Article
Endocrinology & Metabolism
Renjian Li, Ruiqing Bi, Huanyu Cai, Juan Zhao, Peng Sun, Weilong Xu, Yaru Zhou, Wei Yang, Lu Zheng, Xiao-Lin Chen, Guanghui Wang, Dongli Wang, Junfeng Liu, Huailong Teng, Guotian Li
Summary: Melatonin, a low-cost natural compound, has versatile biological functions. This study found that melatonin has a broad-spectrum fungicidal effect and can inhibit the growth and infection of plant pathogens. By suppressing the phosphorylation of Mps1, a critical protein kinase, melatonin effectively fights against fungal pathogens. Chemical modifications can improve the fungicidal activities of melatonin, showing potential for developing eco-friendly melatonin derivatives for agricultural applications.
JOURNAL OF PINEAL RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Yuning Chen, Ya-Nan Zhang, Renhong Yan, Guifeng Wang, Yuanyuan Zhang, Zhe-Rui Zhang, Yaning Li, Jianxia Ou, Wendi Chu, Zhijuan Liang, Yongmei Wang, Yi-Li Chen, Ganjun Chen, Qi Wang, Qiang Zhou, Bo Zhang, Chunhe Wang
Summary: A monoclonal antibody called 3E8 was found to block multiple coronaviruses, including SARS-CoV-2 and its variants, without affecting the physiological activities of ACE2. It also showed effectiveness in blocking SARS-CoV-2 infection and provided a potential broad-spectrum strategy against coronaviruses that use ACE2 as entry receptors.
SIGNAL TRANSDUCTION AND TARGETED THERAPY
(2021)
Article
Pharmacology & Pharmacy
Cleber C. Melo-Filho, Tesia Bobrowski, Holli-Joi Martin, Zoe Sessions, Konstantin I. Popov, Nathaniel J. Moorman, Ralph S. Baric, Eugene N. Muratov, Alexander Tropsha
Summary: This study identified highly conserved binding sites in key coronavirus proteins, providing important information for the development of broad-spectrum anti-coronaviral medications, and validated the significance of this conservation for drug discovery with existing experimental data.
ANTIVIRAL RESEARCH
(2022)
Review
Pharmacology & Pharmacy
Yuran Qiu, Yuanhao Wang, Zongtao Chai, Duan Ni, Xinyi Li, Jun Pu, Jie Chen, Jian Zhang, Shaoyong Lu, Chuan Lv, Mingfei Ji
Summary: RAS is a key oncogenic protein, and mutations in it can lead to human cancer. Recent studies have identified several phosphorylation residues in RAS protein that can regulate its activity, providing a new direction for developing anti-RAS drugs. This review summarizes the research advances in RAS phosphorylation and provides insights into therapeutic strategies.
ACTA PHARMACEUTICA SINICA B
(2021)
Article
Virology
Yuhang Zhang, Zhenjiang Zhang, Fan Zhang, Jiwen Zhang, Jun Jiao, Min Hou, Nianchao Qian, Dongming Zhao, Xiaofeng Zheng, Xu Tan
Summary: African swine fever (ASF) is a highly contagious and deadly viral disease in swine that threatens the global pig industry. This study aimed to identify potential antiviral drugs against African swine fever virus (ASFV), which is responsible for ASF. Through a luciferase reporter system driven by the p72 promoter, three potent candidates were discovered from over 3200 natural product compounds. Ailanthone (AIL) showed inhibitory effects on ASFV replication at a nanomolar concentration (IC50 ~ 15 nmol/L). The antiviral activity of AIL was found to be associated with the inhibition of the HSP90-p23 cochaperone. Additionally, AIL demonstrated antiviral activity against Zika virus and hepatitis B virus (HBV), indicating its potential as a broad-spectrum antiviral agent.
