Article
Chemistry, Multidisciplinary
Gabriele La Monica, Giuseppe Pizzolanti, Concetta Baiamonte, Alessia Bono, Federica Alamia, Francesco Mingoia, Antonino Lauria, Annamaria Martorana
Summary: RET kinase gain-of-function mutations are the main cause of high aggressiveness and invasiveness of medullary thyroid cancer. Thieno[3,2-c]quinoline compounds were identified as potential RET inhibitors with promising anticancer activity. Further studies revealed the interaction capability of these compounds with the RET tyrosine kinase domain.
Article
Biochemistry & Molecular Biology
Sonia Rocha, Mariana Lucas, Vera L. M. Silva, Pedro M. O. Gomes, Artur M. S. Silva, Alberto N. Araujo, Natalia Aniceto, Rita C. Guedes, M. Luisa Corvo, Eduarda Fernandes, Marisa Freitas
Summary: This study evaluated a library of 22 pyrazole compounds against human PTP1B activity, identifying two potent inhibitors and highlighting the importance of additional benzene rings in enhancing PTP1B inhibition. The most active compounds showed selectivity over TCPTP and molecular docking analyses revealed key residue contacts. This study represents a significant step in the design of novel PTP1B inhibitors.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Article
Biochemistry & Molecular Biology
Vyshakh M. Panakkal, Dominik Havlicek, Ewa Pavlova, Marcela Filipova, Semira Bener, Daniel Jirak, Ondrej Sedlacek
Summary: A straightforward synthetic route to highly fluorinated 19F MRI nanotracers was reported, using water-soluble fluorinated monomers and polymerization-induced self-assembly. The resulting nanoparticles exhibited strong 19F NMR/MRI signals in an aqueous environment and were confirmed to be non-toxic.
Article
Biochemistry & Molecular Biology
Kira V. V. Derkach, Maxim A. A. Gureev, Anastasia A. A. Babushkina, Vladimir N. N. Mikhaylov, Irina O. O. Zakharova, Andrey A. A. Bakhtyukov, Viktor N. N. Sorokoumov, Alexander S. S. Novikov, Mikhail Krasavin, Alexander O. O. Shpakov, Irina A. A. Balova
Summary: This article describes the identification of dual inhibitors of protein phosphotyrosine phosphatase 1B (PTP1B)/T-cell protein phosphotyrosine phosphatase (TC-PTP) based on the 3-(hydroxymethyl)-4-oxo-1,4-dihydrocinnoline scaffold. The compounds were evaluated for their effects on obesity-related parameters and gene expressions. The results indicate the potential of these compounds as dual inhibitors for the treatment of metabolic disorders.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Darshan Joshi, Rajesh Bahekar, Shubhangi Soman, Pradip Jadav, Dipam Patel, Amitgiri Goswami, Jignesh Pethani, Jeevan Kumar, Jitendra Patel, Rajesh Sundar, Poonamgiri Goswami, Krishnarup Goshdastidar, Hoshang Patel, Ankit Patel, Debdutta Bandyopadhyay, Abhijit Chattarjee, Manoranjan Sharma, Mukul Jain, Ranjit Desai
Summary: In this study, novel structural optimizations were conducted to discover effective Bruton's Tyrosine Kinase (BTK) inhibitors for the treatment of autoimmune disorders. Compound 14b was identified as a potent and selective BTK inhibitor with improved oral bioavailability. It displayed strong efficacy in in vitro and in vivo assays, making it a viable therapeutic option for autoimmune disorders.
BIOORGANIC CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Xuemei Qin, Peng Liu, Yihai Li, Liming Hu, Yexin Liao, Tingting Cao, Lifang Yang
Summary: Starting with our previously reported work, a series of novel 3,4-dihydro-2H-[1,4]oxazino[2,3-f]quinazolin-derivatives were designed, synthesized, and evaluated as potent EGFR tyrosine kinase inhibitors. All compounds showed significant inhibitory activities against EGFRwt kinase (IC50 <= 937.7 nM). Among them, compound 7j exhibited the most potent inhibitory activity with an IC50 value of 25.69 nM and demonstrated good antiproliferative activities against NCI-H1563 and H1975 cells. The tested compounds displayed low cytotoxicity against 16HBE cells in vitro. Based on the reported activity, further optimization of the structure is warranted as potential cancer treatment agents.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Biochemistry & Molecular Biology
Dongni Chen, Lan Liu, Yongjun Lu, Senhua Chen
Summary: The study isolated two new fusarielins from a marine-derived fungus, which showed significant inhibitory effects on MptpB, a crucial virulence factor of Mycobacterium tuberculosis. Fusarielin M demonstrated potential as a candidate for anti-TB drug development.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Analytical
Lihua Xu, Biling Huang, Zhiying Hou, Shaohua Huang, Yufen Zhao
Summary: This study demonstrates the simultaneous analysis of a complex mixture using solvent effects by F-19 NMR spectroscopy, which enables the identification and quantification of multiple amino acids. This method has important implications for human health and disease diagnosis.
