Article
Biology
Enric Gutierrez-Martinez, Susana Benet Garrabe, Nicolas Mateos, Itziar Erkizia, Jon Ander Nieto-Garai, Maier Lorizate, Kyra J. E. Borgman, Carlo Manzo, Felix Campelo, Nuria Izquierdo-Useros, Javier Martinez-Picado, Maria F. Garcia-Parajo
Summary: The immunoglobulin-like lectin receptor CD169 (Siglec-1) on activated dendritic cells (DCs) mediates the capture of HIV-1 through binding to sialylated ligands. Activation of DCs leads to basal nanoclustering of Siglec-1, which enhances the receptor's avidity to gangliosides carrying sialic ligands. This facilitates the accumulation of viral particles in a single compartment.
Article
Biochemistry & Molecular Biology
Kolin M. Clark, Josh G. Kim, Qiankun Wang, Hongbo Gao, Rachel M. Presti, Liang Shan
Summary: The sensitization of the CARD8 inflammasome to non-nucleoside reverse transcriptase inhibitors (NNRTIs) can be achieved through chemical inhibition of the negative regulator DPP9. The DPP9 inhibitor Val-boroPro (VbP) can kill HIV-1-infected cells without NNRTIs and synergize with NNRTIs to promote clearance of infected cells. This offers a promising strategy for enhancing NNRTI efficacy in eliminating HIV-1 reservoirs.
NATURE CHEMICAL BIOLOGY
(2023)
Article
Multidisciplinary Sciences
Betty Ha, Kevin P. Larsen, Jingji Zhang, Ziao Fu, Elizabeth Montabana, Lynnette N. Jackson, Dong-Hua Chen, Elisabetta Viani Puglisi
Summary: The reverse transcription of HIV-1 is a crucial step in virus replication, initiated by reverse transcriptase from a host tRNA(3)(Lys) primer and targeted by antivirals like NNRTIs. High-resolution structures of the RTIC are needed to understand initiation, where discrete pausing events occur. The study presents cryo-EM structures of the core RTIC and RTIC with NNRTIs, showing a basis for rapid dissociation of RT and a mechanism of nucleic acid stabilization during initiation. NNRTIs inhibit RTIC and exacerbate pausing during reverse transcription initiation.
NATURE COMMUNICATIONS
(2021)
Article
Biochemistry & Molecular Biology
Xianwen Yang, Zhihui He, Yue Zheng, Ning Wang, Martin Mulinge, Jean-Claude Schmit, Andre Steinmetz, Carole Seguin-Devaux
Summary: Three new compounds were isolated from Cassia abbreviata, with Cassiabrevone being a heterodimer of guibourtinidol and planchol A. These compounds, along with others, showed potent anti-HIV-1 activity.
Article
Microbiology
Grant Eilers, Kushol D. Gupta, Audrey Allen, Saira E. Montermoso, Hemma J. Murali, Robert E. Sharp, Young J. Hwang, Frederic D. E. Bushman, Gregory J. Van Duyne
Summary: HIV integrase plays a crucial role in viral replication by inserting viral DNA into the host genome. Strand transfer inhibitors (STIs) and allosteric inhibitors of integrase (ALLINIs) are two major classes of antivirals that target integrase. In this study, we determined the crystal structure of the minimal ternary complex between the catalytic core domain (CCD), carboxy-terminal domain (CTD), and the ALLINI BI-224436, providing insights for improving ALLINI design and minimizing resistance.
Article
Multidisciplinary Sciences
Jerry Joe E. K. Harrison, Dario Oliveira Passos, Jessica F. Bruhn, Joseph D. Bauman, Lynda Tuberty, Jeffrey J. DeStefano, Francesc Xavier Ruiz, Dmitry Lyumkis, Eddy Arnold
Summary: In this study, the cryo-electron microscopy structure of stable HIV-1 Pol was determined, revealing that RT in the Pol has a similar arrangement to the mature RT heterodimer. The dimerization of RT may activate proteolytic processing by bringing two PR monomers together. This finding suggests that HIV-1 leverages the dimerization interfaces in Pol to regulate assembly and maturation of polyprotein precursors.
