scholarly journals Targeting eukaryotic proteases for natural products-based drug development

2020 ◽  
Vol 37 (6) ◽  
pp. 827-860 ◽  
Author(s):  
Fatma H. Al-Awadhi ◽  
Hendrik Luesch
Keyword(s):  
Natural Products ◽  
Drug Development ◽  
Protease Inhibitors

This review describes the role of natural products as starting points for the development of selective protease inhibitors, examples of approved agents, the clinical and preclinical pipeline, and emerging opportunities beyond classical applications.

scholarly journals Role of Iron Chelation and Protease Inhibition of Natural Products on COVID-19 Infection

2021 ◽  
Vol 10 (11) ◽  
pp. 2306
Author(s):  
Giuseppe Carota ◽  
Simone Ronsisvalle ◽  
Federica Panarello ◽  
Daniele Tibullo ◽  
Anna Nicolosi ◽  
...  
Keyword(s):  
Natural Products ◽  
Protease Inhibitors ◽  
Respiratory Diseases ◽  
Iron Chelation ◽  
Docking Studies ◽  
Virus Infectivity ◽  
Protease Inhibition ◽  
Specific Protocol ◽  
International Attention

Although the epidemic caused by SARS-CoV-2 callings for international attention to develop new effective therapeutics, no specific protocol is yet available, leaving patients to rely on general and supportive therapies. A range of respiratory diseases, including pulmonary fibrosis, have been associated with higher iron levels that may promote the course of viral infection. Recent studies have demonstrated that some natural components could act as the first barrier against viral injury by affecting iron metabolism. Moreover, a few recent studies have proposed the combination of protease inhibitors for therapeutic use against SARS-CoV-2 infection, highlighting the role of viral protease in virus infectivity. In this regard, this review focuses on the analysis, through literature and docking studies, of a number of natural products able to counteract SARS-CoV-2 infection, acting both as iron chelators and protease inhibitors.

Wound Healing Agents: The Role of Natural and Non-Natural Products in Drug Development

2008 ◽  
Vol 8 (9) ◽  
pp. 879-888 ◽  
Author(s):  
Angelo Fatima ◽  
Luzia Modolo ◽  
Andreia Conegero Sanches ◽  
Raphael Porto
Keyword(s):  
Wound Healing ◽  
Natural Products ◽  
Drug Development

943-P: Role of Model-Informed Drug Development in Confirming Additional Clinical Benefits of Dulaglutide

Diabetes ◽  
2020 ◽  
Vol 69 (Supplement 1) ◽  
pp. 943-P
Author(s):  
LAI-SAN THAM ◽  
JEANNE GEISER ◽  
CHENG CAI TANG ◽  
KAREN SCHNECK ◽  
DAVID COX ◽  
...  
Keyword(s):  
Drug Development ◽  
Clinical Benefits

Pharmacologic Role of Vitamin D Natural Products

2014 ◽  
Vol 12 (2) ◽  
pp. 278-285 ◽  
Author(s):  
Pablo Urena-Torres ◽  
Jean Souberbielle
Keyword(s):  
Vitamin D ◽  
Natural Products

scholarly journals Cathepsin L plays a key role in SARS-CoV-2 infection in humans and humanized mice and is a promising target for new drug development

2021 ◽  
Vol 6 (1) ◽  
Author(s):  
Miao-Miao Zhao ◽  
Wei-Li Yang ◽  
Fang-Yuan Yang ◽  
Li Zhang ◽  
Wei-Jin Huang ◽  
...  
Keyword(s):  
Drug Development ◽  
Cathepsin L ◽  
Human Cells ◽  
New Drugs ◽  
Disease Course ◽  
Promising Target ◽  
First Time

AbstractTo discover new drugs to combat COVID-19, an understanding of the molecular basis of SARS-CoV-2 infection is urgently needed. Here, for the first time, we report the crucial role of cathepsin L (CTSL) in patients with COVID-19. The circulating level of CTSL was elevated after SARS-CoV-2 infection and was positively correlated with disease course and severity. Correspondingly, SARS-CoV-2 pseudovirus infection increased CTSL expression in human cells in vitro and human ACE2 transgenic mice in vivo, while CTSL overexpression, in turn, enhanced pseudovirus infection in human cells. CTSL functionally cleaved the SARS-CoV-2 spike protein and enhanced virus entry, as evidenced by CTSL overexpression and knockdown in vitro and application of CTSL inhibitor drugs in vivo. Furthermore, amantadine, a licensed anti-influenza drug, significantly inhibited CTSL activity after SARS-CoV-2 pseudovirus infection and prevented infection both in vitro and in vivo. Therefore, CTSL is a promising target for new anti-COVID-19 drug development.

scholarly journals The Role of Network Science in Glioblastoma

Cancers ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 1045
Author(s):  
Marta B. Lopes ◽  
Eduarda P. Martins ◽  
Susana Vinga ◽  
Bruno M. Costa
Keyword(s):  
Personalized Medicine ◽  
Drug Development ◽  
Information Flow ◽  
Clinical Studies ◽  
Network Science ◽  
Cancer Genomics ◽  
High Dimensional ◽  
Network Discovery ◽  
Software Implementations

Network science has long been recognized as a well-established discipline across many biological domains. In the particular case of cancer genomics, network discovery is challenged by the multitude of available high-dimensional heterogeneous views of data. Glioblastoma (GBM) is an example of such a complex and heterogeneous disease that can be tackled by network science. Identifying the architecture of molecular GBM networks is essential to understanding the information flow and better informing drug development and pre-clinical studies. Here, we review network-based strategies that have been used in the study of GBM, along with the available software implementations for reproducibility and further testing on newly coming datasets. Promising results have been obtained from both bulk and single-cell GBM data, placing network discovery at the forefront of developing a molecularly-informed-based personalized medicine.

scholarly journals Oxidation of Terpenoids to Achieve High-Value Flavor and Fragrances—Questioning Microalgae Oxidative Capabilities in the Biotransformation of the Sesquiterpene Valencene and of Selected Natural Apocarotenoids

Chemistry ◽  
2021 ◽  
Vol 3 (3) ◽  
pp. 821-830
Author(s):  
Davide De Simeis ◽  
Stefano Serra ◽  
Alessandro Di Fonzo ◽  
Francesco Secundo
Keyword(s):  
Experimental Data ◽  
Natural Products ◽  
Aqueous Medium ◽  
Photochemical Reaction ◽  
Substrate Oxidation ◽  
Market Size ◽  
Chlorella Sp ◽  
General Opinion ◽  
Natural Way

Natural flavor and fragrance market size is expected to grow steadily due to the rising consumer demand of natural ingredients. This market request is guided by the general opinion that the production of natural compounds leads to a reduction of pollution, with inherent advantages for the environment and people’s health. The biotransformation reactions have gained high relevance in the production of natural products. In this context, few pieces of research have described the role of microalgae in the oxidation of terpenoids. In this present study, we questioned the role of microalgal based oxidation in the synthesis of high-value flavors and fragrances. This study investigated the role of three different microalgae strains, Chlorella sp. (211.8b and 211.8p) and Chlorococcum sp. (JB3), in the oxidation of different terpenoid substrates: α-ionone, β-ionone, theaspirane and valencene. Unfortunately, the experimental data showed that the microalgal strains used are not responsible for the substrate oxidation. In fact, our experiments demonstrate that the transformation of the four starting compounds is a photochemical reaction that involves the oxygen as oxidant. Even though these findings cast a shadow on the use of these microorganisms for an industrial purpose, they open a new possible strategy to easily obtain nootkatone in a natural way by just using an aqueous medium, oxygen and light.

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