Article
Chemistry, Multidisciplinary
Jingwei Meng, Teng Fei, Jinxiong Cai, Qi Lai, Jinya Zhang, Siping Pang, Chunlin He
Summary: In this work, a novel energetic molecule DATNBP-2 was designed and synthesized, which exhibited high density, high thermal decomposition temperature, and excellent detonation performance. It outperformed traditional explosives in terms of stability.
MATERIALS CHEMISTRY FRONTIERS
(2023)
Article
Biochemistry & Molecular Biology
Pengyu Zhang, Fiorella A. Solari, Johan W. M. Heemskerk, Marijke J. E. Kuijpers, Albert Sickmann, Ulrich Walter, Kerstin Jurk
Summary: The mechanisms controlling the activities of Btk and Syk in human platelets were investigated in this study. It was found that PKC, PKA and PP2A jointly regulate the activation of Btk induced by GPVI. PKC activation promotes the tyrosine phosphorylation of Btk, while PKA activation suppresses the S180 phosphorylation of Btk and S297 phosphorylation of Syk. PP2A inhibition only increases the S297 phosphorylation of Syk. The study reveals the regulatory mechanisms of GPVI-Syk-Btk signaling pathway in human platelets.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Medicine, General & Internal
Arvind Dasari, Sara Lonardi, Rocio Garcia-Carbonero, Elena Elez, Takayuki Yoshino, Alberto Sobrero, James Yao, Pilar Garcia-Alfonso, Judit Kocsis, Antonio Cubillo Gracian, Andrea Sartore-Bianchi, Taroh Satoh, Violaine Randrian, Jiri Tomasek, Geoff Chong, Andrew Scott Paulson, Toshiki Masuishi, Jeremy Jones, Tibor Csoszi, Chiara Cremolini, Francois Ghiringhelli, Ardaman Shergill, Howard S. Hochster, John Krauss, Ali Bassam, Michel Ducreux, Anneli Elme, Laurence Faugeras, Stefan Kasper, Eric Van Cutsem, Dirk Arnold, Shivani Nanda, Zhao Yang, William R. Schelman, Marek Kania, Josep Tabernero, Cathy Eng
Summary: This study evaluated the efficacy and safety of fruquintinib, a highly selective and potent oral inhibitor of VEGFRs 1, 2, and 3, in patients with advanced, chemotherapy-refractory colorectal cancer. The results showed that fruquintinib significantly prolonged overall survival compared to placebo in patients with refractory metastatic colorectal cancer, with clinical significance. Therefore, fruquintinib could become a global treatment option for patients with refractory metastatic colorectal cancer.
Review
Chemistry, Analytical
Juan Gao, Jingyi Jian, Zhengjin Jiang, Ann Van Schepdael
Summary: Tyrosine kinases have been extensively studied as drug targets due to their regulation of cellular processes. The deregulation of tyrosine kinases plays a key role in the pathophysiology of various diseases. Several techniques, including traditional binding assays and high-throughput screening methods, have been developed to discover new tyrosine kinase inhibitors. This review provides insights into the different assay methods for the exploration of novel tyrosine kinase inhibitors.
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
(2023)
Article
Chemistry, Medicinal
Chihoko Yoshimura, Satoru Nagatoishi, Daisuke Kuroda, Yasuo Kodama, Takao Uno, Makoto Kitade, Khoontee Chong-Takata, Hiromi Oshiumi, Hiromi Muraoka, Satoshi Yamashita, Yuichi Kawai, Shuichi Ohkubo, Kouhei Tsumoto
Summary: The study on the binding characteristics of TAS-116 and its analogs revealed that interactions with the hydrophobic pocket of Hsp90 determine the potency and selectivity for the cytosolic Hsp90 isoform.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Multidisciplinary Sciences
Xinran Li, Amy Y. T. Lau, Angel S. N. Ng, Abdullah Aldehaiman, Yuan Zhou, Patrick K. S. Ng, Stefan T. Arold, Lydia W. T. Cheung
Summary: The study demonstrates that driver mutations in p85α can activate multiple kinase pathways and promote malignant growth of cancer cells. These mutations increase HER3 protein levels by inhibiting HER3 ubiquitination and degradation, leading to its heterodimerization with EGFR, HER2, and c-Met, as well as the allosteric activation of these dimerized partners.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2021)
Article
Chemistry, Multidisciplinary
Xinyuan Xi, Fan Lei, Keliang Gao, Jingjing Li, Rihe Liu, Adam R. Karpf, Tatiana K. Bronich
Summary: Combining chemotherapeutic drugs in a single nanocarrier offers advantages in cancer treatment, including reducing toxicity, improving drug properties, and enhancing therapeutic effects. In this study, we developed functional multimodal polypeptide-based polymeric nanogels (NGs) to encapsulate a combination of drugs. These NGs exhibited selective cytotoxicity towards EGFR overexpressing ovarian cancer cells and showed preferential associations with EGFR (+) tumor cells. Furthermore, ligand-installed NGs carrying the drug combination significantly improved the treatment response of ovarian cancer xenografts compared to individual drug-loaded NGs. This work highlights the potential of our carrier system for efficient delivery of drug combinations to treat EGFR overexpressing cancers.