Article
Biochemical Research Methods
Dominik Schauenburg, Fabian Zech, Astrid Johanna Heck, Pascal von Maltitz, Mirja Harms, Siska Fuehrer, Nico Alleva, Jan Muench, Seah Ling Kuan, Frank Kirchhoff, Tanja Weil
Summary: Viral infections are a major threat to human health and require effective antiviral strategies. Antiviral peptides have emerged as a promising therapeutic approach due to their unique properties and mechanisms of action. In this study, we developed a chemical strategy to assemble a heterodimeric peptide conjugate on a protein-based nanoplatform, combining two optimized peptides that inhibit HIV-1 by distinct mechanisms. The constructed peptide showed increased activity against different variants of HIV-1, demonstrating the potential of assembling peptides with different modes of action on nanoplatforms to enhance antiviral activity.
BIOCONJUGATE CHEMISTRY
(2023)
Review
Optics
Mingwei Tang, Yubing Han, Danchen Jia, Qing Yang, Ji-Xin Cheng
Summary: Far-field chemical microscopy, with molecular electronic or vibrational fingerprint information, offers a new perspective for studying three-dimensional biological, material, and chemical systems. Despite the limitation of optics, recent advances in super-resolution techniques have overcome this hurdle, pushing the boundaries of far-field chemical microscopy in terms of spatial resolution. This technique finds applications in various fields including biomedical research, material characterization, environmental study, cultural heritage conservation, and integrated chip inspection.
LIGHT-SCIENCE & APPLICATIONS
(2023)
Article
Biochemistry & Molecular Biology
Sha Hu, Jiong Chen, Jin-Xu Cao, Shuang-Shuang Zhang, Shuang-Xi Gu, Fen-Er Chen
Summary: This review highlights the potential importance of quinolines and isoquinolines as anti-HIV agents, presenting the advances in diverse chemical structures and biological activity of quinoline compounds acting on different targets. It aims to provide useful references and inspirations for medicinal chemists in designing and developing novel HIV inhibitors.
BIOORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Gregory J. Bedwell, Sooin Jang, Wen Li, Parmit K. Singh, Alan N. Engelman
Summary: Research reveals that HIV-1 integration favors recurrent integration gene targets and genic proviruses can promote cell survival in vivo. Despite HIV-1 preference for integrating cancer-related genes, genic proviruses play a limited role in directly affecting cell proliferation.
NUCLEIC ACIDS RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Yali Sang, Christophe Pannecouque, Erik De Clercq, Chunlin Zhuang, Fener Chen
Summary: Fifteen naphthyl-carboxamide-DAPYs were generated to explore chemical space in reverse transcriptase (RT) binding site via lead optimization strategy. They displayed high inhibitory activity against wildtype (WT) and rilpivirine-associated resistant mutant E138K viruses, with compound a1 showing exceptionally inhibitory effects. Molecular docking analysis elucidated the biological activity and offered a structural insight for follow-up research.
BIOORGANIC CHEMISTRY
(2021)
Article
Environmental Sciences
Anna Balenzano, Francesco Mattia, Giuseppe Satalino, Francesco P. Lovergine, Davide Palmisano, Jian Peng, Philip Marzahn, Urs Wegmuller, Oliver Cartus, Katarzyna Dabrowska-Zielinska, Jan P. Musial, Malcolm W. J. Davidson, Valentijn R. N. Pauwels, Michael H. Cosh, Heather McNairn, Joel T. Johnson, Jeffrey P. Walker, Simon H. Yueh, Dara Entekhabi, Yann H. Kerr, Thomas J. Jackson
Summary: This study evaluates a pre-operational soil moisture product at 1 km resolution derived from Sentinel-1 radar satellite data. The retrieval algorithm relies on short term change detection using SAR imaging. Results show that for dense hydrological networks, the RMSE and correlation are around 0.06 m(3)/m(3) and 0.71, respectively, while in sparse networks, the RMSE increases by approximately 0.02 m(3)/m(3) (70% Confidence Level). Globally, the S-1 Theta product has an intrinsic RMSE of about 0.07 m(3)/m(3) and a correlation of 0.54.
