Article
Chemistry, Medicinal
Jiahui Chen, Rui Wang, Nancy Benovich Gilby, Guo-Wei Wei
Summary: The Omicron variant of the SARS-CoV-2 virus has caused global panic due to its high infectivity and ability to escape vaccines. A comprehensive analysis using an artificial intelligence model and antibody structure analysis reveals that Omicron may be over 10 times more contagious than the original virus and has an 88% likelihood of vaccine escape. This study highlights the importance of developing mutation-proof vaccines and antibodies.
JOURNAL OF CHEMICAL INFORMATION AND MODELING
(2022)
Review
Chemistry, Medicinal
Qing-zhang Tuo, Shu-ting Zhang, Peng Lei
Summary: Ischemic stroke caused by arterial occlusion is a common type of stroke that involves multiple cell death pathways such as apoptosis, necroptosis, and autophagy. Understanding these pathways may reveal new neuroprotective interventions for ischemic stroke.
MEDICINAL RESEARCH REVIEWS
(2022)
Article
Chemistry, Medicinal
Yuto Unoh, Shota Uehara, Kenji Nakahara, Haruaki Nobori, Yukiko Yamatsu, Shiho Yamamoto, Yuki Maruyama, Yoshiyuki Taoda, Koji Kasamatsu, Takahiro Suto, Kensuke Kouki, Atsufumi Nakahashi, Sho Kawashima, Takao Sanaki, Shinsuke Toba, Kentaro Uemura, Tohru Mizutare, Shigeru Ando, Michihito Sasaki, Yasuko Orba, Hirofumi Sawa, Akihiko Sato, Takafumi Sato, Teruhisa Kato, Yuki Tachibana
Summary: S-217622 is the first oral noncovalent, nonpeptidic SARS-CoV-2 3CL protease inhibitor clinical candidate, which could be a potential oral agent for treating COVID-19.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Sheikh Mansoor, Owais Ali Wani, Jafar K. Lone, Sweeta Manhas, Navneet Kour, Pravej Alam, Ajaz Ahmad, Parvaiz Ahmad
Summary: Reactive oxygen species (ROS) are highly reactive and dangerous by-products that can cause oxidative cell death, but they also play a beneficial role in regulating biological processes. ROS are generated in various cell compartments of plants and require the action of antioxidants to scavenge them. This review provides a comprehensive overview of the fate of ROS in plants, their role in stress response, and their interaction with other signaling molecules/pathways.
Article
Chemistry, Medicinal
Rolando Cannalire, Carmen Cerchia, Andrea R. Beccari, Francesco Saverio Di Leva, Vincenzo Summa
Summary: This article discusses the urgent need to identify drugs for treating COVID-19 and other coronavirus diseases. Different strategies targeting the virus or host cells are being investigated. The article provides a comprehensive comparative analysis of SARS-CoV-2 proteases and RdRp with other coronavirus counterparts, highlighting the most promising inhibitors reported so far and potential strategies for further development.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Mehmet Gumus, Semsi N. Babacan, Yeliz Demir, Yusuf Sert, Irfan Koca, Ilhami Gulcin
Summary: Human carbonic anhydrase (hCA) isoenzymes are zinc ion-containing metalloenzymes that play a crucial role in various diseases treatment. A novel series of compounds have been identified as highly potent inhibitors for AChE, hCA I, and hCA II, showing more effective inhibition compared to standard drugs. Compound 5f was the most effective against hCA I, compound 5e against hCA II, and compound 5c against AChE.
ARCHIV DER PHARMAZIE
(2022)
Review
Biochemistry & Molecular Biology
Anthony R. Carroll, Brent R. Copp, Rohan A. Davis, Robert A. Keyzers, Michele R. Prinsep
Summary: This review summarizes the literature on marine natural products (MNPs) published in 2020, covering a wide range of compounds isolated from various marine organisms. The focus is on new compounds discovered in 2020, including their biological activities, source organisms, and country of origin. The review also includes a meta analysis of bioactivity data for new MNPs reported in the past five years.
NATURAL PRODUCT REPORTS
(2022)
Review
Biochemistry & Molecular Biology
Giulia Barchielli, Antonella Capperucci, Damiano Tanini
Summary: Selenium is an essential microelement involved in various biological functions and plays a role in preventing and modulating several diseases. Adequate selenium nutrition and supplementation can improve prognosis and reduce disease risk.
Review
Chemistry, Medicinal
Amalia Di Petrillo, Germano Orru, Antonella Fais, Massimo C. Fantini
Summary: Quercetin, a flavonoid found in fruits and vegetables, shows potential as an antiviral agent by inhibiting virus infection, interacting with viral replication enzymes, and reducing inflammation. It can be used in combination with other drugs to enhance effects and reduce side effects. The review aims to summarize the antiviral activities of quercetin on various human viral infections.
