Article
Chemistry, Medicinal
Zhilan Zhou, Jifa Zhang, Enda Zhou, Changyu Ren, Jiaxing Wang, Yuxi Wang
Summary: HCV infection is a global health problem, and developing small-molecule inhibitors targeting NS5B RdRp is of great value. Non-nucleoside inhibitors have more flexible structures and simpler mechanisms compared to nucleoside inhibitors.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Chikara Dohno, Masaki Hagihara, Nursakinah Binti Mohd Zaifuddin, Mizuki Nihei, Kaoru Saito, Kazuhiko Nakatani
Summary: It was demonstrated that a synthetic ligand NA selectively binding to a 5'-CAG-3'/5'-CAG-3' triad induced repeat contractions during DNA polymerase-mediated primer extension through the CAG repeat template. Analysis using capillary electrophoresis and sequencing showed that the d(CAG)(20) template generated shortened nascent strands mainly containing 3-6 CTG units in the presence of NA.
CHEMICAL COMMUNICATIONS
(2021)
Review
Medicine, General & Internal
Jianjing Lin, Shicheng Jia, Weifei Zhang, Mengyuan Nian, Peng Liu, Li Yang, Jianwei Zuo, Wei Li, Hui Zeng, Xintao Zhang
Summary: Osteoarthritis is a degenerative disease characterized by joint pain, caused by factors such as fibrosis, chapping, ulcers, and loss of articular cartilage. Traditional treatments only delay its progression, while small molecule inhibitors targeting proteins show promising effects in managing osteoarthritis. This review examines small molecule inhibitors targeting various proteins and discusses disease-modifying osteoarthritis drugs based on them, providing valuable insights for the treatment of osteoarthritis.
JOURNAL OF CLINICAL MEDICINE
(2023)
Article
Biochemistry & Molecular Biology
Yilun Sun, Jiji Chen, Yves Pommier
Summary: Topoisomerases and PARP are crucial nuclear enzymes for DNA metabolisms, and also targets of anti-tumor chemotherapeutics. We developed an imaging-based approach to monitor real-time trapping of TOPccs and PARP1 in live cells at the single-molecule level. This technique can help elucidate the molecular processes and facilitate the development of new therapies.
NUCLEIC ACIDS RESEARCH
(2023)
Review
Biochemistry & Molecular Biology
Fan Yang, Zhigang Hu, Zhigang Guo
Summary: DNA damage repair is crucial for maintaining genomic stability and integrity, and FEN1 plays a critical role in this process. Abnormal expression or mutation of FEN1 is associated with various diseases, including cancers, making it a therapeutic target for cancer treatment. Small-molecule compounds targeting FEN1 have been developed and show promise in cancer therapy.
Review
Pharmacology & Pharmacy
Ava Safaroghli-Azar, Fatemeh Emadi, Jimma Lenjisa, Laychiluh Mekonnen, Shudong Wang
Summary: As the fifth pillar of cancer treatment, immunotherapy has revolutionized therapeutic strategies by focusing on the host's immune system. The discovery of immune-modulatory effects for kinase inhibitors has opened up new possibilities in this approach, as these small molecule inhibitors not only directly target essential proteins for tumor survival and proliferation, but also stimulate immune responses against malignant cells.
DRUG DISCOVERY TODAY
(2023)
Article
Chemistry, Medicinal
Yuqin Lei, Qi An, Xiao-Fei Shen, Min Sui, Chungen Li, Da Jia, Youfu Luo, Qingxiang Sun
Summary: The research team successfully designed a noncovalent CRM1 inhibitor with high affinity for human and yeast CRM1 through crystal structure studies, showing superior properties compared to covalent inhibitors. This discovery opens up new avenues for the development of more effective, less toxic, and broad-spectrum anticancer/antiviral therapies.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Pharmacology & Pharmacy
Yinrong Wu, Zichao Yang, Kui Cheng, Huichang Bi, Jianjun Chen
Summary: Immunotherapy has revolutionized cancer treatment, with current therapies mostly based on antibodies. However, these therapies have limitations in terms of pharmacokinetics and immunogenicity. To overcome these limitations, researchers have focused on developing small molecule-based immunotherapy. This review provides an overview of the progress in small molecule-based immunomodulators for cancer therapy, including targeting PD-1/PD-L1, chemokine receptors, STING, TLR, etc. The importance of combining small molecule-based immunomodulators with therapeutic antibodies is also highlighted.