ANALYTICAL CHEMISTRY
(2023)
Review
Psychiatry
George R. Uhl
Summary: Substance use disorders pose challenges for developing effective medications due to the complex brain and pharmacological mechanisms involved, as well as genetic and environmental factors. Medical use of stimulants and opioids requires finding a balance between minimizing their contribution to substance use disorders while retaining their benefits for various medical conditions. The data needed for assessing abuse liability and regulatory scheduling differs from that needed for licensing anti-addiction medications, adding further complexity. This article discusses the challenges in developing pentilludin as a novel anti-addiction therapeutic, targeting the protein tyrosine phosphatase D (PTPRD), which is supported by genetic and pharmacologic studies in humans and mice.
FRONTIERS IN PSYCHIATRY
(2023)
Article
Chemistry, Multidisciplinary
Xi Yang, Jinchuang Ning, Yingying Zhao, Suying Xu, Leyu Wang
Summary: A novel molecule (CFO) nanoprobe was developed for in-vivo F-19 MRI and could serve as a general fluorine labeling agent for surface functionalization of nanoparticles, providing a universal method for constructing water-soluble multifunctional nanoplatforms.
CHEMISTRY-AN ASIAN JOURNAL
(2022)
Article
Biochemistry & Molecular Biology
Chenlong Li, Huimin Zhou, Jingjiang Sun, Deshuo Wang, Jun Chang, Qingfu Wang, Yanan Li, Wei Zhao
Summary: F-19 MRI-assisted drug delivery allows for real-time monitoring and tracking of drug transportation. Amphiphilic block copolymers containing hydrophilic polyethylene glycol and F-19-containing hydrophobic segments were synthesized, with the photolysis behavior of the copolymers controlled using o-nitrobenzyl oxygen. Increasing the hydrophobic chain length enhanced drug loading capacity and photoresponsivity, while reducing chain mobility and FMRI-F-19 signal. Nanoparticles with a PTFEA polymerization degree of 10 exhibited detectable FMRI-F-19 signals and sufficient drug loading capacity (loading efficiency = 10%, cumulative release = 49%), providing a promising smart theranostic platform for F-19 MRI.
Article
Chemistry, Multidisciplinary
Bridget Tang, Katie Chong, Arthur J. Ragauskas, Robert Evans
Summary: This article introduces the collaboration between Aston University in the UK and the University of Tennessee and Oak Ridge National Laboratory in the USA, showcasing the accuracy and quantitativeness of low-field NMR spectrometers in the analysis of bio-oils. The research article is available at 10.1002/cssc.202300625.
Article
Chemistry, Organic
Anfeng Li, Xingxing Peng, Mou Jiang, Tingjuan Wu, Kexin Chen, Zhigang Yang, Shizhen Chen, Xin Zhou, Xing Zheng, Zhong-Xing Jiang
Summary: This research synthesized a series of tetra-trifluoromethylated aza-boron dipyrromethenes and systematically studied their physicochemical properties. It identified one compound with 12 symmetrical fluorines as a dual-imaging photosensitizer for photodynamic therapy.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Zhipeng Wang, Stephen F. Martin
Summary: In this study, we designed, synthesized, and evaluated two novel photocages based on the o-nitrobenzyl chemotype and carbazole ring system. The photochemical properties and decaging efficiencies of these new photocages were investigated and compared to the existing nitrodibenzofuran (NDBF) cage. The results showed that one of the new photocages exhibited significantly higher decaging efficiency than the NDBF cage. Additionally, the water solubility of one of the photocages was improved through modification, which is important for applications in aqueous conditions.
CHEMISTRY-A EUROPEAN JOURNAL
(2022)
Review
Chemistry, Multidisciplinary
Andrea Galisova, Amnon Bar-Shir
Summary: Fluorine-containing materials have greatly improved molecular and cellular MRI by providing clear and quantitative detection capabilities. These materials are based on organic molecular backbones and rely on well-defined fluorine MR signals. Recent developments include the use of ultrasmall inorganic nanocrystals as agents for F-19-MRI and the application of Chemical Exchange Saturation Transfer (CEST) to amplify signals of otherwise-undetected fluorinated entities.