PHYTOTHERAPY RESEARCH
(2022)
Article
Chemistry, Medicinal
Sven Ullrich, Kasuni B. Ekanayake, Gottfried Otting, Christoph Nitsche
Summary: The COVID-19 pandemic continues to pose a threat to public health, with emerging variants of SARS-CoV-2 potentially impacting the effectiveness of available vaccines. However, research suggests that the specific M-pro inhibitor nirmatrelvir remains effective against these variants.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2022)
Review
Chemistry, Medicinal
Mohammad Mahboob Alam
Summary: Recent advancements in 1,2,3-triazole hybrids have shown promising potential in the development of anticancer agents. These compounds exhibit remarkable biological potential and offer significant opportunities in combating cancer.
ARCHIV DER PHARMAZIE
(2022)
Review
Chemistry, Medicinal
Asal Jalal Abadi, Sepideh Mirzaei, Mahmood Khaksary Mahabady, Farid Hashemi, Amirhossein Zabolian, Fardin Hashemi, Pourya Raee, Shahin Aghamiri, Milad Ashrafizadeh, Amir Reza Aref, Michael R. Hamblin, Kiavash Hushmandi, Ali Zarrabi, Gautam Sethi
Summary: Curcumin, isolated from Curcuma longa, has potent tumor-suppressor activity and can decrease the adverse impacts of cisplatin (CP) while enhancing its antitumor activity. Curcumin reduces ROS levels to prevent apoptosis in normal cells, inhibits inflammation, and reduces various toxicities caused by CP. Additionally, curcumin potentiates CP cytotoxicity and suppresses tumor-promoting pathways to prevent drug resistance.
PHYTOTHERAPY RESEARCH
(2022)
Review
Biochemistry & Molecular Biology
Zhenyi Hu, Craig M. Crews
Summary: PROTACs are an emerging technology that utilizes the ubiquitin-proteasome system for targeted protein degradation, showing great therapeutic potential in treating diseases. Over the past two decades, significant advancements have been made in PROTAC technology, with an increasing repertoire of targets.
Article
Chemistry, Applied
Jaeho Kim, Moon-Moo Kim
Summary: This study found that emodin derived from Polygonum multiflorum can promote melanin production in B16F1 cells by increasing the expression levels of tyrosinase, tyrosine related protein, MITF, and SIRT1 proteins. These findings suggest that emodin may have the potential to prevent graying of hair.
NATURAL PRODUCT RESEARCH
(2022)
Article
Chemistry, Medicinal
Naoya Kitamura, Michael Dominic Sacco, Chunlong Ma, Yanmei Hu, Julia Alma Townsend, Xiangzhi Meng, Fushun Zhang, Xiujun Zhang, Mandy Ba, Tommy Szeto, Adis Kukuljac, Michael Thomas Marty, David Schultz, Sara Cherry, Yan Xiang, Yu Chen, Jun Wang
Summary: This study discovered 23R, one of the most potent and selective noncovalent SARS-CoV-2 MPpro inhibitors reported to date, and a novel binding pocket in MPpro that can be explored for inhibitor design.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Muhammad Ahsan Altaf, Rabia Shahid, Ming-Xun Ren, Safina Naz, Muhammad Mohsin Altaf, Latif Ullah Khan, Rahul Kumar Tiwari, Milan Kumar Lal, Muhammad Adnan Shahid, Ravinder Kumar, Muhammad Azher Nawaz, Mohammad Shah Jahan, Basit Latief Jan, Parvaiz Ahmad
Summary: This study investigates the defensive role of melatonin (ME) in tomato seedlings under drought stress and finds that ME can improve drought tolerance, enhance growth and photosynthesis, and strengthen antioxidant mechanisms to reduce oxidative damage.
Article
Chemistry, Medicinal
Yingjun Li, Liu Cao, Ge Li, Feng Cong, Yunfeng Li, Jing Sun, Yinzhu Luo, Guijiang Chen, Guanguan Li, Ping Wang, Fan Xing, Yanxi Ji, Jincun Zhao, Yu Zhang, Deyin Guo, Xumu Zhang
Summary: The article reports that the parent nucleoside of remdesivir, GS-441524, shows potent inhibition of SARS-CoV-2 replication and has high efficacy in reducing viral titers in infected organs without notable toxicity in animal studies.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Cecilia C. Ayala-Aguilera, Teresa Valero, Alvaro Lorente-Macias, Daniel J. Baillache, Stephen Croke, Asier Unciti-Broceta
Summary: Kinase inhibitors play a central role in the treatment of progressive disorders, with FDA approving 73 small molecule kinase inhibitor drugs by September 2021. This review summarizes the therapeutic and pharmacological properties of approved kinase inhibitors, as well as their synthesis routes, with an update on drugs approved in 2021.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Zhengnan Shen, Kiira Ratia, Laura Cooper, Deyu Kong, Hyun Lee, Youngjin Kwon, Yangfeng Li, Saad Alqarni, Fei Huang, Oleksii Dubrovskyi, Lijun Rong, Gregory R. J. Thatcher, Rui Xiong
Summary: Researchers have discovered a new antiviral drug that targets the SARS-CoV-2 papain-like protease (PLpro) to inhibit viral replication and improve antiviral potency in human cells.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Joel D. A. Tyndall
Summary: The COVID-19 pandemic has highlighted scientists' ability to respond quickly to global challenges. This article presents the discovery of the orally available 3CL protease inhibitor S-217622 through structure-based drug design, screening, and optimization by Shionogi and Hokkaido University.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