Article
Chemistry, Medicinal
Rikeshwer Prasad Dewangan, Devesh Pratap Verma, Neeraj Kumar Verma, Ankit Gupta, Garima Pant, Kalyan Mitra, Saman Habib, Jimut Kanti Ghosh
Summary: In this study, a new type of proline-rich peptide mimetic was designed and synthesized. These lipopeptides exhibited significant antimicrobial activity against resistant bacteria and demonstrated resistance against trypsin digestion. They also showed synergistic antimicrobial activity when combined with tested antibiotics. The lipopeptides were found to interact with the bacterial ribosome and inhibit protein synthesis. Furthermore, they demonstrated superior clearance of bacteria compared to a conventional antibiotic.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Yunzheng Yan, Jingjing Yang, Dian Xiao, Jiye Yin, Mengwen Song, Yijie Xu, Lei Zhao, Qingsong Dai, Yuexiang Li, Cui Wang, Zhuang Wang, Xiaofeng Ren, Xiaotong Yang, Jie Ni, Miaomiao Liu, Xiaojia Guo, Wei Li, Xingjuan Chen, Zhiqiang Liu, Ruiyuan Cao, Wu Zhong
Summary: This study found that Nafamostat (NM) has the potential to inhibit flavivirus infections. Through in vitro and in vivo experiments, researchers found that NM effectively inhibits the replication of Zika virus and other flaviviruses. Further research revealed the antiviral mechanism of NM and proposed a novel drug design approach targeting the flavivirus envelope protein.
ANTIVIRAL RESEARCH
(2022)
Article
Neurosciences
Fatima Khatoon, Shafiul Haque, Anwar Hashem, Ahmad Mahmoud, Hanaa Tashkandi, Darin Mathkor, Steve Harakeh, Badra Alghamdi, Vijay Kumar
Summary: This study adopts a network-based approach to investigate the molecular interplay between ALS and other human disorders through kinases. By identifying the relationship between kinases and diseases, as well as targeting miRNAs and drug molecules, potential therapeutic targets for ALS treatment have been proposed.
FRONTIERS IN MOLECULAR NEUROSCIENCE
(2022)
Review
Biochemistry & Molecular Biology
Edyta Janik, Marcin Niemcewicz, Marcin Podogrocki, Joanna Saluk-Bijak, Michal Bijak
Summary: COVID-19 is a respiratory disease caused by SARS-CoV-2, for which finding effective drugs remains a urgent target for the global scientific community. The pathogenesis is mainly related to virus replication and excessive immune/inflammatory response. Treatment options include antiviral and immunomodulatory/anti-inflammatory agents.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Agriculture, Multidisciplinary
Wei Gao, Yue Zhang, Rong Ye, Xin Qi, Lei Chen, Xiaoyu Liu, Liangfu Tang, Lai Chen, Hongyu Chen, Zhijin Fan
Summary: Pyruvate kinase (PK) was identified as a potential target for novel fungicides. A series of triazolothiadiazine derivatives were designed and synthesized using a ring expansion strategy and computer-aided pesticide design. Compound 6m showed similar potency to the lead compound YZK-C22 in inhibiting the growth of Rhizoctonia solani, both in vitro and in vivo. Field experiments also demonstrated that 6m had comparable efficacy to thifluzamide against R. solani.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Yan Xiong, Yue Zhong, Hyerin Yim, Xiaobao Yang, Kwang-Su Park, Ling Xie, Poulikos I. Poulikakos, Xiaoran Han, Yue Xiong, Xian Chen, Jing Liu, Jian Jin
Summary: Proteolysis Targeting Chimeras (PROTACs) are effective for degrading disease-causing proteins. A novel approach called bridged PROTAC has been developed to target undruggable proteins by bringing the protein complex close to an E3 ubiquitin ligase using a small molecule binder of the target protein's binding partner. This approach has led to the discovery of MS28, the first-in-class degrader of cyclin D1, and it shows superior degradation efficiency and proliferation inhibition compared to CDK4/6 inhibitors and degraders. The bridged PROTAC strategy could serve as a generalizable platform for targeting undruggable proteins.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2022)
Article
Microbiology
An Fang, Yueming Yuan, Baokuen Sui, Zhihui Wang, Yuan Zhang, Ming Zhou, Huanchun Chen, Zhen F. Fu, Ling Zhao
Summary: This study reveals a novel function of miRNA-200b-3p in negatively regulating IFN-I production during viral infection through MAPK pathway. Application of miR-200b-3p inhibitors exhibits potent antiviral effects. These findings provide fresh insight into host-virus interactions and reveal a potential therapeutic target for common antiviral intervention.