JOURNAL OF CONTROLLED RELEASE
(2023)
Article
Materials Science, Multidisciplinary
Qi Wei, Zhijun Ning
Summary: Chiral perovskite has attracted significant attention recently for its combination of excellent optoelectronic properties of perovskite with unique chiral or spin-related optical and electrical properties. This provides new insights into traditional spin-optoelectronic and spintronic applications.
ACS MATERIALS LETTERS
(2021)
Article
Chemistry, Medicinal
Jannis Born, Tien Huynh, Astrid Stroobants, Wendy D. Cornell, Matteo Manica
Summary: The use of reduced active site sequence representation in kinase-ligand binding affinity prediction has shown significantly higher performance compared to using the full primary structure. This trend persists across different models, data sets, and performance metrics, and holds true when predicting pIC(50) for both unseen ligands and kinases.
JOURNAL OF CHEMICAL INFORMATION AND MODELING
(2022)
Review
Cell Biology
Li Chen, Xiangyi Kong, Yi Fang, Shishir Paunikar, Xiangyu Wang, James A. L. Brown, Emer Bourke, Xingrui Li, Jing Wang
Summary: Discoidin domain receptor tyrosine kinases (DDRs) are a type of receptor tyrosine kinases associated with various diseases, widely expressed in different cell types and involved in signaling pathways, closely related to the development and progression of solid tumors.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY
(2021)
Article
Multidisciplinary Sciences
Bihui Cao, Manting Liu, Lu Wang, Kangshun Zhu, Mingyue Cai, Xiaopei Chen, Yunfei Feng, Shuo Yang, Shengyu Fu, Cheng Zhi, Xiaodie Ye, Jian Zhang, Zhiru Zhang, Xin Yang, Ming Zhao, Qingde Wu, Linfeng Xu, Lili Yang, Hui Lian, Qi Zhao, Zhenfeng Zhang
Summary: The complex immunosuppressive tumor microenvironment and lack of tumor-specific targets hinder the application of CAR T cell therapy in solid tumors. AXL, highly expressed in NSCLC but not in normal tissues, might be a target for CAR T cell therapy. Combining microwave ablation and AXL-CAR T cells shows superior antitumor efficacy.
NATURE COMMUNICATIONS
(2022)
Article
Cell Biology
Chen Wang, Jie Zeng, Li-Jie Li, Min Xue, Si-Li He
Summary: The study showed that Cdc25A regulates ferroptosis in cervical cancer cells by modulating the levels of PKM2 and ErbB2, affecting the response of cervical cancer cells to sorafenib treatment.
CELL DEATH & DISEASE
(2021)
Article
Hematology
Philippe Rousselot, Luigina Mollica, Joelle Guilhot, Agnes Guerci, Franck E. Nicolini, Gabriel Etienne, Laurence Legros, Aude Charbonnier, Valerie Coiteux, Caroline Dartigeas, Martine Escoffre-Barbe, Lydia Roy, Pascale Cony-Makhoul, Viviane Dubruille, Martine Gardembas, Francoise Huguet, Delphine Rea, Emilie Cayssials, Francois Guilhot, Anne Bergeron, Mathieu Molimard, Francois-Xavier Mahon, Jean-Michel Cayuela, Lambert Busque, Stephane Bouchet
Summary: Dasatinib, a second-generation BCR-ABL1 tyrosine kinase inhibitor, is approved for CML patients. This study evaluated therapeutic drug monitoring (TDM) to reduce dasatinib-associated pleural effusion (PlEff) incidence. Results showed that TDM during dasatinib treatment initiation significantly reduced the occurrence of PlEff in the long run without affecting molecular responses.
BRITISH JOURNAL OF HAEMATOLOGY
(2021)
Article
Cell Biology
Wei-Qing Shao, Wen-Wei Zhu, Meng-Jun Luo, Ming-Hao Fan, Qin Li, Sheng-Hao Wang, Zhi-Fei Lin, Jing Zhao, Yan Zheng, Qiong-Zhu Dong, Lu Lu, Hu-Liang Jia, Ju-Bo Zhang, Ming Lu, Jin-Hong Chen, Lun-Xiu Qin
Summary: This study reveals that cholesterol suppresses the autophagic degradation of RTKs in a GOLM1-dependent manner, and lowering cholesterol by statins can enhance the efficacy of multiple tyrosine kinase inhibitors in HCC.
Article
Chemistry, Physical
Zhiwei Ma, Sheng-You Huang, Fei Cheng, Xiaoqin Zou
Summary: Efficient ensemble docking algorithm is applied to dock ligands against multiple protein targets simultaneously. Using protein kinases as an example, the algorithm is shown to be effective in screening for inhibitors and investigating their selectivities for multiple target proteins.
