Article
Plant Sciences
Fei-Hua Yao, Xiao Liang, Xin-Hua Lu, Xia Cheng, Lian-Xiang Luo, Shu-Hua Qi
Summary: Seven new decahydrofluorene-class alkaloids, pyrrospirones K-Q (1-7), were isolated from the marine-derived fungal strain Penicillium sp. SCSIO 41512. Compound 13 exhibited significant inhibitory activity against protein tyrosine phosphatases. Moreover, compounds 1, 2, 5, 8-10, 12, and 13 showed antibacterial activity.
JOURNAL OF NATURAL PRODUCTS
(2022)
Review
Public, Environmental & Occupational Health
Deqiang Liu, Yiming Zhang, Hui Fang, Jinxiang Yuan, Lizhen Ji
Summary: Pseudophosphatases are a class of enzymes that mutate at the catalytically active site and play important roles in life processes and diseases. This review discusses the structures, action types, and signaling mechanisms of pseudophosphatases in various families.
FRONTIERS IN PUBLIC HEALTH
(2022)
Review
Cell Biology
Caroline E. Nunes-Xavier, Laura Zaldumbide, Lorena Mosteiro, Ricardo Lopez-Almaraz, Nagore Garcia de Andoin, Pablo Aguirre, Maite Emaldi, Leire Torices, Jose I. Lopez, Rafael Pulido
Summary: Neuroblastoma is a type of cancer associated with early development and differentiation of neuroendocrine cells, and PTPs play a key role in cell growth and differentiation, potentially serving as biomarkers and molecular targets for neuroblastoma therapies.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY
(2021)
Article
Chemistry, Medicinal
Ling Li, Jin Liu, Zichao Yang, Huiting Zhao, Bulian Deng, Yichang Ren, Ruiyao Mai, Junli Huang, Jianjun Chen
Summary: A series of novel thieno[2,3-d]pyrimidine analogs were designed and synthesized as KRAS G12D inhibitors. Compound KD-8 exhibited potent antiproliferative activity and antitumor efficacy by decreasing the active form of KRAS and inhibiting Raf and Erk in KRAS G12D mutated cancer cell lines.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Microbiology
Kasi Viswanatharaju Ruddraraju, Devesh Aggarwal, Zhong-Yin Zhang
Summary: Tuberculosis is an airborne infectious disease caused by Mycobacterium tuberculosis, and the treatment of drug-resistant TB requires therapeutic agents with novel mechanisms. Antivirulence, focusing on bacterial virulence factors, is an alternative strategy for treating diseases. Recent advances in understanding the roles of mPTPA and mPTPB in the pathogenesis of TB have been made, along with the discovery of potent, selective, and well-characterized small molecule inhibitors for these proteins in the past decade.
Review
Biochemistry & Molecular Biology
Malathi Bheri, Swati Mahiwal, Sibaji K. Sanyal, Girdhar K. Pandey
Summary: Protein phosphorylation and dephosphorylation are important reversible post-translational modifications, with protein phosphatases playing a key role in signaling networks. The classification and mechanism of phosphatases in plant systems still require further investigation.
Article
Health Care Sciences & Services
Federica Zito Marino, Carminia Maria Della Corte, Vincenza Ciaramella, Stefania Erra, Andrea Ronchi, Alfonso Fiorelli, Giovanni Vicidomini, Mario Santini, Giosue Scognamiglio, Floriana Morgillo, Fortunato Ciardiello, Renato Franco, Marina Accardo
Summary: Malignant pleural mesothelioma (MPM) is a highly lethal malignancy that cannot benefit from molecularly targeted therapies. This study found that the co-expression of AXL and MET receptors may play a key role in MPM patients, and the simultaneous inhibition of AXL and MET may affect the proliferation and aggressiveness of MPM cells.
JOURNAL OF PERSONALIZED MEDICINE
(2022)
Review
Multidisciplinary Sciences
Yaping Zhao, Rongrong Liu, Miaomiao Li, Pengfei Liu
Summary: Spleen tyrosine kinase (SYK) plays an important role in liver diseases by regulating signal transduction in various cells, including both hematopoietic and non-hematopoietic cells. Inhibition of SYK activity has been identified as a promising therapeutic strategy, and both hepatic and non-hepatic SYK could be potential targets for treatment. Further research is needed to better understand the significance of SYK in liver diseases and to establish more reliable treatment modes.
Review
Medicine, Research & Experimental
Xia Zhao, Li Xiong, Lingyu She, Liwei Li, Ping Huang, Guang Liang
Summary: Protein tyrosine phosphatases (PTPs) play a significant role in the pathogenesis of Alzheimer's disease (AD) and are closely related to the accumulation of abnormally phosphorylated proteins.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Review
Chemistry, Multidisciplinary
Sijun Pan, Aixiang Ding, Yisi Li, Yaxin Sun, Yueqin Zhan, Zhenkun Ye, Ning Song, Bo Peng, Lin Li, Wei Huang, Huilin Shao
Summary: Significant progress has been made in the development of small-molecule probes in the past decade. While their application in preclinical research is widespread, their clinical translation remains limited due to safety and regulatory concerns. Recent synergistic developments have integrated novel chemical probes with complementary analytical technologies, allowing for molecular characterization of targeted drug interactions directly in the human body or through clinical specimens. These developments offer unprecedented opportunities for drug development, disease diagnostics, and treatment monitoring.
