Review
Oncology
Tomohiro Enokida, Makoto Tahara
Summary: Anti-VEGFR therapy is crucial in treating thyroid cancer but can lead to dangerous adverse reactions. To minimize risks, physicians need to understand the characteristics of these reactions and take appropriate measures. The development of multitarget tyrosine kinase inhibitors has improved prognosis, but effective management of related adverse events is essential.
Article
Oncology
Ji Hyun Lee, Su-Jin Shin, Eun-Ah Choe, Jungyoun Kim, Woo Jin Hyung, Hyo Song Kim, Minkyu Jung, Seung-Hoon Beom, Tae Il Kim, Joong Bae Ahn, Hyun Cheol Chung, Sang Joon Shin
Summary: This study analyzed the incidence of NTRK fusion in KIT/PDGFRA wild-type GISTs and found that 16% of cases in the Yonsei Cancer Center had NTRK fusion. The confirmation of NTRK fusion in KIT/PDGFRA wild-type GISTs provides important information for improving therapeutic outcomes and suggests further research to improve methods for identifying this disease subtype.
Article
Oncology
Wanting Hou, Zhong Jian, Chaoxin Xiao, Yi Cheng, Chengjian Zhao, Zhou Lin, Cao Dan
Summary: A zebrafish xenograft tumor model was used to compare and quantify the antiangiogenic efficacy and safety of nine VEGFR-TKIs. The study found that all nine VEGFR-TKIs exhibited antiangiogenic abilities, with semaxanib being less effective than others. The toxicity assay showed that all tested VEGFR-TKIs were associated with cardiac-related toxicity, particularly apatinib and axitinib, which caused pericardial edema at lower concentrations. The study highlights the potential of the zebrafish model for screening and developing more efficient and less toxic VEGFR-TKIs.
JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY
(2023)
Review
Pharmacology & Pharmacy
Sareshma Sudhesh Dev, Syafiq Asnawi Zainal Abidin, Reyhaneh Farghadani, Iekhsan Othman, Rakesh Naidu
Summary: Receptor tyrosine kinases (RTKs) are crucial cell-surface proteins that regulate essential cellular processes, with alterations in them playing a key role in cancer progression. Curcumin, as an attractive anti-cancer agent, exhibits potent effects by inhibiting RTKs and downstream signaling pathways.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Oncology
Monika Caban, Bettina Koblmueller, Diana Groza, Hemma H. Schueffl, Alessio Terenzi, Alexander Tolios, Thomas Mohr, Marlene Mathuber, Kushtrim Kryeziu, Carola Jaunecker, Christine Pirker, Bernhard K. Keppler, Walter Berger, Christian R. Kowol, Petra Heffeter
Summary: Through chemical modifications, KP2187 has similar activity and action as other clinically used EGFR inhibitors, without interfering with EGFR binding. In vitro and in vivo experiments have shown that KP2187 can significantly inhibit tumor cell proliferation and activate the EGFR signaling pathway. Moreover, KP2187 has a high synergistic effect with VEGFR inhibitors, indicating its potential as a hypoxia-activated prodrug.
Review
Oncology
Kalpana K. Bhanumathy, Amrutha Balagopal, Frederick S. Vizeacoumar, Franco J. Vizeacoumar, Andrew Freywald, Vincenzo Giambra
Summary: Protein phosphorylation is a key regulatory mechanism controlling cellular responses, catalysed by members of the protein kinase superfamily. Tyrosine kinases have been extensively studied for their roles in human malignancies, leading to the development of targeted therapies. Various tyrosine kinases, both receptor and nonreceptor types, play critical roles in the pathogenesis and drug resistance of leukemia, highlighting their potential as therapeutic targets.
Article
Oncology
Christopher Kwok, Adam Khorasanchi, Sarah P. Psutka, Megan Hinkley, Shawn Dason, Debasish Sundi, Yuanquan Yang, Yajing Yang, Claire Verschraegen, Evan E. Gross, Delaney Orcutt, Ming Yin
Summary: This study retrospectively evaluated the efficacy and toxicity of Lenvatinib and everolimus combination therapy in mRCC patients who had previously received ICI and TKI treatment. The results showed that LE therapy had modest efficacies following ICI/TKI treatment, and patients with favorable risk or treated earlier had better treatment response.
FRONTIERS IN ONCOLOGY
(2023)
Review
Chemistry, Analytical
Juan Gao, Jingyi Jian, Zhengjin Jiang, Ann Van Schepdael
Summary: Tyrosine kinases have been extensively studied as drug targets due to their regulation of cellular processes. The deregulation of tyrosine kinases plays a key role in the pathophysiology of various diseases. Several techniques, including traditional binding assays and high-throughput screening methods, have been developed to discover new tyrosine kinase inhibitors. This review provides insights into the different assay methods for the exploration of novel tyrosine kinase inhibitors.