ACTA PHARMACEUTICA SINICA B
(2022)
Article
Chemistry, Medicinal
Zhouling Xie, Xiaoxiao Yang, Yajun Duan, Jihong Han, Chenzhong Liao
Summary: Kinase inhibitors have been successful in treating various diseases beyond cancer, including autoimmune diseases and inflammatory diseases. Several non-oncologic small-molecule kinase inhibitors have been approved, with more in development for different applications.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Chao Zhang, Qian Xie, Chi Cheong Wan, Zhe Jin, Chun Hu
Summary: HIV-1 integrase plays a crucial role in HIV-1 treatment, but issues like drug resistance require further research. This review discussed the structure, function, and recent advances in small-molecule inhibitors of HIV-1 integrase.
CURRENT MEDICINAL CHEMISTRY
(2021)
Article
Microbiology
Karissa J. Munoz, Ming Tan, Christine Sutterlin
Summary: Chlamydia is the most common cause of bacterial sexually transmitted infections. This bacterium infects human cells and reproduces within a cytoplasmic inclusion through an unusual developmental cycle involving two specialized forms. Small molecule inhibitors have been reported to negatively impact the inclusion, chlamydial replication, and the production of infectious progeny, but our study shows that these effects can vary and change over the course of the 48 to 72-hour intracellular infection. We propose analysis approaches to understand these inconsistent effects, including measurement at the end of infection and detailed analysis throughout the developmental cycle. We then apply this approach to investigate and compare the effects of two inhibitors on host lipid synthesis and cholesterol trafficking that affect Chlamydia.
Article
Biochemistry & Molecular Biology
Melika Loriamini, Melissa M. Lewis-Bakker, Kayluz Frias Boligan, Siming Wang, Mairead B. Holton, Lakshmi P. Kotra, Donald R. Branch
Summary: In our initial publication, we demonstrated that small molecules can inhibit phagocytosis based on in vitro testing of over 200 compounds. We found four hit molecules with pyrazole core structure in a chemical library screening. Further evaluation resulted in the selection of two lead compounds with negligible toxicity and high efficacy in inhibiting phagocytosis. The rational development of these discoveries will lead to the selection of a lead compound(s) for pre-clinical evaluation through independent synthesis and in vivo activities.
Review
Chemistry, Medicinal
Jesang Lee, Seung Bum Park
Summary: Covalent inhibitors have been accepted as a practical tool for targeting previously undruggable proteins. Despite the clinical success, there are still unmet medical needs. Categorizing and reviewing covalent inhibitors provide insights into the future development of this field.
Article
Biochemical Research Methods
Jana Van Dycke, Arno Cuvry, Jan Knickmann, Annelii Ny, Sebastian Rakers, Stefan Taube, Peter de Witte, Johan Neyts, Joana Rocha-Pereira
Summary: This study utilizes zebrafish larvae as an in vivo model to study human norovirus infection and evaluate antiviral effects and toxicities. Through steps such as virus injection and RNA quantification, viral replication of HuNoV can be studied within 3-4 days, and the antiviral effects and toxicities of small molecules can be evaluated in HuNoV-infected zebrafish larvae.
Article
Immunology
B. Uma Reddy, Nanda Kishore Routhu, Anuj Kumar
Summary: This review provides an overview of the potential anti-SARS-CoV-2 activities of plants and their bioactive compounds, highlighting their roles in inhibiting viral infection, as well as their anti-inflammatory and antioxidant properties. It also discusses plant-based therapies in various stages of clinical trials.