CHEMICAL SOCIETY REVIEWS
(2023)
Editorial Material
Biochemistry & Molecular Biology
Gabriel E. Valdebenito, Anitta R. Chacko, Michael R. Duchen
Summary: The mitochondrial F1Fo-ATP synthase can both synthesize ATP and pump protons, with potential implications for diseases. In a recent study, Acin-Perez et al. identified (+)-epicatechin as a compound that selectively inhibits ATP hydrolysis without affecting ATP synthesis. They found that this compound has significant benefits for cell and tissue function in disease models, suggesting a novel therapeutic approach for mitochondrial disease.
Article
Multidisciplinary Sciences
Vijil Chenthamarakshan, Samuel C. Hoffman, C. David Owen, Petra Lukacik, Claire Strain-Damerell, Daren Fearon, Tika R. Malla, Anthony Tumber, Christopher J. Schofield, Helen M. E. Duyvesteyn, Wanwisa Dejnirattisai, Loic Carrique, Thomas S. Walter, Gavin R. Screaton, Tetiana Matviiuk, Aleksandra Mojsilovic, Jason Crain, Martin A. Walsh, David I. Stuart, Payel Das
Summary: We validate the broad utility of a deep generative framework trained on protein sequences, small molecules, and their interactions to discover inhibitors for emerging drug-target proteins. By using protein sequence-conditioned sampling, we successfully designed small-molecule inhibitors for two dissimilar targets without knowing their structures or active molecules. In vitro experiments showed micromolar-level inhibition for two out of four synthesized candidates for each target. The most potent inhibitor also exhibited activity against several variants in live virus neutralization assays, demonstrating the effectiveness and efficiency of the generative foundation model in accelerated inhibitor discovery without target structure or binder information.
Review
Biochemistry & Molecular Biology
Andrew M. Mattei, Jonathan D. Smailys, Emma Marie Wilber Hepworth, Shanta D. Hinton
Summary: Pseudophosphatases, atypical members of the protein tyrosine phosphatase family, play important roles in physiology and pathophysiology as key regulators in signaling cascades. By investigating their involvement in diseases and pathologies, pseudophosphatases have emerged as potential therapeutic drug targets.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Cell Biology
Ziping Han, Lingzhi Li, Yuyou Huang, Haiping Zhao, Yumin Luo
Summary: Accumulating evidence suggests PBK/TOPK plays a role in mitosis and cell-cycle progression, with potential therapeutic implications in cancer. However, further research is needed to understand the applicability of PBK/TOPK inhibitors in clinical practice, given their overexpression in normal and pathological proliferative cells.
Article
Oncology
Giulia Mura, Elif Karaca Atabay, Matteo Menotti, Cinzia Martinengo, Chiara Ambrogio, Gloria Giacomello, Maddalena Arigoni, Martina Olivero, Raffaele A. Calogero, Roberto Chiarle, Claudia Voena
Summary: Anaplastic Large Cell Lymphoma (ALCL) is driven by the chimeric tyrosine kinase NPM-ALK, which downregulates the expression of CD45 via STAT3 and acts as a rheostat of ALK oncogenic signaling and resistance to TKI treatment. CD45 is a key regulator of T cell activation and cytokine responses through the JAK/STAT pathway. In ALK+ ALCL, NPM-ALK inhibits T cell molecules expression and activates surrogate TCR signaling. Inhibition of NPM-ALK kinase activity leads to increased expression of CD45RO isoform. Knocking-out CD45 results in increased resistance to ALK TKI treatment.
