Article
Oncology
Murali K. Mamidi, Hasan Mahmud, Guru P. Maiti, Mariana T. Mendez, Stacey M. Fernandes, Sara K. Vesely, Jennifer Holter-Chakrabarty, Jennifer R. Brown, Asish K. Ghosh
Summary: Idelalisib targets PI3K delta in the BCR pathway in CLL patients, but only generates a partial response, indicating potential escape signals in leukemic cells. Further studies using a CLL-derived cell line, MEC1, showed that AKT activation level was restored in idelalisib-treated cells over time. It was found that targeting both PI3K delta and PI3K beta inhibited AKT reactivation, suggesting that isoform-specific inhibitors may be a more effective strategy for treating CLL patients.
Article
Chemistry, Medicinal
Nilanjan Adhikari, Tarun Jha, Balaram Ghosh
Summary: Acetylation of histone and non-histone proteins has been linked to various disease states, making histone deacetylase 3 (HDAC3) an important drug target. Despite efforts, few selective inhibitors for HDAC3 have been reported, with research discussing its role in different diseases and various potential inhibitors. This could lead to the discovery of newer, more effective, and selective HDAC3 inhibitors.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Bin Wang, Youcai Liu, Lejing Zhang, Yajuan Wang, Zhaoxi Li, Xin Chen
Summary: In this paper, a series of novel compounds were designed as selective histone deacetylase 6 inhibitors. Compound 8f showed high inhibitory activity and selectivity, as well as good antiproliferative activity against multiple tumor cells.
Article
Pharmacology & Pharmacy
Vijay Kanoje, Dilip Pandey, Akshaya Wagh, Sukanya Patra, Ajit Kumar Marisetti, Madhusudhan Reddy, Charudatt Samant, Nilesh Mahajan, Milind Gholve, Sudeep Sabde, Sneha Trivedi, Trupti Bhankhede, Vinod Patil, Prashant Nigade, Dipak Modi, Maneesh Mehta, Prajakta Ahirrao, Swathi Tota, Bidyut Nanda, Shashikant Pawar, Anuradha Polawar, Kaustubh Tamane, Sandip Kuldharan, Gururaj Vishwase, Nirmal Jana, Sachin J. Mahangare, Prashant Vidhate, Dipak Lagad, Jayasagar Gundu, Samiron Phukan, Manojkumar Shukla, Lakshmi Narasimham, Kumar V. S. Nemmani, Mandar Bhonde, Sharad Sharma, Rajender K. Kamboj, Venkata P. Palle
Summary: This study describes the in vitro and in vivo activity and drug-like properties of the PI3K delta specific inhibitor LL-00071210 in rheumatoid arthritis models. LL-00071210 shows excellent selectivity and stability, demonstrating potential as a clinical drug for the treatment of autoimmune diseases.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2022)
Article
Allergy
Marcus Maurer, William Berger, Ana Gimenez-Arnau, Koremasa Hayama, Vipul Jain, Adam Reich, Sibylle Haemmerle, Karine Lheritier, Pauline Walsh, Summer Xia, Julian Storim
Summary: Remibrutinib is highly effective in the treatment of CSU, with rapid onset of action and a favorable safety profile.
JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Pedro Novais, Patricia M. A. Silva, Joana Moreira, Andreia Palmeira, Isabel Amorim, Madalena Pinto, Honorina Cidade, Hassan Bousbaa
Summary: The study revealed the mechanism of action of diarylpentanoid BP-M345 on cancer cells, inhibiting mitosis through microtubule perturbation and causing cancer cell death, highlighting its potential as an antitumor agent.
