: 10.2174/1568026619666191114101425
Price: $95


Current Topics in Medicinal Chemistry

Editor-in-Chief:

Allen B. Reitz
Fox Chase Chemical Diversity Center, Inc.
Doylestown, PA
USA

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A Review for Lithium: Pharmacokinetics, Drug Design and Toxicity

(E-pub Abstract Ahead of Print)

Author(s): Wen Jinhua, Darrell Sawmiller*, Brendan Wheeldon, Tan Jun.

Journal Name: CNS & Neurological Disorders - Drug Targets
(Formerly Current Drug Targets - CNS & Neurological Disorders)

Abstract:

Background: Lithium as a mood stabilizer has been used as the standard pharmacological treatment for bipolar disorder (BD) for more than 60 years. Recent studies have also shown that it has potential for treatment of many other neurodegenerative disorders, including Alzheimer’s, Parkinson’s and Huntington’s disease, through its neurotrophic, neuroprotective, antioxidant and anti-inflammatory actions. Therefore, exploring its pharmacokinetic features and designing more excellent lithium preparations are becoming important research topics.

Methods: We reviewed many studies on the pharmacokinetics, drug design and toxicity of lithium based on recent relevant research progress from PubMed, Web of Science, Elsevier and Springer databases. Keywords used for searching references were lithium, pharmacology, pharmacokinetics, drug design and toxicity.

Results: Lithium is rapidly and completely absorbed from the gastrointestinal tract after oral administration. Its level is initially highest in serum and then is evidently redistributed to various tissue compartments. It is not metabolized and over 95% of lithium is excreted unchanged through the kidney, but different lithium preparations may have different pharmacokinetics features. Lithium has a narrow therapeutic window limited by various adverse effects, but some novel drugs of lithium may overcome these problems.

Conclusion: Various formulations of lithium have potential for treating neurodegenerative brain diseases but further study on their pharmacokinetics will be required in order to determine the optimal formulation, dosage and route of administration.

Keywords: Lithium, Pharmacokinetics, Pharmacodynamics, Toxicity, Lithium Salts, Drug Design

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(E-pub Abstract Ahead of Print)
DOI: 10.2174/1871527318666191114095249
Price: $95



EDITORIAL: Current Advances of Drug Target Research in Medicinal Chemistry

Author(s): Guo-Ping Zhou.

Journal Name: Current Topics in Medicinal Chemistry

Volume 19 , Issue 25 , 2019

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VOLUME: 19
ISSUE: 25
Year: 2019
Page: [2269 - 2270]
Pages: 2
DOI: 10.2174/156802661925191114094117



Omega-3 Fatty Acids as Druggable Therapeutics for Neurodegenerative Disorders

(E-pub Abstract Ahead of Print)

Author(s): Neha Milind Chitre, Nader H. Moniri, Kevin Sean Murnane*.

Journal Name: CNS & Neurological Disorders - Drug Targets
(Formerly Current Drug Targets - CNS & Neurological Disorders)

Abstract:

Neurodegenerative disorders are commonly associated with a complex pattern of pathophysiological hallmarks including increased oxidative stress and neuroinflammation, which makes their treatment challenging. Omega-3 fatty acids (O3FA) are natural products with reported neuroprotective, anti-inflammatory, and antioxidant effects. These effects have been attributed to their incorporation into neuronal membranes or via activation of intracellular or recently discovered cell-surface receptors (i.e., free-fatty acid receptors; FFAR). Molecular docking studies have investigated the roles of O3FA as FFAR agonists and have led to the development of receptor specific targeted agonists for therapeutic purposes. Moreover, novel formulation strategies for targeted delivery of O3FA to the brain have supported their development as therapeutics for neurodegenerative disorders. Despite the compelling evidence of the beneficial effects of O3FA for several neuroprotective functions, they are currently only available as unregulated dietary supplements, with only a single FDA-approved prescription product, indicated for triglyceride reduction. This review highlights the relative safety and efficacy of O3FA, their drug-like properties, and their capacity to be formulated in clinically viable drug delivery systems. Interestingly, the presence of cardiac conditions like hypertriglyceridemia is associated with brain pathophysiological hallmarks of neurodegeneration such as neuroinflammation, thereby further suggesting potential therapeutic roles of O3FA for neurodegenerative disorders. Taken together, this review article summarizes and integrates the compelling evidence regarding the feasibility of developing O3FA and their synthetic derivatives as potential drugs for neurodegenerative disorders.

Keywords: Omega-3 Fatty Acids, Neurodegenerative Disorders, Prescription Therapies, Free Fatty Acid Receptor, Synthetic Agonists

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(E-pub Abstract Ahead of Print)
DOI: 10.2174/1871527318666191114093749
Price: $95


Current Topics in Medicinal Chemistry

Editor-in-Chief:

Allen B. Reitz
Fox Chase Chemical Diversity Center, Inc.
Doylestown, PA
USA

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