CHEMICAL COMMUNICATIONS
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
Jinhao Lyu, Qi Duan, Sa Xiao, Zhihua Meng, Xiaoyan Wu, Wen Chen, Guohua Wang, Qingliang Niu, Xin Li, Yitong Bian, Dan Han, Weiting Guo, Shuai Yang, Xiangbing Bian, Yina Lan, Liuxian Wang, Tingyang Zhang, Caohui Duan, Dekang Zhang, Xueyang Wang, Ling Chen, Chenglin Tian, Xin Zhou, Xin Lou
Summary: The postlabeling delay (PLD) parameter in arterial spin labeling (ASL) is sensitive to arterial transit delays and influences cerebral blood flow measurements. This study assessed the impact of ASL acquisition at different PLDs for the quantification of penumbral tissue and compared it with dynamic susceptibility contrast MRI (DSC-MRI) as the reference method. The results showed that ASL with a PLD of 1.500 msec had a significantly larger hypoperfusion volume compared to DSC-MRI, while ASL with a PLD of 2.500 msec did not show a significant difference.
JOURNAL OF MAGNETIC RESONANCE IMAGING
(2023)
Article
Clinical Neurology
Jinhao Lyu, Sa Xiao, Zhihua Meng, Xiaoyan Wu, Wen Chen, Guohua Wang, Qingliang Niu, Xin Li, Yitong Bian, Dan Han, Weiting Guo, Shuai Yang, Xiangbing Bian, Qi Duan, Yina Lan, Liuxian Wang, Tingyang Zhang, Caohui Duan, Ling Chen, Chenglin Tian, Yuesong Pan, Xin Zhou, Xin Lou
Summary: The study aimed to propose a new imaging marker, CCR, and evaluate its predictive ability for functional outcomes in acute ischemic stroke patients using machine learning. The prediction model incorporating CCR showed improved discriminatory power in predicting unfavorable outcomes compared to the model without CCR. CCR is identified as a robust predictor of functional outcomes in patients with acute large vessel occlusion.
TRANSLATIONAL STROKE RESEARCH
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
Qian Zhou, Haidong Li, Qiuchen Rao, Ming Zhang, Xiuchao Zhao, Luyang Shen, Yuan Fang, Hongchuang Li, Xiaoling Liu, Sa Xiao, Lei Shi, Yeqing Han, Chaohui Ye, Xin Zhou
Summary: In this study, a variable-sampling-ratio compressed sensing (VCS) technique was developed to accelerate HP Xe-129 multiple b-values DW-MRI, reducing the acquisition time. The VCS technique allowed differentiation of pulmonary morphometric parameters between cigarette smokers and healthy volunteers. This method shows promise for diagnosing lung diseases in clinical practice.
Correction
Nanoscience & Nanotechnology
Lijun Zhu, Yu Li, Mou Jiang, Changsheng Ke, Hanxiong Long, Maosong Qiu, Lei Zhang, Chaohui Ye, Xin Zhou, Zhong-Xing Jiang, Shizhen Chen
ACS APPLIED MATERIALS & INTERFACES
(2023)
Article
Nanoscience & Nanotechnology
Lijun Zhu, Yu Li, Mou Jiang, Changsheng Ke, Hanxiong Long, Maosong Qiu, Lei Zhang, Chaohui Ye, Xin Zhou, Zhong-Xing Jiang, Shizhen Chen
Summary: This study developed a method to fluorinate bovine serum albumin with 34 cysteine residues, creating fluorine-19 magnetic resonance imaging (19F MRI)-traceable theranostics. The fluorinated albumin with a non-binding fluorocarbon and a long linker was found to avoid 19F signal splitting and line broadening. The self-assembled nanoparticles of paclitaxel and IR-780 showed high tumor accumulation and enabled 19F MRI-near infrared fluorescence imaging (NIR FLI)-guided synergistic chemotherapy, photothermal and photodynamic therapy.
ACS APPLIED MATERIALS & INTERFACES
(2023)
Article
Biochemical Research Methods
Caihong Tang, Yue Zeng, Jianxin Zhang, Xing Zheng, Feng Tang, Xu Yao, Zhong-Xing Jiang, Wei Shi, Wei Huang
Summary: In this study, a facile and efficient method was developed to assemble dual-site-specific ADCs with defined DARs at both the N-glycosylation site and K248 site, either with the same payloads or with two types of payloads. The constructed dual-site ADCs showed acceptable homogeneity, excellent buffer stability, and enhanced in vitro and in vivo efficiency.
