Review
Biochemistry & Molecular Biology
Mai Tanaka, Dietmar W. Siemann
Summary: Dysregulated signaling pathways in cancer cells and the tumor microenvironment, including the Axl and Gas6 pathways, have led to the development of therapeutic agents targeting the Gas6/Axl pathway. Promising results have been observed in both preclinical and clinical settings, indicating potential clinical efficacy of targeting Gas6 and Axl.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Pharmacology & Pharmacy
Ava Safaroghli-Azar, Fatemeh Emadi, Jimma Lenjisa, Laychiluh Mekonnen, Shudong Wang
Summary: As the fifth pillar of cancer treatment, immunotherapy has revolutionized therapeutic strategies by focusing on the host's immune system. The discovery of immune-modulatory effects for kinase inhibitors has opened up new possibilities in this approach, as these small molecule inhibitors not only directly target essential proteins for tumor survival and proliferation, but also stimulate immune responses against malignant cells.
DRUG DISCOVERY TODAY
(2023)
Review
Chemistry, Medicinal
Xinjian Tian, Feng Xu, Qiangsheng Zhu, Ziwen Feng, Wei Dai, Yeling Zhou, Qi-Dong You, Xiaoli Xu
Summary: This review focuses on the connection between the cGAS-STING signaling pathway and autoimmune and inflammatory disorders. It summarizes the development and optimization of cGAS-STING inhibitors and discusses their therapeutic effects on inflammatory diseases. The review also proposes suggestions and insights for future exploration in this area.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Pharmacology & Pharmacy
Huy Nguyen, Sung-Jin Lee, Yang Li
Summary: Retinal ischemia is a major cause of visual impairment and blindness worldwide, often associated with various disorders. Diabetic retinopathy is a common cause, and its exact pathogenesis remains unclear, but vascular leakage plays a significant role in visual impairment. Current treatments have limitations, therefore there is a need for new therapies to address vessel regeneration and reperfusion in ischemic retinal areas. The Wnt signaling pathway in the retina could provide a novel disease modifying therapy.
Review
Oncology
Ye Jin, Tianjia Liu, Haoming Luo, Yangyang Liu, Da Liu
Summary: Dysregulation of epigenetic enzyme-mediated transcription is closely related to tumors, and small-molecule compounds targeting epigenetic regulation show promise as therapeutics. Berberine and ginsenosides are natural compounds that target epigenetic regulatory enzymes for cancer treatment.
FRONTIERS IN ONCOLOGY
(2022)
Review
Chemistry, Multidisciplinary
Qian Wu, Li Jiang, Si-cheng Li, Qiao-jun He, Bo Yang, Ji Cao
Summary: PD-1/PD-L1 signaling pathway is a target for anticancer drugs, and the development of small molecule inhibitors provides a new avenue for tumor immunotherapy.
ACTA PHARMACOLOGICA SINICA
(2021)
Review
Chemistry, Multidisciplinary
Jia Zheng, Wei Zhang, Linfeng Li, Yi He, Yue Wei, Yongjun Dang, Shenyou Nie, Zufeng Guo
Summary: Targeted therapy is a groundbreaking innovation in cancer treatment, with FGFRs being recognized as promising therapeutic targets. Several generations of FGFR kinase inhibitors have been developed over the past two decades.
FRONTIERS IN CHEMISTRY
(2022)
Review
Genetics & Heredity
Ankita Sharma, Rafeeq Mir, Sanjeev Galande
Summary: This review discusses the role of the Wnt/beta-catenin pathway in cell proliferation, differentiation, and migration, as well as its impact on embryonic development, tissue regeneration, and cancer. It highlights the influence of epigenetic factors on the pathway and the crosstalk with other signaling pathways, particularly the Hippo/YAP pathway. The review also emphasizes recent advances in developing potential therapeutic interventions targeting the epigenetic machinery for treating various cancers and regenerative therapies.
FRONTIERS IN GENETICS
(2021)
Article
Medicine, Research & Experimental
Annoor Awadasseid, Yanling Wu, Wen Zhang
Summary: Immune checkpoint blockade targeting the PD-1/PD-L1 signaling pathway has shown promising results in cancer therapy by degrading anti-tumor immune response. The axis PD-1/PD-L1 is crucial for immune escape of cancer and has a significant impact on cancer treatment. Further research on PD-1 and PD-L1 function aims to enhance cancer therapy.