JOURNAL OF PHYSICAL CHEMISTRY B
(2021)
Article
Multidisciplinary Sciences
Vy Nguyen, Christopher Wilson, Marc Hoemberger, John B. Stiller, Roman V. Agafonov, Steffen Kutter, Justin English, Douglas L. Theobald, Dorothee Kern
Article
Biochemistry & Molecular Biology
Markus Niklasson, Renee Otten, Alexandra Ahlner, Cecilia Andresen, Judith Schlagnitweit, Katja Petzold, Patrik Lundstrom
JOURNAL OF BIOMOLECULAR NMR
(2017)
Article
Biotechnology & Applied Microbiology
Luke W. Koblan, Jordan L. Doman, Christopher Wilson, Jonathan M. Levy, Tristan Tay, Gregory A. Newby, Juan Pablo Maianti, Aditya Raguram, David R. Liu
NATURE BIOTECHNOLOGY
(2018)
Article
Multidisciplinary Sciences
Renee Otten, Lin Liu, Lillian R. Kenner, Michael W. Clarkson, David Mavor, Dan S. Tawfik, Dorothee Kern, James S. Fraser
NATURE COMMUNICATIONS
(2018)
Article
Biology
Warintra Pitsawong, Vanessa Buosi, Renee Otten, Roman Agafonov, Adelajda Zorba, Nadja Kern, Steffen Kutter, Gunther Kern, Ricardo A. P. Padua, Xavier Meniche, Dorothee Kern
Article
Multidisciplinary Sciences
Ricardo A. P. Padua, Yizhi Sun, Ingrid Marko, Warintra Pitsawong, John B. Stiller, Renee Otten, Dorothee Kern
NATURE COMMUNICATIONS
(2018)
Article
Multidisciplinary Sciences
Holly A. Rees, Christopher Wilson, Jordan L. Doman, David R. Liu
Article
Chemistry, Physical
John B. Stiller, S. Jordan Kerns, Marc Hoemberger, Young-Jin Cho, Renee Otten, Michael F. Hagan, Dorothee Kern
Article
Multidisciplinary Sciences
Andrew V. Anzalone, Peyton B. Randolph, Jessie R. Davis, Alexander A. Sousa, Luke W. Koblan, Jonathan M. Levy, Peter J. Chen, Christopher Wilson, Gregory A. Newby, Aditya Raguram, David R. Liu
Article
Multidisciplinary Sciences
Adelajda Hadzipasic, Christopher Wilson, Vy Nguyen, Nadja Kern, Chansik Kim, Warintra Pitsawong, Janice Villali, Yuejiao Zheng, Dorothee Kern
Article
Biochemistry & Molecular Biology
Mandana Arbab, Max W. Shen, Beverly Mok, Christopher Wilson, Zaneta Matuszek, Christopher A. Cassa, David R. Liu
Article
Biotechnology & Applied Microbiology
Christopher Wilson, Peter J. Chen, Zhuang Miao, David R. Liu
NATURE BIOTECHNOLOGY
(2020)
Article
Multidisciplinary Sciences
Luke W. Koblan, Michael R. Erdos, Christopher Wilson, Wayne A. Cabral, Jonathan M. Levy, Zheng-Mei Xiong, Urraca L. Tavarez, Lindsay M. Davison, Yantenew G. Gete, Xiaojing Mao, Gregory A. Newby, Sean P. Doherty, Narisu Narisu, Quanhu Sheng, Chad Krilow, Charles Y. Lin, Leslie B. Gordon, Kan Cao, Francis S. Collins, Jonathan D. Brown, David R. Liu
Summary: Using adenine base editor (ABE), researchers successfully corrected the pathogenic mutation in fibroblasts from children with Hutchinson-Gilford progeria syndrome, mitigating RNA mis-splicing, reducing progerin levels, and correcting nuclear abnormalities. In vivo base editing with AAV9 encoding ABE in transgenic mice resulted in substantial, durable correction of the mutation, restoration of normal RNA splicing, and improvement of vascular pathology, ultimately extending the lifespan of the mice. These findings demonstrate the potential of in vivo base editing as a treatment for genetic diseases.
Article
Multidisciplinary Sciences
Renee Otten, Ricardo A. P. Padua, H. Adrian Bunzel, Vy Nguyen, Warintra Pitsawong, MacKenzie Patterson, Shuo Sui, Sarah L. Perry, Aina E. Cohen, Donald Hilvert, Dorothee Kern
Article
Biotechnology & Applied Microbiology
Benjamin W. Thuronyi, Luke W. Koblan, Jonathan M. Levy, Wei-Hsi Yeh, Christine Zheng, Gregory A. Newby, Christopher Wilson, Mantu Bhaumik, Olga Shubina-Oleinik, Jeffrey R. Holt, David R. Liu
NATURE BIOTECHNOLOGY
(2019)