keyword
https://read.qxmd.com/read/37736340/vandetanib-alters-the-tumoricidal-capacity-of-human-breast-cancer-stem-cells-via-inhibiting-vasculogenic-capacity
#21
JOURNAL ARTICLE
Sanya Haiaty, Mohammad-Reza Rashidi, Maryam Akbarzadeh, Ahad Bazmany, Mostafa Mostafazadeh, Saba Nikanfar, Roya Shabkhizan, Rostam Rezaeian, Reza Rahbarghazi, Mohammad Nouri
INTRODUCTION: The inhibition of vascularization into tumor stroma as well as dynamic cell growth is the center of attention. Here, we aimed to examine the role of vandetanib on angiogenesis capacity of breast cancer stem cell (CSCs). METHODS: MDA-MB-231 cells were exposed to different doses of vandetanib and survival rate was monitored. Stimulatory effects of vascular endothelial growth factor (VEGF), fibroblast growth factor (FGF), and epidermal growth factor (EGF) were evaluated in vandetanib-treated MDA-MB-231 cells...
2023: BioImpacts: BI
https://read.qxmd.com/read/37535881/d898_e901-ret-deletion-is-oncogenic-responds-to-selpercatinib-and-treatment-resistance-can-arise-via-ret-independent-mechanisms
#22
JOURNAL ARTICLE
Tommaso Porcelli, Marialuisa Moccia, Maria Angela De Stefano, Raffaele Ambrosio, Ettore Capoluongo, Massimo Santoro, Julien Hadoux, Martin Schlumberger, Francesca Carlomagno, Domenico Salvatore
PURPOSE: We analyzed the oncogenic potential of RET Δ898-901 mutant and its response to selpercatinib, vandetanib, and cabozantinib in vitro and in a clinical case. MATERIALS AND METHODS: A 35-year-old man with a medullary thyroid cancer (MTC) harboring a somatic D898_E901 RET deletion was sequentially treated with vandetanib, selpercatinib, cabozantinib, and fluorouracil (5-FU)-dacarbazine. Functional study of RET Δ898-901 mutant was performed in HEK-293T, NIH-3T3, and Ba/F3 cells...
August 2023: JCO Precision Oncology
https://read.qxmd.com/read/37511745/personalized-medicine-in-medullary-thyroid-carcinoma-a-broad-review-of-emerging-treatments
#23
REVIEW
Rui Sousa Martins, Tito Teles Jesus, Luís Cardoso, Paula Soares, João Vinagre
Medullary thyroid carcinoma (MTC) arises from parafollicular cells in the thyroid gland, and although rare, it represents an aggressive type of thyroid cancer. MTC is recognized for its low mutational burden, with point mutations in RET or RAS genes being the most common oncogenic events. MTC can be resistant to cytotoxic chemotherapy, and multitarget kinase inhibitors (MKIs) have been considered a treatment option. They act by inhibiting the activities of specific tyrosine kinase receptors involved in tumor growth and angiogenesis...
July 13, 2023: Journal of Personalized Medicine
https://read.qxmd.com/read/37492082/evaluation-of-chronic-drug-induced-electrophysiological-and-cytotoxic-effects-using-human-induced-pluripotent-stem-cell-derived-cardiomyocytes-hipsc-cms
#24
JOURNAL ARTICLE
C Altrocchi, K Van Ammel, M Steemans, M Kreir, F Tekle, A Teisman, D J Gallacher, H R Lu
Introduction: Cardiotoxicity is one of the leading causes of compound attrition during drug development. Most in vitro screening platforms aim at detecting acute cardio-electrophysiological changes and drug-induced chronic functional alterations are often not studied in the early stage of drug development. Therefore, we developed an assay using human-induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs) that evaluates both drug-induced acute and delayed electrophysiological and cytotoxic effects of reference compounds with clinically known cardiac outcomes...
2023: Frontiers in Pharmacology
https://read.qxmd.com/read/37482237/learning-from-covid-19-how-drug-hunters-can-prepare-for-the-next-pandemic
#25
JOURNAL ARTICLE
Ana C Puhl, Thomas Lane, Sean Ekins
Over 3 years, the SARS-CoV-2 pandemic killed nearly 7 million people and infected more than 767 million globally. During this time, our very small company was able to contribute to antiviral drug discovery efforts through global collaborations with other researchers, which enabled the identification and repurposing of multiple molecules with activity against SARS-CoV-2 including pyronaridine tetraphosphate, tilorone, quinacrine, vandetanib, lumefantrine, cetylpyridinium chloride, raloxifene, carvedilol, olmutinib, dacomitinib, crizotinib, and bosutinib...