REMOTE SENSING OF ENVIRONMENT
(2021)
Article
Immunology
Poonam Suryawanshi, Rajani Bagul, Ashwini Shete, Madhuri Thakar
Summary: The study demonstrated that HIV-1 Env could serve as a latency reversal agent (LRA), and only ADCC mediating antibodies were able to kill the reactivated HIV reservoirs. The findings have implications in designing antibody-mediated immunotherapy for eradicating latent HIV reservoir.
FRONTIERS IN IMMUNOLOGY
(2021)
Article
Microbiology
Jyothi K. Rajashekar, Jonathan Richard, Jagadish Beloor, Jeremie Prevost, Sai Priya Anand, Guillaume Beaudoin-Bussieres, Liang Shan, Dietmar Herndler-Brandstetter, Gabrielle Gendron-Lepage, Halima Medjahed, Catherine Bourassa, Fleur Gaudette, Irfan Ullah, Kelly Symmes, Andrew Peric, Emily Lindemuth, Frederic Bibollet-Ruche, Jun Park, Hung-Ching Chen, Daniel E. Kaufmann, Beatrice H. Hahn, Joseph Sodroski, Marzena Pazgier, Richard A. Flavell, Amos B. Smith, Andres Finzi, Priti Kumar
Summary: Research has shown that CD4mc can sensitize HIV-1-infected cells to ADCC by facilitating antibody recognition of epitopes on the viral envelope that are otherwise occluded. Combining CD4mc with specific antibodies can reduce viral replication and reservoir size by enhancing ADCC. The dependence on NK cells and Fc effector functions for these effects highlights the importance of ADCC in combating HIV-1.
CELL HOST & MICROBE
(2021)
Article
Biochemistry & Molecular Biology
Yinyin Zhuang, Xiaoyu Shi
Summary: Super-resolution microscopy bypasses the diffraction limit of resolution and enables imaging at the molecular level. Expansion microscopy, a chemical approach that physically enlarges cells and tissues, has emerged as a new trend in super-resolution microscopy. It offers lower cost and higher imaging depth compared to optical approaches but requires a more complex procedure.
CURRENT OPINION IN STRUCTURAL BIOLOGY
(2023)
Article
Medicine, General & Internal
Qiaoli Peng, Runhong Zhou, Yuewen Wang, Meiqing Zhao, Na Liu, Shuang Li, Haode Huang, Dawei Yang, Ka-Kit Au, Hui Wang, Kwan Man, Kwok-Yung Yuen, Zhiwei Chen
Summary: This study compares the immunogenicity and durability of BNT162b2-mRNA and CoronaVac-inactivated vaccines in fully vaccinated individuals in Hong Kong. The results show that both vaccines induce neutralizing antibodies and spike-specific CD4 T cell responses, but CoronaVac vaccine induces lower immune responses compared to BNT162b2 vaccine. Against SARS-CoV-2 variants of concern, CoronaVac vaccine shows weaker neutralizing antibody responses compared to BNT162b2 vaccine. Three months after vaccination, neutralizing antibody levels to variants of concern decrease, along with waning memory T cell responses, especially among CoronaVac vaccine recipients.
Article
Multidisciplinary Sciences
Qian Wang, Yicheng Guo, Sho Iketani, Manoj S. Nair, Zhiteng Li, Hiroshi Mohri, Maple Wang, Jian Yu, Anthony D. Bowen, Jennifer Y. Chang, Jayesh G. Shah, Nadia Nguyen, Zhiwei Chen, Kathrine Meyers, Michael T. Yin, Magdalena E. Sobieszczyk, Zizhang Sheng, Yaoxing Huang, Lihong Liu, David D. Ho
Summary: SARS-CoV-2 Omicron subvariants BA.2.12.1 and BA.4/5 have become dominant in the United States and South Africa, raising concerns about their ability to evade neutralizing antibodies and compromise the efficacy of COVID-19 vaccines and therapeutic monoclonals. A systematic antigenic analysis reveals that BA.2.12.1 and BA.4/5 have different levels of resistance to antibodies, with BA.2.12.1 being modestly resistant and BA.4/5 being substantially resistant. Certain mutations in the spike protein facilitate antibody escape, but compromise the spike affinity for the viral receptor. Only bebtelovimab retains full potency against both subvariants.
