Article
Chemistry, Medicinal
Mingfeng Yu, Yuchao Yang, Matthew Sykes, Shudong Wang
Summary: Tankyrases are multifunctional enzymes that regulate various biological processes, including telomere maintenance and cellular signaling. Their involvement in human diseases, especially cancer, has led to increased interest in tankyrase inhibitors as potential therapeutics. This review provides an overview of tankyrases and their cancer-related functions, and discusses the progress of small-molecule inhibitors targeting tankyrases, including their binding modes and clinically trialed inhibitors.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Zhiqing Liu, Pingyuan Wang, Eric A. Wold, Qiaoling Song, Chenyang Zhao, Changyun Wang, Jia Zhou
Summary: Researchers have made significant progress in the discovery and development of small-molecule inhibitors targeting the canonical WNT pathway in recent years, with a focus on specific target proteins and candidates in clinical trials. The study also highlights the challenges and opportunities in effectively targeting this pathway while maintaining a balance between efficacy and toxicity.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Chemistry, Medicinal
Zhen Wang, Zilu Li, Haitao Ji
Summary: Aberrant activation of the Wnt/beta-catenin signaling pathway is associated with cancer, and direct targeting of beta-catenin is a promising strategy but challenging. Research has identified potential small-molecule binding sites and summarized bioactive small molecules that target beta-catenin directly.
MEDICINAL RESEARCH REVIEWS
(2021)
Article
Oncology
Yang Zhou, Jiang Xu, Haichang Luo, Xiangjing Meng, Ming Chen, Di Zhu
Summary: Abnormal activation of the Wnt/beta-catenin signaling pathway is closely related to tumorigenesis and immune surveillance, leading to increased resistance to immunotherapy.
Review
Biochemistry & Molecular Biology
Andrew R. Conery, Jennifer L. Rocnik, Patrick Trojer
Summary: The approval of the first histone methyltransferase inhibitor in 2020 marks a significant milestone in the field of targeted manipulation of chromatin regulatory pathways for cancer treatment. Despite the complexity of identifying key targets for therapeutic intervention, approaches in chemical biology have played a critical role in discovering key nodes in these pathways and translating them into potential cancer therapies. This review highlights the importance of chemical probes, drug candidates, and translational strategies in maximizing the impact of epigenetic writer enzymes in cancer therapy.
NATURE CHEMICAL BIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Na Young Kim, Chakrabhavi Dhananjaya Mohan, Arunachalam Chinnathambi, Sulaiman Ali Alharbi, Gautam Sethi, Kanchugarakoppal S. Rangappa, Kwang Seok Ahn
Summary: In this study, the researchers demonstrated the effect of EPBS on EGFR and Wnt/β-catenin pathways in NSCLC cells. They found that EPBS selectively induced cytotoxicity in A549 cells expressing wildtype EGFR, and suppressed the expression of EGFR, Wnt3a, β-catenin, and FZD-1. EPBS reduced β-catenin levels through the activation of GSK-3 β and reversed the effects of lithium chloride treatment. Additionally, forced expression or depletion of EGFR affected the levels of Wnt3a, β-catenin, and FZD-1 in NSCLC cells.
Review
Biology
Zachary Kaplan, Steven P. Zielske, Kristina G. Ibrahim, Frank C. Cackowski
Summary: Wnt family proteins and beta-catenin play critical roles in developmental and oncogenic processes, particularly in prostate cancer bone metastasis. The processes involve EMT at the primary tumor, migration in the blood stream, and acquisition of stem-like properties in the bones through signaling pathways involving Wnt and beta-catenin.
Article
Biotechnology & Applied Microbiology
Zhi Fang, Min Zhong, Ling Zhou, Yi Le, Heng Wang, Ziling Fang
Summary: LRP8 is markedly overexpressed in NSCLC tissues and cell lines, correlating with poor clinicopathological characteristics and prognosis. Depletion of LRP8 suppresses proliferation, migration, invasion, and epithelial-mesenchymal transition of NSCLC cells, partly by inhibiting the Wnt/beta-catenin pathway.