July 21, 2023: Drug Discovery Today
https://read.qxmd.com/read/37465525/psychiatric-adverse-reactions-to-non-selective-ret-multi-kinase-inhibitors-a-large-scale-pharmacovigilance-analysis
#26
JOURNAL ARTICLE
Xuyan Wang, Donghong Yin, Yang Tang, Feng Xiao, Shuyun Wang
Objective: The development of non-selective multi-kinase inhibitors (MKIs) has improved the. survival outcomes of patients with cancers. Psychiatric disorders represent an MKIs related AE of particular concern, as they are often ignored and may harm the patient's personal and social functioning. Therefore, we use the public database to describe and evaluate psychiatric adverse events related to various non-selective RET MKIs. Provide evidence for optimizing drug administration in the clinic. Methods: We analyzed spontaneous reports submitted to the Food and Drug Administration Adverse Events Reporting System FDA Adverse Event Reporting System in an observational and retrospective manner...
2023: Frontiers in Pharmacology
https://read.qxmd.com/read/37453330/quinazoline-based-vegfr-2-inhibitors-as-potential-anti-angiogenic-agents-a-contemporary-perspective-of-sar-and-molecular-docking-studies
#27
REVIEW
Mahfam Moradi, Alireza Mousavi, Zahra Emamgholipour, Johanna Giovannini, Setareh Moghimi, Fariba Peytam, Amin Honarmand, Stéphane Bach, Alireza Foroumadi
Angiogenesis, the formation of new blood vessels from the existing vasculature, is pivotal in the migration, growth, and differentiation of endothelial cells in normal physiological conditions. In various types of tumour microenvironments, dysregulated angiogenesis plays a crucial role in supplying oxygen and nutrients to cancerous cells, leading to tumour size growth. VEGFR-2 tyrosine kinase has been extensively studied as a critical regulator of angiogenesis; thus, inhibition of VEGFR-2 has been widely used for cancer treatments in recent years...
July 8, 2023: European Journal of Medicinal Chemistry
https://read.qxmd.com/read/37434642/kinase-inhibitors-in-thyroid-cancers
#28
REVIEW
Vineeth Sukrithan, Prachi Jain, Manisha H Shah, Bhavana Konda
OBJECTIVE: The treatment landscape for thyroid cancers has changed rapidly with the availability of kinase inhibitors against VEGFR, BRAF, MEK, NTRK, and RET. We provide an up-to-date review of the role of kinase inhibitors in thyroid cancer and discuss upcoming trials. DESIGN & METHODS: A comprehensive review of the available literature describing kinase inhibitors in thyroid cancer was performed. RESULTS AND CONCLUSIONS: Kinase inhibitors have become the standard of care for patients with metastatic radioactive iodine-refractory thyroid cancer...
January 1, 2023: Endocr Oncol
https://read.qxmd.com/read/37425604/innovation-and-precision-medicine-applied-to-a-medullary-thyroid-cancer-a-clinical-case
#29
Helena Guedes, Inês Leão, Adriana Soares, Raquel Basto, Ana Joaquim
Medullary thyroid carcinoma (MTC) is a rare type of neuroendocrine tumor, accounting for 3%-4% of all thyroid cancers. Seventy-five percent are sporadic, of which 60% have pathogenic REarranged during Transfection (RET) somatic mutations. The sporadic RET-mutated MTC poses novel challenges for targeted treatment. The authors present a case of a 60-year-old male diagnosed in 2018 with MTC who underwent total thyroidectomy with sternotomy and bilateral cervical lymph node dissection - pT3N1b R1 L1 V1 Pn0 cM1 (hepatic and lung metastasis)...
June 2023: Curēus
https://read.qxmd.com/read/37418333/two-drugs-for-ret-altered-cancers-retevmo-and-gavreto
#30
JOURNAL ARTICLE
(no author information available yet)
No abstract text is available yet for this article.
July 10, 2023: Medical Letter on Drugs and Therapeutics
https://read.qxmd.com/read/37361540/validation-of-mirnas-as-diagnostic-and-prognostic-biomarkers-and-possible-therapeutic-targets-in-medullary-thyroid-cancers
#31
JOURNAL ARTICLE
Alberto Mondin, Loris Bertazza, Susi Barollo, Maria Chiara Pedron, Jacopo Manso, Ilaria Piva, Daniela Basso, Isabella Merante Boschin, Maurizio Iacobone, Raffaele Pezzani, Caterina Mian, Simona Censi
INTRODUCTION: Medullary thyroid cancer (MTC) is a rare type of neuroendocrine tumor that produces a hormone called calcitonin (CT). Thyroidectomy is the preferred treatment for MTC, as chemotherapy has been shown to have limited effectiveness. Targeted therapy approaches are currently being used for patients with advanced, metastatic MTC. Several studies have identified microRNAs, including miR-21, as playing a role in the development of MTC. Programmed cell death 4 (PDCD4) is a tumor suppressor gene that is an important target of miR-21...