Article
Chemistry, Medicinal
Huachao Bin, Pei Chen, Ming Wu, Falu Wang, Guifeng Lin, Shulei Pan, Jingming Liu, Bo Mu, Jinshan Nan, Qiao Huang, Linli Li, Shengyong Yang
Summary: This study reports the discovery of a potent and highly selective ATR inhibitor, SKLB-197, which demonstrated strong activity against ATR and weak or no activity against other protein kinases. SKLB-197 showed significant antitumor activity against ATM-deficient tumors both in vitro and in vivo, and it exhibited favorable pharmacokinetic properties. These findings suggest that SKLB-197 could be a promising lead compound for drug discovery targeting ATR.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Jingbo Zhang, Huimin Jiang, Songwen Lin, Deyu Wu, Hua Tian, Lin Jiang, Yiman Cui, Jing Jin, Xiaoguang Chen, Heng Xu
Summary: In this study, novel and selective PI3Kδ inhibitors were designed and synthesized, among which compound 6 showed significant anticancer activity in cellular and mouse models, making it a promising candidate for the treatment of B-cell malignancies.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Naga Rajiv Lakkaniga, Zhengyu Wang, Yao Xiao, Anupreet Kharbanda, Li Lan, Hong-yu Li
Summary: Aurora Kinase B, as a therapeutic target for cancer treatment, has been studied for more than two decades. Inhibitors of Aurora Kinase B show promising biological results in vitro and in vivo experiments. Although no approved inhibitors for clinical use are available due to associated side effects, they exhibit excellent synergy with other treatment methods, making them a potential adjuvant therapy for difficult-to-treat cancers.
MEDICINAL RESEARCH REVIEWS
(2023)
Article
Chemistry, Medicinal
Zhonghua Li, Yong Yuan, Pan Wang, Zijuan Zhang, Huifen Ma, Yiran Sun, Xiaowei Zhang, Xiaofang Li, Yonghui Qiao, Feiyu Zhang, Yunfang Su, Junying Song, Zhishen Xie, Lixin Li, Liying Ma, Jinlian Ma, Zhenqiang Zhang
Summary: In this study, a novel pool of TCP derivatives with triazolopyrimidine as a privileged heterocyclic motif was reported, which showed nanomolar inhibitory potency against LSD1 and broad-spectrum antiproliferative activities against tumor cells. Compound 9j was identified as a selective and cellular active inhibitor, and showed remarkable efficacy in reducing tumor size and extending survival in a mouse model.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Xi Zhang, Yu-ting Duan, Yi Wang, Xing-dong Zhao, Yi-ming Sun, Dong-ze Lin, Yi Chen, Yu-xiang Wang, Zu-wen Zhou, Yan-xin Liu, Li-hua Jiang, Mei-yu Geng, Jian Ding, Ling-hua Meng
Summary: The novel PI3K delta inhibitor SAF-248 exhibits high selectivity for PI3K delta and superior antiproliferative activity against DLBCL cells. It induces cell apoptosis by blocking PI3K signaling and shows dose-dependent inhibition of xenograft growth. Co-targeting mTORC1, MYC, and JAK/STAT signaling pathways enhances SAF-248's activity, making it a promising treatment option for DLBCL.