BIOCONJUGATE CHEMISTRY
(2023)
Article
Engineering, Biomedical
Yu Li, Jing Zhang, Lijun Zhu, Mou Jiang, Changsheng Ke, Hanxiong Long, Ruoyun Lin, Chaohui Ye, Xin Zhou, Zhong-Xing Jiang, Shizhen Chen
Summary: Developing a theranostic system that integrates multimodal imaging, synergistic therapeutic, and formulation entities is a promising strategy for efficient cancer treatment. In this study, versatile all-in-one heptamethine cyanine amphiphiles (PEG-Cy-Fs) were developed for the convenient construction of theranostic platforms. These amphiphiles self-assembled with a chemotherapy drug tamoxifen (TAM) into stable nanoparticles (SoFoTm/PEG-Cy-F-18) with multiple capabilities, enabling the targeted chemo-photodynamic-photothermal therapy of breast cancer with high therapeutic index in mice.
ADVANCED HEALTHCARE MATERIALS
(2023)
Article
Chemistry, Multidisciplinary
Shizhen Chen, Zhong-Xing Jiang, Lan Yang, Yu Li, Changsheng Ke, Yujie Zheng, Hanxiong Long, Zhen Ouyang, Ruoyun Lin, Xin Zhou
Summary: The one-pot nucleophilic ring-opening reaction of oligoethylene glycol macrocyclic sulfates provides an efficient strategy for the monofunctionalization of oligoethylene glycols without protecting or activating group manipulation. In this strategy, the hydrolysis process is generally promoted by sulfuric acid, which is hazardous, difficult to handle, environmentally unfriendly, and unfit for industrial operation. Here, we explored a convenient handling solid acid, Amberlyst-15, as a replacement for sulfuric acid to accomplish the hydrolysis of sulfate salt intermediates. With this method, 18 valuable oligoethylene glycol derivatives were prepared with high efficiency, and gram-scale applicability of this method has been successfully demonstrated to afford a clickable oligoethylene glycol derivative 1b and a valuable building block 1g for F-19 magnetic resonance imaging traceable biomaterial construction.
Editorial Material
Chemistry, Analytical
Guanshu Liu, Xing Yang, Xin Zhou
Article
Chemistry, Multidisciplinary
Ruifang Wang, Maosong Qiu, Lei Zhang, Meiju Sui, Long Xiao, Qiao Yu, Chaohui Ye, Shizhen Chen, Xin Zhou
Summary: This study proposed a cascade-augmented nanoimmunomodulator with multienzyme-like activities for enhanced immunotherapy against cold tumors. The nanoplatform can generate oxygen radicals and deplete glutathione in the tumor microenvironment, promoting immune cell maturation and infiltration of anti-tumor cells for tumor suppression.
ADVANCED MATERIALS
(2023)
Article
Chemistry, Organic
Yuyin Mao, Na Li, Jie Liu, Zhong-Xing Jiang, Zhigang Yang
Summary: Gem-difluorinated 1,2-diazetidines were synthesized via metal-free [3+1] annulation between C,N-cyclic azomethine imines with difluorocarbene. A plausible mechanism involving the difluorocarbene pathway was proposed based on carbene trapping and control experiments. Many compounds exhibited significant antiproliferative activity.
Article
Chemistry, Physical
Xiangyu Li, Na Li, Lan Yang, Rui Jiang, Yong He, Jian Shi, Zhong-Xing Jiang, Zhigang Yang
Summary: This study demonstrates a method using metal catalysts to control switchable nucleophilic sites, and provides a strategy to construct CF3-containing thiazoles and allenes via a multicomponent reaction. The reaction is practical and convenient, compatible with various sensitive functional groups and shows high inhibitory activities against human cancer cell lines. The CF3-containing thiazoles increase the level of reactive oxygen species in MCF-7 cells, suggesting a potential mechanism for inducing tumor cell apoptosis.
Article
Chemistry, Multidisciplinary
Xin Guo, Lei Zhang, Jiesheng Hu, Balazs Szilagyi, Meng Yu, Shizhen Chen, Gyula Tircso, Xin Zhou, Jun Tao
Summary: This study investigates the magnetic-coupling effects and paraCEST properties of a homodinuclear Ni(ii) complex, showing that magnetic coupling reduces relaxation rate and enhances proton resonances, resulting in enhanced CEST efficiency. The study reveals the crucial role of magnetic coupling in optimizing the performance of paramagnetic metal complexes and provides guidance for the design of other MRI contrast agents.