MICROBIAL PATHOGENESIS
(2022)
Article
Virology
Shivaprasad Shwetha, Anuj Kumar, Ranajoy Mullick, Deeptha Vasudevan, Nilanjan Mukherjee, Saumitra Das
JOURNAL OF VIROLOGY
(2015)
Article
Chemistry, Multidisciplinary
Abirami Lakshminarayanan, B. Uma Reddy, Nallani Raghav, Vijay Kumar Ravi, Anuj Kumar, Prabal K. Maiti, A. K. Sood, N. Jayaraman, Saumitra Das
Article
Immunology
Anuj Kumar, Soma Das, Ranajoy Mullick, Priyanka Lahiri, Ranjitha Tatineni, Debashree Goswami, Prasanna Bhat, Joseph Torresi, Eric James Gowans, Anjali Anoop Karande, Saumitra Das
Article
Biotechnology & Applied Microbiology
Soma Das, Ranajoy Mullick, Anuj Kumar, Himani Tandon, Mihika Bose, K. Gouthamchandra, Madhavi Chandra, Bagepally Ravishankar, M. N. Khaja, Narayanaswamy Srinivasan, Saumitra Das, Shaila Melkote Subbarao, Anjali Anoop Karande
JOURNAL OF GENERAL VIROLOGY
(2017)
Article
Oncology
Shruti Bhargava, Abhirami Visvanathan, Vikas Patil, Anuj Kumar, Santosh Kesari, Saumitra Das, Alangar S. Hegde, Arimappamagan Arivazhagan, Vani Santosh, Kumaravel Somasundaram
Article
Pharmacology & Pharmacy
B. Uma Reddy, Ranajoy Mullick, Anuj Kumar, Geetika Sharma, Paromita Bag, Chaitrali Laha Roy, Govindarajan Sudha, Himani Tandon, Pratik Dave, Ashutosh Shukla, Priyanka Srinivasan, Madhusudhan Nandhitha, Narayanaswamy Srinivasan, Saumitra Das
ANTIVIRAL RESEARCH
(2018)
Article
Infectious Diseases
Meenakshi Kar, Amul Nisheetha, Anuj Kumar, Suraj Jagtap, Jitendra Shinde, Mohit Singla, M. Saranya, Awadhesh Pandit, Anmol Chandele, Sushil K. Kabra, Sudhir Krishna, Rahul Roy, Rakesh Lodha, Chitra Pattabiraman, Guruprasad R. Medigeshi
INTERNATIONAL JOURNAL OF INFECTIOUS DISEASES
(2019)
Article
Biophysics
Sreenath Balakrishnan, Suma S. Mathad, Geetika Sharma, Shilpa R. Raju, Uma B. Reddy, Saumitra Das, G. K. Ananthasuresh
BIOPHYSICAL JOURNAL
(2019)
Article
Chemistry, Multidisciplinary
Uma B. Reddy, Himani Tandon, Manoj K. Pradhan, Harikrishnan Adhikesavan, Narayanaswamy Srinivasan, Saumitra Das, Narayanaswamy Jayaraman
Article
Biotechnology & Applied Microbiology
Arun Sankaradoss, Suraj Jagtap, Junaid Nazir, Shefta E. Moula, Ayan Modak, Joshuah Fialho, Meenakshi Iyer, Jayanthi S. Shastri, Mary Dias, Ravisekhar Gadepalli, Alisha Aggarwal, Manoj Vedpathak, Sachee Agrawal, Awadhesh Pandit, Amul Nisheetha, Anuj Kumar, Mahasweta Bordoloi, Mohamed Shafi, Bhagyashree Shelar, Swathi S. Balachandra, Tina Damodar, Moses Muia Masika, Patrick Mwaura, Omu Anzala, Kar Muthumani, Ramanathan Sowdhamini, Guruprasad R. Medigeshi, Rahul Roy, Chitra Pattabiraman, Sudhir Krishna, Easwaran Sreekumar
Summary: The study developed a DNA vaccine candidate for dengue virus by combining different serotypes of envelope protein and non-structural protein 1. The vaccine induced neutralizing antibodies and antigen-specific T cell responses in mice, and passive transfer of immune sera provided protection. This alternative strategy for dengue vaccine design shows potential for broad-spectrum protection.
Review
Immunology
Anissa Guillemin, Anuj Kumar, Melanie Wencker, Emiliano P. Ricci
Summary: Innate immunity is the first line of defense against infections and tissue damage, and it relies on a dynamic and coordinated gene expression program. Transcriptional and post-transcriptional regulatory pathways, involving RNA-binding proteins and other effectors, play crucial roles in shaping the innate immune response. Recently, microRNAs and post-transcriptional modification of RNA bases have also emerged as essential players in this process.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Immunology
B. Uma Reddy, Nanda Kishore Routhu, Anuj Kumar
Summary: This review provides an overview of the potential anti-SARS-CoV-2 activities of plants and their bioactive compounds, highlighting their roles in inhibiting viral infection, as well as their anti-inflammatory and antioxidant properties. It also discusses plant-based therapies in various stages of clinical trials.
MICROBIAL PATHOGENESIS
(2022)
Article
Multidisciplinary Sciences
Yuxin Song, Xuan-Nhi Nguyen, Anuj Kumar, Claire da Silva, Lea Picard, Lucie Etienne, Andrea Cimarelli
Summary: This study identifies Trim69 as a negative regulator of various viral infections by regulating the properties of microtubules to limit viral spread. It highlights the importance of the cytoskeleton as an unappreciated battleground in host-pathogen interactions.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2022)
Article
Nanoscience & Nanotechnology
Mousumi Beto Mukherjee, Ranajoy Mullick, B. Uma Reddy, Saumitra Das, Ashok M. Raichur
ACS APPLIED BIO MATERIALS
(2020)