ACTA PHARMACOLOGICA SINICA
(2022)
Article
Chemistry, Medicinal
Chengbin Yang, Chenyue Xu, Zhipeng Li, Yi Chen, Tianze Wu, Hui Hong, Mingzhu Lu, Yu Jia, Yongtai Yang, Xiaofeng Liu, Mingli Deng, Zhenxia Chen, Qingquan Li, Yun Ling, Yaming Zhou
Summary: FD223, a potent and selective PI3K delta inhibitor developed based on the indole scaffold, showed high potency and selectivity against PI3K delta in AML cell lines, with favorable in vivo antitumor efficacy and no observable toxicity, indicating its potential for further development as a promising treatment for leukemia such as AML.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Xiaqiu Qiu, Yuanqing Li, Bin Yu, Jie Ren, Huidan Huang, Min Wang, Hong Ding, Zhiyu Li, Jubo Wang, Jinlei Bian
Summary: CDK9 inhibitor BAY-1143572 converted into PROTACs leads to degradation of CDK9 in acute myeloid leukemia cells, with the most potent molecule B03 showing enhanced antiproliferative activity. This enhanced activity is mediated by increased kinase inhibitory activity and apoptosis induction levels. B03 can also induce CDK9 degradation in vivo, indicating its potential as a therapeutic strategy in acute myeloid leukemia.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Yaqing Zuo, Rongrong Li, Yan Zhang, Guochen Bao, Yi Le, Longjia Yan
Summary: A series of 5-trifluoromethylpyrimidine derivatives were designed and synthesised as EGFR inhibitors, showing excellent antitumor activities, especially compound 9u. Further research revealed that compound 9u could induce cell apoptosis and arrest the cell cycle, suggesting its potential as an antitumor reagent.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Audrey L. Smith, Alexandria P. Eiken, Sydney A. Skupa, Dalia Y. Moore, Lelisse T. Umeta, Lynette M. Smith, Elizabeth R. Lyden, Christopher R. D'Angelo, Avyakta Kallam, Julie M. Vose, Tatiana G. Kutateladze, Dalia El-Gamal
Summary: This study demonstrates the preclinical efficacy of SRX3305, a novel inhibitor, in chronic lymphocytic leukemia (CLL). SRX3305 can target multiple disease-driving factors in CLL, inhibiting cell proliferation and migration.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Engineering, Biomedical
Yuyang Wei, Zhenmin Zou, Zhihui Qian, Lei Ren, Guowu Wei
Summary: Human finger joints are traditionally simplified as rigid joints in robotic hand design and biomechanical hand modelling, but the effect of different joint configurations on hand performance is not well understood. This study investigates the grasping performance of hands with rigid and flexible joints using a computational human hand model. The results show that the rigid joint configuration leads to reductions in hand contact force, pressure, and area compared to the flexible joint configuration. Grasping quality can be significantly reduced by the rigid joint configuration due to its weak rotational stiffness.
IEEE TRANSACTIONS ON NEURAL SYSTEMS AND REHABILITATION ENGINEERING
(2023)
Article
Engineering, Biomedical
Zheqi Hu, Lei Ren, Guowu Wei, Zhihui Qian, Wei Liang, Wei Chen, Xuewei Lu, Luquan Ren, Kunyang Wang
Summary: This study aims to determine the contribution of major muscles and the energy flow in the human musculoskeletal system during walking at different speeds. Gait experiments were performed, and muscle forces and mechanical work were calculated. The results showed that different muscles play different roles in energy absorption and generation during different phases of walking. These findings provide insights into human musculoskeletal behaviors during locomotion and can be applied in the bio-design of assistive devices.
IEEE TRANSACTIONS ON NEURAL SYSTEMS AND REHABILITATION ENGINEERING
(2023)
Article
Engineering, Manufacturing
Chi Ma, Bing Zhu, Zhihui Qian, Lei Ren, Hengyi Yuan, Yunhao Meng
Summary: In this study, flexible multimodal tactile sensors were fabricated using conductive inks optimized by a direct ink writing process. The rheological properties and printing speed were found to be crucial for printing conductive paths with controllable shape and good conductivity. The sensors showed excellent sensitivities for temperature, strain, and pressure, and exhibited reliability and durability through cyclic loading-unloading tests. The sensors also demonstrated great potential in health monitoring devices, flexible smart robots, and human-machine interfaces in intelligent automobiles.
JOURNAL OF MANUFACTURING PROCESSES
(2023)
Article
Medicine, General & Internal
Mai-Qing Yang, Zhi-Qiang Wang, Li-Qian Chen, Su-Mei Gao, Xing-Ning Fu, Hai-Ning Zhang, Ke-Xin Zhang, Hong-Tao Xu
Summary: This study investigated the clinicopathological characteristics of three cases of thymic lipofibroadenomas. Thymic lipofibroadenomas are extremely rare benign thymic tumors, and surgical removal is usually curative.