Article
Oncology
Yi Liao, Jianguo Feng, Weichao Sun, Chao Wu, Jingyao Li, Tao Jing, Yuteng Liang, Yonghui Qian, Wenlan Liu, Haidong Wang
Summary: The study revealed that CIRP is highly expressed in NSCLC tissue and promotes the progression of the disease by affecting cell cycle, DNA replication, and the Wnt signaling pathway. This finding may provide a new target for NSCLC therapy.
JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH
(2021)
Review
Oncology
Stefan Koch
Summary: This article discusses the control of the Wnt pathway by FOX proteins, and the contribution of their interaction to cancer initiation and progression. Further research on FOX biology may lead to new targeted treatments for cancer.
Review
Biochemistry & Molecular Biology
Qiyun Xiao, Johannes Werner, Nachiyappan Venkatachalam, Kim E. Boonekamp, Matthias P. Ebert, Tianzuo Zhan
Summary: Targeting cancer hallmarks is crucial for improving anti-cancer treatment, but cross-talk between signaling pathways often leads to resistance. This article provides an overview of the molecular interactions between the p53 and Wnt pathways in cancer, including complex feedback loops and reciprocal transactivation, as well as the mutational landscape of genes associated with these pathways.
Review
Chemistry, Medicinal
Panpan Yang, Yumeng Zhu, Qinwen Zheng, Sha Meng, Yongya Wu, Wen Shuai, Qiu Sun, Guan Wang
Summary: The Wnt/fl-catenin signaling pathway is involved in various cellular processes and its abnormal activation has been linked to cancer development. Fl-catenin, a core component of this pathway, is a key factor in its activation. Therefore, the development of Fl-catenin inhibitors has become an important focus in anticancer drug research. However, challenges in terms of selectivity, specificity, and physicochemical properties need to be addressed. This review highlights the progress made in the research of small molecule inhibitors targeting Fl-catenin and discusses the future prospects in drug development.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Oncology
Iram Fatima, Susmita Barman, Rajani Rai, Kristina W. Thiel, Vishal Chandra
Summary: The role of Wnt signaling in endometrial carcinoma, including its activation mechanisms and links to cell cycle regulation, hormonal pathways, and other signaling cascades, remains a significant research focus. Therapeutic interference with Wnt signaling poses a challenge, and further advancements in drug discovery are needed.
Article
Oncology
Chun Tang, Xuehui Wang, Changle Ji, Wenfang Zheng, Yunhe Yu, Xiaochong Deng, Xiqian Zhou, Lin Fang
Summary: The study demonstrated that miR-640 suppresses the tumorigenesis of breast cancer cells by regulating the Wnt/β-catenin signaling pathway, making it a potential novel target for targeted therapy in breast cancer.
FRONTIERS IN ONCOLOGY
(2021)
Review
Medicine, Research & Experimental
Yong Ji, Jian Lv, Di Sun, Yufeng Huang
Summary: This review explores the significant role of the Wnt/β-catenin signaling pathway in colorectal cancer tumorigenesis, metastasis, and recurrence, as well as its potential value in diagnosis and therapeutics.