Article
Chemistry, Medicinal
Qingqing Liu, Ka-Yi Kwan, Tianyu Cao, Bingpeng Yan, Kumar Ganesan, Lei Jia, Feng Zhang, Chunyu Lim, Yaobin Wu, Yibin Feng, Zhiwei Chen, Li Liu, Jianping Chen
Summary: The percolation extract of Spatholobus suberectus Dunn (SSP) was found to have broad-spectrum viral entry inhibitory activity against SARS-CoV-1/2 and other enveloped viruses. In vivo studies showed no abnormal toxicity or behavior in long-term SSP treatment. These findings suggest that SSP has the potential to be developed as a drug candidate for preventing and treating COVID-19 and other emerging enveloped viruses.
PHYTOTHERAPY RESEARCH
(2022)
Article
Multidisciplinary Sciences
Biao Zhou, Runhong Zhou, Bingjie Tang, Jasper Fuk-Woo Chan, Mengxiao Luo, Qiaoli Peng, Shuofeng Yuan, Hang Liu, Bobo Wing-Yee Mok, Bohao Chen, Pui Wang, Vincent Kwok-Man Poon, Hin Chu, Chris Chung-Sing Chan, Jessica Oi-Ling Tsang, Chris Chun-Yiu Chan, Ka-Kit Au, Hiu-On Man, Lu Lu, Kelvin Kai-Wang To, Honglin Chen, Kwok-Yung Yuen, Shangyu Dang, Zhiwei Chen
Summary: Here, researchers successfully screened and isolated a broadly neutralizing antibody ZCB11 that can neutralize all variants of concern of SARS-CoV-2, showing particularly potent activity against the Omicron variant. Further studies demonstrated that ZCB11 predominantly interacts with the receptor-binding domain of the Omicron variant, blocking ACE2 binding. Prophylactic or therapeutic administration of ZCB11 protected against lung infection in animal models challenged with the Omicron variant.
NATURE COMMUNICATIONS
(2022)
Article
Gastroenterology & Hepatology
Zhiwu Tan, Mei Sum Chiu, Xinxiang Yang, Ming Yue, Tan To Cheung, Dongyan Zhou, Yuewen Wang, Anthony Wing-Hung Chan, Chi Wing Yan, Ka Yi Kwan, Yik Chun Wong, Xin Li, Jingying Zhou, Ka Fai To, Jiye Zhu, Chung Mau Lo, Alfred Sze-Lok Cheng, Stephen Lam Chan, Li Liu, You-Qiang Song, Kwan Man, Zhiwei Chen
Summary: A PD-1 isoform called Delta 42PD-1 plays an important role in the development and resistance to nivolumab immune checkpoint blockade (ICB) in hepatocellular carcinoma (HCC). We investigated the role of Delta 42PD-1 in HCC patients and found that Delta 42PD-1(+) T cells accounted for up to 71% of cytotoxic T lymphocytes in untreated HCC patients and were associated with HCC severity. These Delta 42PD-1(+) T cells were more exhausted than PD-1(+) T cells. HCC patients treated with anti-PD-1 ICB showed increased frequencies of Delta 42PD-1(+) T cells over time, especially in patients with progressive disease. Delta 42PD-1(+) T cells sustained HCC through toll-like receptor 4 signaling. An anti-Delta 42PD-1 antibody inhibited tumor growth in murine HCC models.
Article
Virology
Fang Zhao, Zhiwei Chen, Hui Wang, Allen Ka Loon Cheung
Summary: This study found that the presence of human cytomegalovirus (HCMV) in urine is associated with early prognosis of end-organ diseases (EODs) in patients with stage 2/3 HIV-1 infection. The detection of HCMV in urine should be implemented as a routine test.