Review
Immunology
Panagiotis F. Christopoulos, Torleif T. Gjolberg, Stig Kruger, Guttorm Haraldsen, Jan Terje Andersen, Eirik Sundlisaeter
Summary: The Notch signaling pathway plays a supporting role in various inflammation-driven diseases, but targeting this pathway for treatment has proven challenging due to its broad involvement in regenerative and homeostatic processes. Efforts to intervene with the Notch pathway by targeting Notch ligands and/or receptors through distinct therapeutic strategies, including antibody designs, are ongoing. Lessons learned from Notch targeting in cancer treatment may help guide the development of therapeutic strategies for chronic inflammatory diseases.
FRONTIERS IN IMMUNOLOGY
(2021)
Review
Pharmacology & Pharmacy
Andrew Morris, Piyusha P. Pagare, Jiong Li, Yan Zhang
Summary: The Wnt/8-β-catenin pathway plays a crucial role in cancer treatment, but developing small-molecule inhibitors through traditional methods has proven difficult. Computer-aided drug discovery efforts have shown promise, and a more efficient and cost-effective approach to developing inhibitors for this pathway is needed.
DRUG DISCOVERY TODAY
(2022)
Review
Endocrinology & Metabolism
Wencai Wang, Luyao Ma, Yongqiang Zhao, Menghao Liu, Wei Ye, Xianfeng Li
Summary: This article reviews the pathogenesis of pituitary adenoma and the role of the Wnt signaling pathway. It discusses the potential of combining Wnt pathway inhibitors with immunotherapy for the treatment of pituitary adenoma.
FRONTIERS IN ENDOCRINOLOGY
(2023)
Review
Genetics & Heredity
Jingyao Cui, Haoran Chen, Kaiwen Zhang, Xin Li
Summary: Wnt pathway plays a crucial role in cancer bone metastasis and targeted therapeutic strategies have shown promise. Current progress includes research on pharmacological Wnt modulators against breast cancer bone metastasis and exploration of emerging therapeutic strategies based on Wnt pathway-related targets, providing new ideas for the development of Wnt-based intervention strategies in the future.
JOURNAL OF MOLECULAR MEDICINE-JMM
(2022)
Review
Biochemistry & Molecular Biology
Dunja Mudri, Ines Bilic Curcic, Lucija Mestrovic, Ivica Mihaljevic, Tomislav Kizivat
Summary: Graves' disease is an autoimmune disease that leads to excessive production of thyroid hormones, affecting various organ systems. It can cause skeletal disorders and decrease bone density. The Wnt signaling pathway plays a role in maintaining bone mass, with inhibition causing bone loss and stimulation increasing it.
Review
Biochemistry & Molecular Biology
Manzar Alam, Md. Meraj Ansari, Saba Noor, Taj Mohammad, Gulam Mustafa Hasan, Syed Naqui Kazim, Md. Imtaiyaz Hassan
Summary: TBK1 plays a fundamental role in regulating cellular responses and controlling signaling cascades. Dysregulation of the TBK1 pathway is associated with various pathophysiological conditions. Inhibitors targeting TBK1 have potential therapeutic applications for diseases, including cancer.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2022)
Article
Chemistry, Medicinal
Jiawang Liu, Shilong Zheng, Shanchun Guo, Changde Zhang, Qiu Zhong, Qiang Zhang, Peng Ma, Elena V. Skripnikova, Melyssa R. Bratton, Thomas E. Wiese, Guangdi Wang
ACS MEDICINAL CHEMISTRY LETTERS
(2017)
Article
Chemistry, Medicinal
Shilong Zheng, Shanchun Guo, Qiu Zhong, Changde Zhang, Jiawang Liu, Lin Yang, Qiang Zhang, Guangdi Wang
ACS MEDICINAL CHEMISTRY LETTERS
(2018)
Article
Oncology
Tulasi Ponnapakkam, Tyjah Saulsberry, Tarius Hill, Miriam Hill-Odom, Navneet Goyal, Murali Anbalagan, Jiawang Liu, Maryam Foroozesh
Article
Nutrition & Dietetics
Qi Zhao, Hui Shen, Kuan-Jui Su, Ji-Gang Zhang, Qing Tian, Lan-Juan Zhao, Chuan Qiu, Qiang Zhang, Timothy J. Garrett, Jiawang Liu, Hong-Wen Deng
NUTRITION & METABOLISM
(2018)
Article
Cell Biology