Article
Engineering, Biomedical
Yang Wu, Cheerlavancha Raju, Zheng Hou, Zhangyong Si, Chen Xu, Dicky Pranantyo, Kalisvar Marimuthu, Partha Pratim De, Oon Tek Ng, Kevin Pethe, En-Tang Kang, Mary B. Chan-Park
Summary: This study demonstrates the effectiveness of a novel mixed-charge copolymer brush coating in combating biofilm formation, outperforming traditional zwitterionic polymers. By utilizing oppositely charged monomers, a greater than 99% reduction in biofilm formation was achieved against various bacteria in vitro, with excellent long-term efficacy in murine infection models. These findings suggest the potential of combining readily available singly charged monomers for potent antibiofilm applications.
Article
Multidisciplinary Sciences
Chung-Yi Wu, Cheng-Wei Cheng, Chih-Chuan Kung, Kuo-Shiang Liao, Jia-Tsrong Jan, Che Ma, Chi-Huey Wong
Summary: The development of mRNA vaccines has proven to be an effective and rapid strategy to control the spread of new pathogens. mRNA vaccines with deleted glycosites in the SARS-CoV-2 spike protein elicited stronger immune responses and broader protection compared to unmodified mRNA. This study suggests that development of broad-spectrum mRNA vaccines may not be achieved with the use of expressed proteins as antigens.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2022)
Article
Chemistry, Medicinal
Run-Zhu Fan, Lin Chen, Tong Su, Wei Li, Jia-Luo Huang, Jun Sang, Gui-Hua Tang, Sheng Yin
Summary: In this study, a series of highly potent anti-TNBC small molecule compounds were isolated through bioassay-guided isolation, with 8,9-seco-ent-kaurane 6 showing promising activity and selectivity. The compounds may induce apoptosis, autophagy, and metastasis suppression in TNBC cells by inhibiting Akt, and demonstrate significant tumor growth suppression effects in vivo. These results suggest that these compounds hold potential for future development as novel anti-TNBC agents.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Virology
Ellen Wu, Yueqi Du, Xiang Gao, Jie Zhang, John Martin, Makedonka Mitreva, Lee Ratner
JOURNAL OF VIROLOGY
(2019)
Article
Gastroenterology & Hepatology
Jeffrey B. Schwimmer, Jethro S. Johnson, Jorge E. Angeles, Cynthia Behling, Patricia H. Belt, Ingrid Borecki, Craig Bross, Janis Durelle, Nidhi P. Goyal, Gavin Hamilton, Mary L. Holtz, Joel E. Lavine, Makedonka Mitreva, Kimberly P. Newton, Amy Pan, Pippa M. Simpson, Claude B. Sirlin, Erica Sodergren, Rahul Tyagi, Katherine P. Yates, George M. Weinstock, Nita H. Salzman
Article
Multidisciplinary Sciences
Rahul Tyagi, Mostafa A. Elfawal, Scott A. Wildman, Jon Helander, Christina A. Bulman, Judy Sakanari, Bruce A. Rosa, Paul J. Brindley, James W. Janetka, Raffi Aroian, Makedonka Mitreva
SCIENTIFIC REPORTS
(2019)
Review
Genetics & Heredity
Douglas P. Jasmer, Bruce A. Rosa, Rahul Tyagi, Makedonka Mitreva
FRONTIERS IN GENETICS
(2019)
Article
Public, Environmental & Occupational Health
Mara Zambruni, Theresa J. Ochoa, Anoma Somasunderam, Miguel M. Cabada, Maria L. Morales, Makedonka Mitreva, Bruce A. Rosa, Gonzalo J. Acosta, Natalia I. Vigo, Maribel Riveros, Sara Arango, David Durand, Maitreyee N. Berends, Peter Melby, Netanya S. Utay
AMERICAN JOURNAL OF TROPICAL MEDICINE AND HYGIENE
(2019)
Article
Biochemistry & Molecular Biology