JOURNAL OF CLINICAL VIROLOGY
(2023)
Article
Immunology
Mengxiao Luo, Biao Zhou, Eswar R. Reddem, Bingjie Tang, Bohao Chen, Runhong Zhou, Hang Liu, Lihong Liu, Phinikoula S. Katsamba, Ka-Kit Au, Hiu-On Man, Kelvin Kai-Wang To, Kwok-Yung Yuen, Lawrence Shapiro, Shangyu Dang, David D. Ho, Zhiwei Chen
Summary: In this study, the diversity, potency, breadth, and structural insights of bNAbs derived from memory B cells of BNT162b2-vaccinated individuals after Omicron BA.1 breakthrough infection were determined. The infection activated diverse memory B cell clonotypes that generated potent class I/II and III bNAbs with new epitopes mapped to the receptor-binding domain (RBD). While the top eight bNAbs neutralized wildtype and BA.1 effectively, they displayed different IgH/IgL sequences and neutralization profiles against other variants of concern (VOCs). Two class III NAbs, P2D9 and P3E6, showed comparable potency against BA.4/BA.5, but structural analysis revealed distinct modes of action. P3E6 neutralized all tested variants through a unique bivalent interaction with two RBDs. These findings provide new insights into the hybrid immunity generated by BNT162b2-induced diverse memory B cells in response to Omicron breakthrough infection.
EMERGING MICROBES & INFECTIONS
(2023)
Article
Chemistry, Multidisciplinary
Zhiwei Chen, Yaoji Sun, Jiawei Wang, Xi Zhou, Xiangjian Kong, Jiashen Meng, Xingcai Zhang
Summary: The intelligent responsive drug delivery system has great potential in cancer precision therapy by intelligently releasing antitumor drugs through pH response and thermal stimulation.
Article
Virology
Lok Yan Yim, Ka Shing Lam, Tsz-Yat Luk, Yufei Mo, Xiaofan Lu, Jinlin Wang, Ka-Wai Cheung, Grace Chung Yan Lui, Denise Pui Chung Chan, Bonnie Chun Kwan Wong, Thomas Tsz-Kan Lau, Chiu Bong Ngan, Dongyan Zhou, Yik Chun Wong, Zhiwu Tan, Li Liu, Hao Wu, Tong Zhang, Shui Shan Lee, Zhiwei Chen
Summary: The study reveals that plasma transforming growth factor beta (TGF-beta) is elevated during acute HIV-1 infection in men who have sex with men (MSM). TGF-beta signaling plays a crucial role in mediating HIV-1 infection of activated and resting memory CD4(+) T cells by upregulating the HIV-1 coreceptor CCR5. TGF-beta also increases CCR7 and CXCR3 expression on memory CD4(+) T cells, potentially promoting viral infection and latency establishment.
JOURNAL OF VIROLOGY
(2023)
Article
Multidisciplinary Sciences
Shaofeng Deng, Ying Liu, Rachel Chun-Yee Tam, Pin Chen, Anna Jinxia Zhang, Bobo Wing-Yee Mok, Teng Long, Anja Kukic, Runhong Zhou, Haoran Xu, Wenjun Song, Jasper Fuk-Woo Chan, Kelvin Kai-Wang To, Zhiwei Chen, Kwok-Yung Yuen, Pui Wang, Honglin Chen
Summary: Current available vaccines for COVID-19 are effective in reducing severe diseases and deaths caused by SARS-CoV-2 infection but less optimal in preventing infection. Next-generation vaccines which are able to induce mucosal immunity in the upper respiratory to prevent or reduce infections caused by highly transmissible variants of SARS-CoV-2 are urgently needed. We have developed an intranasal vaccine candidate based on a live attenuated influenza virus (LAIV) with a deleted NS1 gene that encodes cell surface expression of the receptor-binding-domain (RBD) of the SARS-CoV-2 spike protein, designated DelNS1-RBD4N-DAF. Immune responses and protection against virus challenge following intranasal administration of DelNS1-RBD4N-DAF vaccines were analyzed in mice and compared with intramuscular injection of the BioNTech BNT162b2 mRNA vaccine in hamsters. DelNS1-RBD4N-DAF LAIVs induced high levels of neutralizing antibodies against various SARS-CoV-2 variants in mice and hamsters and stimulated robust T cell responses in mice. Notably, vaccination with DelNS1-RBD4N-DAF LAIVs, but not BNT162b2 mRNA, prevented replication of SARS-CoV-2 variants, including Delta and Omicron BA.2, in the respiratory tissues of animals. The DelNS1-RBD4N-DAF LAIV system warrants further evaluation in humans for the control of SARS-CoV-2 transmission and, more significantly, for creating dual function vaccines against both influenza and COVID-19 for use in annual vaccination strategies.