Qi Zhao, Hui Shen, Kuan-Jui Su, Qing Tian, Lan-Juan Zhao, Chuan Qiu, Timothy J. Garrett, Jiawang Liu, David Kakhniashvili, Hong-Wen Deng
Article
Immunology
Dong Yang, Xiaoping He, Shaoji Li, Jiawang Liu, Jennifer Stabenow, Lillian Zalduondo, Stephen White, Ying Kong
JOURNAL OF INFECTIOUS DISEASES
(2019)
Review
Biochemistry & Molecular Biology
Maryam Foroozesh, Jayalakshmi Sridhar, Navneet Goyal, Jiawang Liu
Article
Oncology
Shanchun Guo, Changde Zhang, Madhusoodanan Mottamal, Ahamed Hossain, Jiawang Liu, Guangdi Wang
BREAST CANCER RESEARCH AND TREATMENT
(2020)
Article
Microbiology
Dong Yang, Zachary E. Taylor, Scott Handy, Shaoji Li, Jiawang Liu, Jennifer Stabenow, Lillian Zalduondo, Colleen B. Jonsson, Elliot Altman, Ying Kong
FRONTIERS IN MICROBIOLOGY
(2020)
Article
Hematology
Jungang Chen, Navneet Goyal, Lu Dai, Zhen Lin, Luis Del Valle, Jovanny Zabaleta, Jiawang Liu, Steven R. Post, Maryam Foroozesh, Zhiqiang Qin
Article
Endocrinology & Metabolism
Qi Zhao, Zunsong Hu, Mehmet Kocak, Jiawang Liu, Jay H. Fowke, Joan C. Han, David Kakhniashvili, Kaja Z. Lewinn, Nicole R. Bush, W. Alex Mason, Frances A. Tylavsky
Summary: Prenatal metabolomics profiles can improve the prediction of childhood growth trajectories and obesity risk, with specific prenatal metabolites associated with children's BMI trajectories and overweight/obesity status.
INTERNATIONAL JOURNAL OF OBESITY
(2021)
Article
Biotechnology & Applied Microbiology
Yu Lu, Di Zhu, Lin Gui, Yuanming Li, Wenjing Wang, Jiawang Liu, Yuji Wang
Summary: In this study, a novel dual-targeting ruthenium candidate 2b was reported to possess anti-tumor and anti-metastatic properties, targeting tumor sites through the EPR effect and TF/TFR interaction. In vitro and in vivo experiments demonstrated that 2b inhibited tumor growth and prevented lung metastasis effectively.
JOURNAL OF NANOBIOTECHNOLOGY
(2021)
Article
Nanoscience & Nanotechnology
Yu Lu, Zidong Peng, Di Zhu, Yijiang Jia, Ayijiang Taledaohan, Yuanming Li, Jiawang Liu, Yanming Wang, Yuji Wang
Summary: A targeted drug delivery system combining PAD4 inhibitors and gold nanoparticles was developed to reduce gold accumulation in organs and lower chemotherapeutic drug doses. The study showed that gold nanorods loaded with PAD4 inhibitors had better tumor inhibitory activity and could effectively inhibit tumor growth and reduce metastasis through combination therapy, improving biosafety.
INTERNATIONAL JOURNAL OF NANOMEDICINE
(2021)
Article
Chemistry, Medicinal
Madison N. Sluter, Ruida Hou, Lexiao Li, Nelufar Yasmen, Ying Yu, Jiawang Liu, Jianxiong Jiang
Summary: EP2 antagonists provide a more specific approach to modulating downstream prostanoid synthases or receptors, potentially becoming candidates for next-generation anti-inflammatory therapies. Their emergence reshapes our understanding of the role of EP2 receptors in inflammation-related conditions, with significant implications for disease treatment.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Jiawang Liu, Nirmal Rajasekaran, Ahamed Hossain, Changde Zhang, Shanchun Guo, Borui Kang, Hunsoon Jung, Hongjoong Kim, Guangdi Wang
Summary: Fulvestrant-3-boronic acid (ZB716), an oral selective estrogen receptor degrader (SERD) under clinical development, has been investigated in ADME studies to characterize its absorption, metabolism, and pharmacokinetics. ZB716 exhibits high plasma protein binding and low intestinal mucosal permeability, with high clearance in hepatocytes and metabolism primarily by CYP2D6 and CYP3A. In enzyme activity assays, ZB716 induces certain cytochrome P450 enzymes in a concentration-dependent manner. Pharmacokinetic studies in rats and dogs demonstrate oral bioavailability and dose-proportional drug exposure, with drug accumulation as measured by maximum concentration and area under the concentration-time curve (AUC).