2023: Frontiers in Endocrinology
https://read.qxmd.com/read/37282639/repurposing-antipsychotic-agents-against-targets-of-angiogenesis-pathways-for-cancer-therapy-an-in-silico-approach
#32
JOURNAL ARTICLE
Kanmodi Rahmon, Habeeb Bankole, Oddiri Regina, Arowosegbe Michael, Alabi Ridwan, Ahmodu Oladejo, AbdulRasheed Bilal, Muritala Rauf, Rahmon Saheed
BACKGROUND: Antipsychotics interfere with virtually all hallmarks of cancer, including angiogenesis. Vascular endothelial growth factor receptors (VEGFRs) and platelet-derived growth receptors (PDGFRs) play crucial roles in angiogenesis and represent targets of many anti-cancer agents. We assessed and compared the binding effects of antipsychotics and receptor tyrosine kinase inhibitors (RTKIs) on VEGFR2 and PDGFRα. METHODS: FDA-approved antipsychotics and RTKIs were retrieved from DrugBank...
June 6, 2023: Current Drug Discovery Technologies
https://read.qxmd.com/read/37257629/molecular-basis-and-targeted-therapy-in-thyroid-cancer-progress-and-opportunities
#33
REVIEW
Lizhuo Zhang, Qingqing Feng, Jiafeng Wang, Zhuo Tan, Qinglin Li, Minghua Ge
Thyroid cancer (TC) is the most prevalent endocrine malignant tumor. Surgery, chemotherapy, radiotherapy, and radioactive iodine (RAI) therapy are the standard TC treatment modalities. However, recurrence or tumor metastasis remains the main challenge in the management of anaplastic thyroid cancer (ATC) and radioiodine (RAI) radioactive iodine-refractory differentiated thyroid cancer (RR-DTC). Several multi-tyrosine kinase inhibitors (MKIs), or immune checkpoint inhibitors in combination with MKIs, have emerged as novel therapies for controlling the progression of DTC, medullary thyroid cancer (MTC), and ATC...
May 29, 2023: Biochimica et Biophysica Acta. Reviews on Cancer
https://read.qxmd.com/read/37247926/pancreatic-stromal-cell-derived-oncostatin-m-confers-drug-resistance-to-a-multi-tyrosine-kinase-inhibitor-in-pancreatic-cancer-cells
#34
JOURNAL ARTICLE
Daisuke Tatsuda, Junjiro Yoshida, Tomokazu Ohishi, Manabu Kawada
BACKGROUND/AIM: Pancreatic cancer is known to have one of the worst prognoses of all cancers, and its tumor cells are highly resistant to chemotherapeutic drugs. Pancreatic cancer cells coexist with stromal cells; however, their involvement in anticancer drug resistance remains poorly understood. Thus, in this study, we analyzed drug sensitivity using an in vitro co-culture system containing pancreatic cancer cells and stromal cells treated with a compound library. MATERIALS AND METHODS: We examined the viability of the pancreatic cancer cell lines BxPC-3, Capan-1, and Panc-1 against compounds in an in vitro co-culture model containing pancreatic stromal cells (PSCs) and analyzed the protein expression for drug resistance by western blotting...
June 2023: Anticancer Research
https://read.qxmd.com/read/37225005/investigating-the-relevance-of-cyp2j2-inhibition-for-drugs-known-to-cause-intermediate-to-high-risk-torsades-de-pointes
#35
JOURNAL ARTICLE
Jacqueline Wen Hui Leow, Yuxiang Gu, Eric Chun Yong Chan
Cardiac cytochrome P450 2J2 (CYP2J2) metabolizes endogenous polyunsaturated fatty acid, arachidonic acid (AA), to bioactive regioisomeric epoxyeicosatrienoic acid (EET) metabolites. This endogenous metabolic pathway has been postulated to play a homeostatic role in cardiac electrophysiology. However, it is unknown if drugs that cause intermediate to high risk torsades de pointes (TdP) exhibit inhibitory effects against CYP2J2 metabolism of AA to EETs. In this study, we demonstrated that 11 out of 16 drugs screened with intermediate to high risk of TdP as defined by the Comprehensive in vitro Proarrhythmia Assay (CiPA) initiative are concurrently reversible inhibitors of CYP2J2 metabolism of AA, with unbound inhibitory constant (Ki,AA,u ) values ranging widely from 0...