INTERNATIONAL JOURNAL OF MOLECULAR MEDICINE
(2022)
Article
Chemistry, Medicinal
Hamdy M. Abdel-Rahman, Mohamed Abdel-Aziz, Heather N. Tinsley, Bernard D. Gary, Joshua C. Canzoneri, Gary A. Piazza
ARCHIV DER PHARMAZIE
(2016)
Article
Oncology
Sangbin Lim, Hao Liu, Luciana Madeira da Silva, Ritu Arora, Zixing Liu, Joshua B. Phillips, David C. Schmitt, Tung Vu, Steven McClellan, Yifeng Lin, Wensheng Lin, Gary A. Piazza, Oystein Fodstad, Ming Tan
Article
Chemistry, Medicinal
Mohamed Salah Rezk, Mohammad Abdel-Halim, Adam Keeton, Derek Franklin, Matthias Bauer, Farnk Michael Boeckler, Matthias Engel, Rolf Wolfgang Hartmann, Yanping Zhang, Gary Anthony Piazza, Ashraf Hassan Abadi
CHEMICAL & PHARMACEUTICAL BULLETIN
(2016)
Article
Chemistry, Medicinal
Engi A. Hassaan, Sara C. Sigler, Tamer M. Ibrahim, Kevin J. Lee, Lauren K. Cichon, Bernard D. Gary, Joshua C. Canzoneri, Gary A. Piazza, Ashraf H. Abadi
MEDICINAL CHEMISTRY
(2016)
Article
Multidisciplinary Sciences
W. Joon Chung, Jennifer L. Goeckeler-Fried, Viktoria Havasi, Annette Chiang, Steven M. Rowe, Zackery E. Plyler, Jeong S. Hong, Marina Mazur, Gary A. Piazza, Adam B. Keeton, E. Lucile White, Lynn Rasmussen, Allan M. Weissman, R. Aldrin Denny, Jeffrey L. Brodsky, Eric J. Sorscher
Article
Chemistry, Medicinal
Hatem A. Abdel-Aziz, Wagdy M. Eldehna, Adam B. Keeton, Gary A. Piazza, Adnan A. Kadi, Mohamed W. Attwa, Ali S. Abdelhameed, Mohamed I. Attia
DRUG DESIGN DEVELOPMENT AND THERAPY
(2017)
Article
Oncology
Bing Zhu, Ashley Lindsey, Nan Li, Kevin Lee, Veronica Ramirez-Alcantara, Joshua C. Canzoneri, Alexandra Fajardo, Luciana Madeira da Silva, Meagan Thomas, John T. Piazza, Larry Yet, Brian T. Eberhardt, Evrim Gurpinar, Dennis Otali, William Grizzle, Jacob Valiyaveettil, Xi Chen, Adam B. Keeton, Gary A. Piazza
Article
Multidisciplinary Sciences
Mohamed I. Attia, Wagdy M. Eldehna, Samar A. Afifi, Adam B. Keeton, Gary A. Piazza, Hatem A. Abdel-Aziz
Editorial Material
Oncology
Krista Wood, Raeann Donnenwirth, Kourtney Mills, Heather N. Tinsley
Article
Biochemistry & Molecular Biology
Mohammad Abdel-Halim, Heather Tinsley, Adam B. Keeton, Mohammed Weam, Noha H. Atta, Mennatallah A. Hammam, Amr Hefnawy, Rolf W. Hartmann, Matthias Engel, Gary A. Piazza, Ashraf H. Abadi
BIOORGANIC CHEMISTRY
(2020)
Review
Medicine, Research & Experimental
Kevin Lee, Gary A. Piazza
JOURNAL OF BIOMEDICAL RESEARCH
(2017)
Article
Cell Biology
Gregory Tombline, Jonathan I. Millen, Bogdan Polevoda, Matan Rapaport, Bonnie Baxter, Michael Van Meter, Matthew Gilbertson, Joe Madrey, Gary A. Piazza, Lynn Rasmussen, Krister Wennerberg, E. Lucile White, John L. Nitiss, David S. Goldfarb
Article
Pharmacology & Pharmacy
Ahmed K. Elhady, Sara C. Sigler, Nazih Noureldin, Joshua C. Canzoneri, Nermin S. Ahmed, Gary A. Piazza, Ashraf H. Abadi
SCIENTIA PHARMACEUTICA
(2016)
Article
Biochemistry & Molecular Biology
Jeevan K. Prasain, Rajani Rajbhandari, Adam B. Keeton, Gary A. Piazza, Stephen Barnes
Article
Medicine, Research & Experimental
Jason D. Whitt, Adam B. Keeton, Bernard D. Gary, Larry A. Sklar, Kamlesh Sodani, Zhe-Sheng Chen, Gary A. Piazza
JOURNAL OF BIOMEDICAL RESEARCH
(2016)