FRONTIERS IN ONCOLOGY
(2023)
Article
Multidisciplinary Sciences
Helen He Zhu, Xiaolin Luo, Kaiqing Zhang, Jian Cui, Huifang Zhao, Zhongzhong Ji, Zhicheng Zhou, Jufang Yao, Lifan Zeng, Kaihong Ji, Wei-Qiang Gao, Zhong-Yin Zhang, Gen-Sheng Feng
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2015)
Article
Chemistry, Medicinal
Rongjun He, Zhi-Hong Yu, Ruo-Yu Zhang, Li Wu, Andrea M. Gunawan, Brandon S. Lane, Joong S. Shim, Li-Fan Zeng, Yantao He, Lan Chen, Clark D. Wells, Jun O. Liu, Zhong-Yin Zhang
ACS MEDICINAL CHEMISTRY LETTERS
(2015)
Article
Multidisciplinary Sciences
Severa Bunda, Kelly Burrell, Pardeep Heir, Lifan Zeng, Amir Alamsahebpour, Yoshihito Kano, Brian Raught, Zhong-Yin Zhang, Gelareh Zadeh, Michael Ohh
NATURE COMMUNICATIONS
(2015)
Article
Oncology
Yunpeng Bai, Zhi-Hong Yu, Sijiu Liu, Lujuan Zhang, Ruo-Yu Zhang, Li-Fan Zeng, Sheng Zhang, Zhong-Yin Zhang
Article
Medicine, Research & Experimental
Jianxun Wang, Masayuki Mizui, Li-Fan Zeng, Roderick Bronson, Michele Finnell, Cox Terhorst, Vasileios C. Kyttaris, George C. Tsokos, Zhong-Yin Zhang, Maria I. Kontaridis
JOURNAL OF CLINICAL INVESTIGATION
(2016)
Article
Oncology
Ruo-Yu Zhang, Zhi-Hong Yu, Lifan Zeng, Sheng Zhang, Yunpeng Bai, Jinmin Miao, Lan Chen, Jingwu Xie, Zhong-Yin Zhang
Article
Biochemistry & Molecular Biology
Lakshmi Prabhu, Lan Chen, Han Wei, Ozlem Demir, Ahmad Safa, Lifan Zeng, Rommie E. Amaro, Bert H. O'Neil, Zhon-Yin Zhang, Tao Lu
MOLECULAR BIOSYSTEMS
(2017)
Article
Oncology
Lakshmi Prabhu, Han Wei, Lan Chen, Ozlem Demir, George Sandusky, Emily Sun, John Wang, Jessica Mo, Lifan Zeng, Melissa Fishel, Ahmad Safa, Rommie Amaro, Murray Korc, Zhong-Yin Zhang, Tao Lu
Article
Chemistry, Medicinal
Li-Fan Zeng, Ruo-Yu Zhang, Zhi-Hong Yu, Sijiu Li, Li Wu, Andrea M. Gunawan, Brandon S. Lane, Raghuveer S. Mali, Xingjun Li, Rebecca J. Chan, Reuben Kapur, Clark D. Wells, Zhong-Yin Zhang
JOURNAL OF MEDICINAL CHEMISTRY
(2014)
Article
Urology & Nephrology
Ashley Kidwell, Shiv Pratap Singh Yadav, Bernhard Maier, Amy Zollman, Kevin Ni, Arvin Halim, Danielle Janosevic, Jered Myslinski, Farooq Syed, Lifan Zeng, Alain Bopda Waffo, Kimihiko Banno, Xiaoling Xuei, Emma H. Doud, Pierre C. Dagher, Takashi Hato
Summary: This study reveals that translation shutdown in late-phase sepsis-induced kidney injury is caused by excessive phosphorylation of eIF2 alpha and sustained by reduced expression of the counter-regulatory phosphatase Ppp1r15a. Overcoming the repression of Ppp1r15a enables translation salvage and improves kidney function in an endotoxemia model. The existence of an upstream open reading frame (uORF) in Ppp1r15a is a potential therapeutic target for rescuing translation in late-phase sepsis.
JOURNAL OF THE AMERICAN SOCIETY OF NEPHROLOGY
(2023)
Article
Medicine, Research & Experimental
Anh K. Lam, Junping Zhang, Dylan Frabutt, Patrick L. Mulcrone, Lei Li, Lifan Zeng, Roland W. Herzog, Weidong Xiao
Summary: Adeno-associated virus (AAV) is the leading platform for gene therapy. Liquid chromatography and mass spectrometry (LC-MS) is an accurate and efficient method for characterizing AAV capsid proteins. LC-MS/MS peptide mapping can be used to determine the targeted lysine residues in chemically modified AAV capsid proteins.
MOLECULAR THERAPY-METHODS & CLINICAL DEVELOPMENT
(2022)
Article
Biochemistry & Molecular Biology
Sana Sarvi, Richard Crispin, Yuting Lu, Lifan Zeng, Thomas D. Hurley, Douglas R. Houston, Alex von Kriegsheim, Che-Hong Chen, Daria Mochly-Rosen, Marco Ranzani, Marie E. Mathers, Xiaowei Xu, Wei Xu, David J. Adams, Neil O. Carragher, Mayumi Fujita, Lynn Schuchter, Asier Unciti-Broceta, Valerie G. Brunton, E. Elizabeth Patton
CELL CHEMICAL BIOLOGY
(2018)
Meeting Abstract
Cardiac & Cardiovascular Systems
Jianxun Wang, Li-Fan Zeng, Zhong-Yin Zhang, Maria Kontaridis
Article
Medicine, Research & Experimental
Keisuke Maeshima, Stephanie M. Stanford, Deepa Hammaker, Cristiano Sacchetti, Li-fan Zeng, Rizi Ai, Vida Zhang, David L. Boyle, German R. Aleman Muench, Gen-Sheng Feng, John W. Whitaker, Zhong-Yin Zhang, Wei Wang, Nunzio Bottini, Gary S. Firestein
Meeting Abstract
Rheumatology
Keisuke Maeshima, Stephanie M. Stanford, Deepa Hammaker, Cristiano Sacchetti, Rizi Ai, Vida Zhang, David L. Boyle, Lifan Zeng, German Muench, Gen-Sheng Feng, John Whitaker, Zhong-Yin Zhang, Wei Wang, Nunzio Bottini, Gary S. Firestein
ARTHRITIS & RHEUMATOLOGY
(2015)