May 22, 2023: European Journal of Pharmaceutical Sciences
https://read.qxmd.com/read/37170983/traditional-chinese-medicine-targeting-sarcoma-virus-oncogene-related-diseases
#36
JOURNAL ARTICLE
Yiying Wang, Xiaoyu Wang, Kexin Su, Yifu Yang
The sarcoma virus oncogene (Src) tyrosine kinase, a nonreceptor protein-tyrosine kinase, plays a crucial role in cell survival, migration, differentiation and proliferation. The study of Src has developed considerably since it was first discovered as a proto-oncogene. Src has also been associated with inflammation and bone-related diseases. Src inhibitors (bosutinib, ponatinib, dasatinib, and vandetanib) have been put into clinical use. However, their side effects and cardiovascular toxicity may be a concern...
April 26, 2023: Current Cancer Drug Targets
https://read.qxmd.com/read/37111291/structure-activity-relationship-studies-based-on-quinazoline-derivatives-as-egfr-kinase-inhibitors-2017-present
#37
REVIEW
Alexandru Șandor, Ioana Ionuț, Gabriel Marc, Ilioara Oniga, Dan Eniu, Ovidiu Oniga
The epidermal growth factor receptor (EGFR) plays a critical role in the tumorigenesis of various forms of cancer. Targeting the mutant forms of EGFR has been identified as an attractive therapeutic approach and led to the approval of three generations of inhibitors. The quinazoline core has emerged as a favorable scaffold for the development of novel EGFR inhibitors due to increased affinity for the active site of EGFR kinase. Currently, there are five first-generation (gefitinib, erlotinib, lapatinib, vandetanib, and icotinib) and two second-generation (afatinib and dacomitinib) quinazoline-based EGFR inhibitors approved for the treatment of various types of cancers...
April 3, 2023: Pharmaceuticals
https://read.qxmd.com/read/37067769/metabolic-adverse-events-of-multitarget-kinase-inhibitors-a-systematic-review
#38
REVIEW
Elisa Acitelli, Carlo Maiorca, Giorgio Grani, Marianna Maranghi
PURPOSE: Multitargeted kinase inhibitors (MKIs) are used for the treatment of several cancers. By targeting multiple signaling pathways, MKIs have become cornerstones of the oncologic treatment. Although their use leads to important results in terms of survival, treatment with MKIs can determine important side effects the clinician must be aware of. Among those, arterial hypertension, mucositis and skin lesions are universally reported, while data about metabolic alterations are scarce...
July 2023: Endocrine
https://read.qxmd.com/read/37061272/vandetanib
#39
JOURNAL ARTICLE
Ahmed I Al-Ghusn, Ahmed H Bakheit, Mohamed W Attwa, Haitham AlRabiah
Vandetanib is an anti-cancer drug called an antineoplastic kinase inhibitor. The FDA authorized vandetanib on April6, 2011 for the treatment of nonresectable, locally progressed, or metastatic medullary thyroid carcinoma in adults. Because Vandetanib can make the Q-T interval last longer, it shouldn't be given to people with serious heart problems like congenital long QT syndrome or heart failure that hasn't been fixed yet. This chapter provides an overview of Vandetanib's physical and molecular properties, mode of action, pharmacokinetics, and common applications...
2023: Profiles of Drug Substances, Excipients, and related Methodology
https://read.qxmd.com/read/36975442/initial-experiences-of-selective-ret-inhibitor-selpercatinib-in-adults-with-metastatic-differentiated-thyroid-carcinoma-and-medullary-thyroid-carcinoma-real-world-case-series-in-korea
#40
Han-Sang Baek, Jeonghoon Ha, Seunggyun Ha, Ja Seong Bae, Chan Kwon Jung, Dong-Jun Lim
Recently, selpercatinib, a highly selective inhibitor of RET receptor tyrosine kinase, has been used for RET -altered thyroid cancer. We present four cases of patients with advanced thyroid cancer who were treated with selpercatinib. The first patient was a 63-year-old male with advanced medullary thyroid cancer (MTC) treated with vandetanib. Six months ago, he had an intracranial hemorrhage and swallowing difficulty. He started selpercatinib with percutaneous endoscopic gastrostomy (PEG). For 11 months, a partial response (PR) was observed stably with PEG administration without any more cardiovascular events...
March 3, 2023: Current Oncology
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