Young-Jun Choi, Santiago Fontenla, Peter U. Fischer, Thanh Hoa Le, Alicia Costabile, David Blair, Paul J. Brindley, Jose F. Tort, Miguel M. Cabada, Makedonka Mitreva
MOLECULAR BIOLOGY AND EVOLUTION
(2020)
Article
Immunology
Lucja A. Labuda, Ayola A. Adegnika, Bruce A. Rosa, John Martin, Ulysse Ateba-Ngoa, Abena Serwaa Amoah, Honorine Mbenkep Lima, Lynn Meurs, Moustapha Mbow, Mikhael D. Manurung, Jeannot F. Zinsou, Hermelijn H. Smits, Peter G. Kremsner, Makedonka Mitreva, Maria Yazdanbakhsh
JOURNAL OF INFECTIOUS DISEASES
(2020)
Article
Immunology
Jose Alberto Choreno-Parra, Suhas Bobba, Javier Rangel-Moreno, Mushtaq Ahmed, Smriti Mehra, Bruce Rosa, John Martin, Makedonka Mitreva, Deepak Kaushal, Joaquin Zuniga, Shabaana A. Khader
JOURNAL OF INFECTIOUS DISEASES
(2020)
Article
Cell Biology
Mushtaq Ahmed, Shyamala Thirunavukkarasu, Bruce A. Rosa, Kimberly A. Thomas, Shibali Das, Javier Rangel-Moreno, Lan Lu, Smriti Mehra, Stanley Kimbung Mbandi, Larissa B. Thackray, Michael S. Diamond, Kenneth M. Murphy, Terry Means, John Martin, Deepak Kaushal, Thomas J. Scriba, Makedonka Mitreva, Shabaana A. Khader
SCIENCE TRANSLATIONAL MEDICINE
(2020)
Article
Multidisciplinary Sciences
Joseph R. Fauver, John Martin, Gary J. Weil, Makedonka Mitreva, Peter U. Fischer
SCIENTIFIC REPORTS
(2019)
Article
Microbiology
Bruce A. Rosa, Kathie Mihindukulasuriya, Kymberlie Hallsworth-Pepin, Aye Wollam, John Martin, Caroline Snowden, William Michael Dunne, George M. Weinstock, Carey-Ann D. Burnham, Makedonka Mitreva
Article
Infectious Diseases
Jayden Logan, Mark S. Pearson, Srikanth S. Manda, Young-Jun Choi, Matthew Field, Ramon M. Eichenberger, Jason Mulvenna, Shivashankar H. Nagaraj, Ricardo T. Fujiwara, Pedro Gazzinelli-Guimaraes, Lilian Bueno, Vitor Mati, Jeffrey M. Bethony, Makedonka Mitreva, Javier Sotillo, Alex Loukas
PLOS NEGLECTED TROPICAL DISEASES
(2020)
Article
Infectious Diseases
Douglas P. Jasmer, Bruce A. Rosa, Rahul Tyagi, Christina A. Bulman, Brenda Beerntsen, Joseph F. Urban, Judy Sakanari, Makedonka Mitreva
PLOS NEGLECTED TROPICAL DISEASES
(2020)
Article
Microbiology
Rahul Tyagi, Christina A. Bulman, Fidelis Cho-Ngwa, Chelsea Fischer, Chris Marcellino, Michelle R. Arkin, James H. McKerrow, Case W. McNamara, Matthew Mahoney, Nancy Tricoche, Shabnam Jawahar, James W. Janetka, Sara Lustigman, Judy Sakanari, Makedonka Mitreva
Summary: 18 hits with anti-macrofilaricidal activity were identified, with azoles and aspartic protease inhibitors being prioritized for further study. These drugs showed activity against Onchocerca spp. as well, with the potential to identify selective drugs that prevent adverse events in co-infected individuals.
Article
Microbiology
Liana Beld, Hyeim Jung, Christina A. Bulman, Bruce A. Rosa, Peter U. Fischer, James W. Janetka, Sara Lustigman, Judy A. Sakanari, Makedonka Mitreva
Summary: Current treatments for lymphatic filariasis and onchocerciasis are not effective in killing the adult parasitic nematodes. Researchers have found that certain HIV antiretroviral drugs, specifically aspartyl protease inhibitors, show potential in killing adult filarial nematodes. Nelfinavir had the best potency in killing the nematodes, followed by ritonavir and lopinavir. These findings suggest that these drugs could be explored as potential treatments for parasitic nematode infections.