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Journal articles on the topic 'Lapatinib: Chemistry'

Author: Grafiati

Published: 2 June 2025

Last updated: 31 July 2025

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1

Akash, Darekar* Dr. V. M. Satpute Ghodake S. R. "Overview of Lapatinib: Chemistry, Pharmacology, and Clinical Applications." International Journal of Pharmaceutical Sciences 3, no. 5 (2025): 3774–87. https://doi.org/10.5281/zenodo.15489237.

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The present study focuses on the development and validation of a sensitive, accurate, and reproducible bioanalytical method for the estimation of Lapatinib in active pharmaceutical ingredient (API) form and marketed formulations using human plasma. Lapatinib, a dual tyrosine kinase inhibitor used in the treatment of HER2-positive breast cancer, requires precise quantification in biological matrices for effective pharmacokinetic and bioequivalence studies. A high-performance liquid chromatography (HPLC) method coupled with UV detection was developed for the extraction and quantification of Lapa

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Huynh, Thanh Kieu, Chien-Yi Ho, Chi-Hua Tsai, et al. "Proteasome Inhibitors Suppress ErbB Family Expression through HSP90-Mediated Lysosomal Degradation." International Journal of Molecular Sciences 20, no. 19 (2019): 4812. http://dx.doi.org/10.3390/ijms20194812.

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Although dual EGFR/HER2 tyrosine kinase inhibitor lapatinib has provided effective clinical benefits for HER2-positive breast cancer patients, acquired resistance to this drug remains a major concern. Thus, the development of alternative therapeutic strategies is urgently needed for patients who failed lapatinib treatment. Proteasome inhibitors have been reported to possess high anti-tumor activity to breast cancer cells. Therefore, this study aims to examine whether and how proteasome inhibitor bortezomib can overcome lapatinib resistance. Treatments with several proteasome inhibitors, includ

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January, Jaymi Leigh, Ziyanda Zamaswazi Tshobeni, Nokwanda Precious Pearl Ngema, et al. "Novel Cytochrome P450-3A4 Enzymatic Nanobiosensor for Lapatinib (a Breast Cancer Drug) Developed on a Poly(anilino-co-4-aminobenzoic Acid-Green-Synthesised Indium Nanoparticle) Platform." Biosensors 13, no. 9 (2023): 897. http://dx.doi.org/10.3390/bios13090897.

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Breast cancer (BC) is one of the most common types of cancer disease worldwide and it accounts for thousands of deaths annually. Lapatinib is among the preferred drugs for the treatment of breast cancer. Possible drug toxicity effects of lapatinib can be controlled by real-time determination of the appropriate dose for a patient at the point of care. In this study, a novel highly sensitive polymeric nanobiosensor for lapatinib is presented. A composite of poly(anilino-co-4-aminobenzoic acid) co-polymer {poly(ANI-co-4-ABA)} and coffee extract-based green-synthesized indium nanoparticles (InNPs)

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Walker, Rashidra R., Jankiben R. Patel, Akash Gupta, et al. "Glyceollins Trigger Anti-Proliferative Effects in Hormone-Dependent Aromatase-Inhibitor-Resistant Breast Cancer Cells through the Induction of Apoptosis." International Journal of Molecular Sciences 23, no. 5 (2022): 2887. http://dx.doi.org/10.3390/ijms23052887.

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Aromatase inhibitors (AIs) are standard treatment for estrogen-dependent postmenopausal breast tumors; however, resistance develops leading to tumor relapse and metastasis. We previously demonstrated that glyceollin inhibits proliferation, survival, and migration of hormone-independent letrozole-resistant breast cancer. Since many AI-resistant tumors remain hormone-dependent, identifying distinctions between estrogen-receptor-positive (ER+) and ER-negative (ER-) AI-resistant tumor response to therapy is critical. We hypothesize that treating ER+ letrozole-resistant T47D breast cancer cells (T4

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Behera, Ranjan, Sarah M. Thomas, and Kojo Mensa-Wilmot. "New Chemical Scaffolds for Human African Trypanosomiasis Lead Discovery from a Screen of Tyrosine Kinase Inhibitor Drugs." Antimicrobial Agents and Chemotherapy 58, no. 4 (2014): 2202–10. http://dx.doi.org/10.1128/aac.01691-13.