WORLD JOURNAL OF CLINICAL CASES
(2023)
Article
Robotics
Jianwei Sun, Zhenyu Wang, Meiling Zhang, Songyu Zhang, Zhihui Qian, Jinkui Chu
Summary: This letter proposes a design method for a metamorphic foot structure based on spring-loaded linkages, which can switch between metatarsal and toe positions. The foot mechanism's degrees of freedom are constrained using the singular position characteristic of a four-bar mechanism, and the structural parameters are calculated based on static analysis. Simulation and physical prototyping experiments verify the effectiveness of the design method, showing that the novel metamorphic foot mechanism provides a uniform solution for walking and running movements.
IEEE ROBOTICS AND AUTOMATION LETTERS
(2023)
Article
Biodiversity Conservation
Dechun Jiang, Xumao Zhao, Jordi Lopez-Pujol, Zhiqiang Wang, Yanhua Qu, Yanming Zhang, Tongzuo Zhang, Dayong Li, Ke Jiang, Bin Wang, Chaochao Yan, Jia-Tang Li
Summary: Climate change and human disturbance have been affecting the distribution of endemic vertebrate species in the Qinghai-Tibet Plateau over the past 40 years. This study used occurrence records of 19 terrestrial vertebrate species to quantify the effects of climate change and human disturbance on their distribution. The results showed that climate change had a larger impact on range variation than human disturbance, and most mammals, amphibians, and reptiles experienced an increase in their suitable geographic range.
CONSERVATION BIOLOGY
(2023)
Article
Environmental Sciences
Tian-Tian Zuo, Jia Zhu, Fei Gao, De-Juan Kong, Ji-Shuang Wang, Qing-Hui Song, Hai-Yan Wang, Lei Sun, Wan-Qiang Zhang, Yuan-Sheng Guo, Jian-Bo Yang, Feng Wei, Qi Wang, Hong-yu Jin, Shuang-Cheng Ma
Summary: This study assessed the health risks of arsenic (As) and lead (Pb) in medical earthworms by analyzing their relative bioavailability (RBA) and bioaccessibility using in vitro physiologically based extraction (PBET) assay. The results showed that As-RBA ranged from 7.2% to 45.1%, and Pb-RBA ranged from 16.1% to 49.8%. In addition, the bioaccessibility of As and Pb varied from 6.7% to 48.3% and 7.8% to 52.5%, respectively. Furthermore, strong in vivo-in vitro correlations (IVIVCs) were observed between metal-RBA and bioaccessibility in medical earthworms.
ENVIRONMENT INTERNATIONAL
(2023)
Article
Engineering, Multidisciplinary
Shengli Wang, Zhihui Qian, Xiangyu Liu, Guangsheng Song, Kunyang Wang, Jianan Wu, Jing Liu, Lei Ren, Luquan Ren
Summary: Accurate knowledge of the kinematics of the in vivo Ankle Joint Complex (AJC) is critical for understanding biomechanics and rehabilitation. However, the detailed analysis of 3D motion of the ankle joints during normal walking is lacking. This study analyzed the natural motions and coupled patterns of the tibiotalar and subtalar joints during walking, revealing significant differences in range of motion and coordinated coupled motion of the two joints.
JOURNAL OF BIONIC ENGINEERING
(2023)
Article
Oncology
Yang-kun Wang, Xue-xia Lv, Zhi-qiang Wang, Yong-mei Zhou, Bo Jiang, Su-nan Wang, Xiao-dong Chen
Summary: This study aimed to investigate the relationship between microlymphangiogenesis, microangiogenesis, and combined detection of PD-1/ki67 in gastric cancer patients and their disease prognosis. Immunohistochemistry was used to detect microlymphatic density (MLD) and microvessel density (MVD) in different zones of gastric cancer tissue, as well as the expression of PD-1 and ki67. The results showed that the central zone had fewer atretic cord-like lymphatic vessels but the peripheral zone had more lymphatic vessels, and the MLD was significantly decreased in the central zone compared to the peripheral zone. The expression of PD-1 and ki67 also differed between the zones. The differences in microlymphangiogenesis, microangiogenesis, and PD-1/ki67 expression were not statistically significant among different histological types, but were significantly decreased in early-stage gastric cancer compared to advanced-stage cancer. These findings suggest that MLD, MVD, PD-1, and ki67 are important indicators for predicting the prognosis of gastric cancer.
JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY
(2023)
Article
Critical Care Medicine
Man Li, Junqiao Lv, Zhiqiang Wang, Liping Wang, Zhixin Qin, Chen Deng, Jinming Liu, Lin Sun
Summary: HMGB1 promotes the expression of NKCC1 and NHE1 in astrocytes and endothelial cells through activation of the HMGB1-TLR4-TRIF-NF-kappa B signaling pathway, leading to cytotoxic and ionic edema following spinal cord injury. Inhibition of HMGB1 reduces the expression of NKCC1 and NHE1 and decreases spinal cord edema. These findings are important for understanding the regulation of spinal cord edema after injury.
JOURNAL OF NEUROTRAUMA
(2023)
Review
Medicine, General & Internal
Mai-Qing Yang, Zhi-Qiang Wang, Xiu-Feng Li, Li-Qian Chen, Hai-Ning Zhang, Ke-Xin Zhang, Hong-Tao Xu
Summary: This report describes a rare case of primary salivary gland-type acinic cell carcinoma (ACC) in the trachea and lungs. Due to its rarity, it can be misdiagnosed as another type of tracheal or lung tumor. Pathological features and immunohistochemistry are helpful in diagnosing primary ACC of the trachea and lungs.
Article
Nursing
Jiaojiao Sun, Yunxu Zhou, Zhiqiang Wang
Summary: This study established a depression risk warning model for patients with pulmonary nodules based on data analysis of 535 patients. Serum CRP, calcium, social support, and education level were identified as independent risk factors for depression in these patients. The model showed good predictive effect on depression in patients with pulmonary nodules.
PERSPECTIVES IN PSYCHIATRIC CARE
(2023)
Article
Oncology
Tian Wang, Jiaojiao Sun, Danfeng Gu, Siwen Shen, Yunxu Zhou, Zhiqiang Wang
Summary: The study aimed to investigate the dyadic relationships between perceived social support, illness uncertainty, anxiety, and depression among lung cancer patients and their family caregivers. A total of 308 patient-caregiver dyads were included, and questionnaires were used to assess their perceived social support, illness uncertainty, anxiety, and depression. The findings showed that both patient and caregiver perceived social support had actor and partner effects on anxiety and depression, and illness uncertainty mediated the effect of social support on anxiety and depression. Lung cancer stage played a moderating role in patient-caregiver dyads.
SUPPORTIVE CARE IN CANCER
(2023)
Article
Psychology, Developmental
Chunhua Ma, Yongfeng Ma, Youpeng Wang, Xiaoyu Lan
Summary: The present study investigated the underlying mechanism and conditional process of the positive association between bullying victimization and internalizing problems among adolescents. It found that self-esteem partially mediated this association, with bullying victimization negatively impacting self-esteem which, in turn, was negatively associated with internalizing problems. Moreover, the study revealed that peer autonomy support moderated these associations, buffering against the negative effects of bullying victimization and self-esteem on internalizing problems. These findings have important implications for early interventions and prevention efforts aimed at mitigating the adverse consequences of bullying victimization on adolescent emotional well-being.
JOURNAL OF GENETIC PSYCHOLOGY
(2023)
Article
Sport Sciences
Zhiqiang Wang, Yaping Zhong, Sugai Wang
Summary: This review examined the anthropometric, physiological, and physical profiles of elite snowboarding athletes. The findings suggest that elite speed-based and skill-based athletes generally have low body fat percentages, and differences exist in height and body mass between male speed-based and skill-based athletes. The predominant energy system in snowboarding is anaerobic metabolism, while muscle oxidative metabolism can aid in recovery. Lower-body strength, eccentric force production, and explosive concentric power production are crucial for various aspects of snowboarding performance. Further research is needed to explore anthropometry, energy system contributions, and training effects across different snowboarding disciplines.
STRENGTH AND CONDITIONING JOURNAL
(2023)