NATURE COMMUNICATIONS
(2023)
Article
Engineering, Biomedical
Shuxun Chen, Zhiwu Tan, Pan Liao, Yanfang Li, Yun Qu, Qi Zhang, Mingxuan Yang, Kannie Wai Yan Chan, Li Zhang, Kwan Man, Zhiwei Chen, Dong Sun
Summary: This study reports the fabrication of biocompatible and biodegradable GelMA microrobots through two-photon polymerization, and demonstrates programmed degradation and drug release by varying the local exposure dose. The GelMA microspheres are further functionalized for the delivery of DNA vaccines to dendritic cells and primary cells, leading to fast, enhanced, and durable antigen expression in mice.
ADVANCED HEALTHCARE MATERIALS
(2023)
Editorial Material
Microbiology
Jiasheng Zhou, Shibo Jiang, Tongqing Zhou, Zhiwei Chen, Xia Jin, Wenyan Zhang, Supachai Rerks-ngarm, Anna Kramvis, Kai Deng, Linqi Zhang
FRONTIERS IN MICROBIOLOGY
(2023)
Article
Immunology
Ruiqi Zhang, Kwok-Hung Chan, Pui Wang, Runhong Zhou, Henry Kwong-Chi Yau, Creany Ka-Wai Wong, Meena Wai-Lam Au, Anthony Raymond Tam, Chi-Tao Ng, Matthew Kwok-Chung Lou, Na Liu, Haode Huang, Shaofeng Deng, Rachel Chun-Yee Tam, Ying Liu, Teng Long, Hoi-Wah Tsoi, Miko K. W. Ng, Jian-Piao Cai, Kelvin Kai-Wang To, Man-Fung Yuen, Zhiwei Chen, Honglin Chen, Kwok-Yung Yuen, Ivan Fan-Ngai Hung
Summary: An intranasal COVID-19 vaccine, DelNS1-based RBD vaccines composed of H1N1 subtype (DelNS1-nCoV-RBD LAIV) was developed and tested for safety and immunogenicity in healthy adults. The study recruited 29 participants who were randomly assigned to receive the low or high dose vaccine or a placebo. The vaccine showed moderate mucosal immunogenicity and was well-tolerated, indicating the need for further clinical trials.
Article
Health Care Sciences & Services
Runhong Zhou, Na Liu, Xin Li, Qiaoli Peng, Cheuk-Kwan Yiu, Haode Huang, Dawei Yang, Zhenglong Du, Hau-Yee Kwok, Ka-Kit Au, Jian-Piao Cai, Ivan Fan-Ngai Hung, Kelvin Kai -Wang To, Xiaoning Xu, Kwok-Yung Yuen, Zhiwei Chen
Summary: The ongoing outbreak of SARS-CoV-2 Omicron BA.2 infections in Hong Kong, the model city of universal masking of the world, has resulted in a major public health crisis. The timely third-dose vaccination provided significant protection with lower incidence rates of breakthrough infections. Third-dose vaccination activated spike (S)-specific memory B cells and Omicron cross-reactive T cell responses, which correlated with reduced frequencies of breakthrough infections and disease severity.
LANCET REGIONAL HEALTH-WESTERN PACIFIC
(2023)
Review
Immunology
Haoran Xu, Runhong Zhou, Zhiwei Chen
Summary: This article discusses the unique role of TRM cells in immune defense, explores the cellular mechanisms underlying their development and their responsiveness in different tissue microenvironments, and emphasizes the translational potential of TRM cells and their applications in disease protection.
CLINICAL AND EXPERIMENTAL IMMUNOLOGY
(2023)
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