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ABSTRACTHuman African trypanosomiasis (HAT) is caused by the protozoanTrypanosoma brucei. New drugs are needed to treat HAT because of undesirable side effects and difficulties in the administration of the antiquated drugs that are currently used. In human proliferative diseases, protein tyrosine kinase (PTK) inhibitors (PTKIs) have been developed into drugs (e.g., lapatinib and erlotinib) by optimization of a 4-anilinoquinazoline scaffold. Two sets of facts raise a possibility that drugs targeted against human PTKs could be “hits” for antitrypanosomal lead discoveries. First, trypanosome prot

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Kang, Jia, Zanzan Guo, Haoqi Zhang, Rongqi Guo, Xiaofei Zhu, and Xiaofang Guo. "Dual Inhibition of EGFR and IGF-1R Signaling Leads to Enhanced Antitumor Efficacy against Esophageal Squamous Cancer." International Journal of Molecular Sciences 23, no. 18 (2022): 10382. http://dx.doi.org/10.3390/ijms231810382.

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Both the epidermal growth factor receptor (EGFR) and insulin-like growth factor 1 receptor (IGF-1R) have been implicated in the development of cancers, and the increased expression of both receptors has been observed in esophageal cancer. However, the tyrosine kinase inhibitors of both receptors have thus far failed to provide clinical benefits for esophageal cancer patients. Studies have confirmed the complicated crosstalks that exist between the EGFR and IGF-1R pathways. The EGFR and IGF-1R signals act as mutual compensation pathways, thereby conveying resistance to EGFR or IGF-1R inhibitors

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Achounna, Angèle Sorel, David Ordaz-Rosado, Janice García-Quiroz, et al. "EB1089 Increases the Antiproliferative Response of Lapatinib in Combination with Antiestrogens in HER2-Positive Breast Cancer Cells." International Journal of Molecular Sciences 25, no. 6 (2024): 3165. http://dx.doi.org/10.3390/ijms25063165.

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HER2-positive breast cancer is associated with aggressive behavior and reduced survival rates. Calcitriol restores the antiproliferative activity of antiestrogens in estrogen receptor (ER)-negative breast cancer cells by re-expressing ERα. Furthermore, calcitriol and its analog, EB1089, enhance responses to standard anti-cancer drugs. Therefore, we aimed to investigate EB1089 effects when added to the combined treatment of lapatinib and antiestrogens on the proliferation of HER2-positive breast cancer cells. BT-474 (ER-positive/HER2-positive) and SK-BR-3 (ER-negative/HER2-positive) cells were

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Yamaura, Kei, Keiko Kuwata, Tomonori Tamura, et al. "Live cell off-target identification of lapatinib using ligand-directed tosyl chemistry." Chem. Commun. 50, no. 91 (2014): 14097–100. http://dx.doi.org/10.1039/c4cc05885b.

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9

Clayton, Natasha S., Edward P. Carter, Abbie E. Fearon, et al. "HDAC Inhibition Restores Response to HER2-Targeted Therapy in Breast Cancer via PHLDA1 Induction." International Journal of Molecular Sciences 24, no. 7 (2023): 6228. http://dx.doi.org/10.3390/ijms24076228.

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The downregulation of Pleckstrin Homology-Like Domain family A member 1 (PHLDA1) expression mediates resistance to targeted therapies in receptor tyrosine kinase-driven cancers. The restoration and maintenance of PHLDA1 levels in cancer cells thus constitutes a potential strategy to circumvent resistance to inhibitors of receptor tyrosine kinases. Through a pharmacological approach, we identify the inhibition of MAPK signalling as a crucial step in PHLDA1 downregulation. Further ChIP-qPCR analysis revealed that MEK1/2 inhibition produces significant epigenetic changes at the PHLDA1 locus, spec

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10

de Sousa, Ana Carolina C., Keletso Maepa, Jill M. Combrinck, and Timothy J. Egan. "Lapatinib, Nilotinib and Lomitapide Inhibit Haemozoin Formation in Malaria Parasites." Molecules 25, no. 7 (2020): 1571. http://dx.doi.org/10.3390/molecules25071571.