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
(2023)
Article
Veterinary Sciences
C. J. Fisher, A. T. Lejeune, M. J. Dark, O. M. Hernandez, K. Shiomitsu
Summary: Ponatinib has shown cytotoxic effects on canine mast cell tumor cell lines, inducing apoptosis. The study confirmed the expression of three tyrosine kinase receptors and highlighted ponatinib as a potential therapeutic agent for canine mast cell tumors. Further research is needed to explore the prognostic value of these receptors in canine MCTs.
VETERINARY JOURNAL
(2021)
Review
Biochemistry & Molecular Biology
Kang Cheng, Chen-Fu Liu, Guo-Wu Rao
Summary: Inhibiting angiogenesis, particularly through targeting VEGFR-2, is an effective strategy for tumor growth inhibition. This paper reviews the research progress of VEGFR-2 inhibitors in terms of drug development and chemical synthesis.
CURRENT MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Pearly Shuyi Ng, Klement Foo, Sandra Sim, Gang Wang, Chuhui Huang, Li Hong Tan, Anders Poulsen, Boping Liu, Doris Hui Ying Tee, Nur Huda Binte Ahmad, Sifang Wang, Zhiyuan Ke, May Ann Lee, Zekui P. Kwek, Joma Joy, Jothi Anantharajan, Nithya Baburajendran, Vishal Pendharkar, Vithya Manoharan, Susmitha Vuddagiri, Kanda Sangthongpitag, Jeffrey Hill, Thomas H. Keller, Alvin W. Hung
Summary: This study identified a new indazole-based AXL inhibitor through a fragment-based lead discovery approach, providing a suitable starting point for further optimization efforts.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Meng-di Dai, Yue-liang Wang, Jun Fan, Yang Dai, Yin-chun Ji, Yi-ming Sun, Xia Peng, Lan-lan Li, Yu-ming Wang, Wen-hu Duan, Jian Ding, Jing Ai
Summary: DW14383 is a promising selective irreversible pan-FGFR inhibitor with pan-tumor spectrum potential in FGFR1-4 aberrant cancers, which has the potential to overcome compensatory activation among FGFR1-4.
ACTA PHARMACOLOGICA SINICA
(2021)
Article
Biochemistry & Molecular Biology
Masoumeh Divar, Najmeh Edraki, Tahereh Damghani, Fatemeh Moosavi, Maryam Mohabbati, Alireza Alipour, Somayeh Pirhadi, Luciano Saso, Soghra Khabnadideh, Omidreza Firuzi
Summary: Despite advances in therapeutic strategies, cancer remains a leading cause of death. This study synthesized a new series of spiro[indoline-3,2'-quinazoline]-2,4'(3'H)-dione derivatives and evaluated their potential as kinase inhibitors with anti-cancer effects. The most promising compounds exhibited anti-proliferative activity against various cancer cell lines and altered the distribution of cells in the cell cycle. FLT3 kinase was identified as the primary target of these compounds. Compound 5f showed potent inhibitory activity against wild-type FLT3 and its mutant, D835Y. Docking and simulation studies revealed the important interactions of compound 5f with FLT3. These findings suggest that these spiroindoline quinazolinedione compounds could be promising candidates for novel anticancer drugs.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Review
Endocrinology & Metabolism
Artak Labadzhyan, Shlomo Melmed
Summary: Molecular therapeutic targets in growth hormone-secreting adenomas have potential for drug development, including surface receptors recognized by approved drugs and markers for new drug candidates. Current medical therapies control the disease in most patients but the degree of control varies and is related to disease aggressiveness and tumor factors. Understanding the mechanisms behind these molecular markers and their relationship to outcomes holds promise for expanding treatment options and personalized approaches.
FRONTIERS IN ENDOCRINOLOGY
(2022)
Article
Medicine, General & Internal
J. R. Brown, B. Eichhorst, P. Hillmen, W. Jurczak, M. Kazmierczak, N. Lamanna, S. M. O'Brien, C. S. Tam, L. Qiu, K. Zhou, M. Simkovic, J. Mayer, A. Gillespie-Twardy, A. Ferrajoli, P. S. Ganly, R. Weinkove, S. Grosicki, A. Mital, T. Robak, A. Osterborg, H. A. Yimer, T. Salmi, M. -D. -Y. Wang, L. Fu, J. Li, K. Wu, A. Cohen, M. Shadman
Summary: In a multinational phase 3 trial, zanubrutinib was found to be superior to ibrutinib in treating relapsed or refractory CLL or SLL, with better efficacy and fewer side effects.
NEW ENGLAND JOURNAL OF MEDICINE
(2023)