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With the continued loss of antimalarials to resistance, drug repositioning may have a role in maximising efficiency and accelerating the discovery of new antimalarial drugs. Bayesian statistics was previously used as a tool to virtually screen USFDA approved drugs for predicted β-haematin (synthetic haemozoin) inhibition and in vitro antimalarial activity. Here, we report the experimental evaluation of nine of the highest ranked drugs, confirming the accuracy of the model by showing an overall 93% hit rate. Lapatinib, nilotinib, and lomitapide showed the best activity for inhibition of β-haema

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Faizan, Syed, Sirajunisa Talath, Adil Farooq Wali, et al. "Anticancer potential of novel symmetrical and asymmetrical dihydropyridines against breast cancer via EGFR inhibition: molecular design, synthesis, analysis and screening." RSC Advances 14, no. 16 (2024): 11368–87. http://dx.doi.org/10.1039/d4ra01424c.

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Our study introduces novel symmetrical and asymmetrical dihydropyridines as breast cancer inhibitors, showing cytotoxicity against MCF-7 cells and EGFR kinase inhibition. Molecular docking and dynamics validate superior binding to Lapatinib.

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12

Ayubbi, Muhammad Reza Pahlevy Al, Rika Melati, and Umul Karimah. "PENAMBATAN MOLEKUL SIANIDIN Ipomoea batatas L. SEBAGAI INHIBITOR HUMAN EPIDERMAL RECEPTOR 2 (HER-2) PADA KANKER PAYUDARA." Journal of Sustainable Transformation 1, no. 2 (2023): 60–67. http://dx.doi.org/10.59310/jst.v1i2.14.

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HER-2 (Human Epidermal Receptor 2) is a receptor on the cell surface that affects cell proliferation, this receptor support controls healthy cell growth,divide and repair cells when they are damaged. When HER-2 had overexpressed will not controlled cancer cell division. Overexpressed HER-2 could inhibited with cyanidine compound flavonoid derivatives from Ipomoea batatas L. (purple sweet potato). This study aim to measured potential of Ipomoea batatas L. cyanidin compounds in inhibited overexpressed HER-2 using computational chemistry methods specifically is molecular docking. Stages of molecu

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13

Bitay, Enikő, Attila Levente Gergely, József Kántor, and Zoltán-István Szabó. "Evaluation of Lapatinib-Loaded Microfibers Prepared by Centrifugal Spinning." Polymers 14, no. 24 (2022): 5557. http://dx.doi.org/10.3390/polym14245557.

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Lapatinib (Lap) is a lypophilic drug frequently used in cancer treatment; however, due to its limited solubility and permeability, achieving therapeutic dose through oral administration proves to be a challenge. There are various methods for enhancing the solubility of Lap and other similar drugs, one being the preparation of amorphous solid dispersions (ASD). In this study, a Lap-loaded polyvinylpyrrolidone (PVP) fiber mat was created with centrifugal spinning from a PVP/Lap solution in dimethyl formamide and ethanol. The production rate was 12.2 g/h dry fibers, and the fibers had an average

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14

Kitagawa, Daisuke, Masaki Gouda, and Yasuyuki Kirii. "Quick Evaluation of Kinase Inhibitors by Surface Plasmon Resonance Using Single-Site Specifically Biotinylated Kinases." Journal of Biomolecular Screening 19, no. 3 (2013): 453–61. http://dx.doi.org/10.1177/1087057113506051.

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In evaluating kinase inhibitors, kinetic parameters such as association/dissociation rate constants are valuable information, as are equilibrium parameters KD and IC50 values. Surface plasmon resonance (SPR) is a powerful technique to investigate these parameters. However, results are often complicated because of impaired conformations by inappropriate conditions required for protein immobilization and/or heterogeneity of the orientation of immobilization. In addition, conventional SPR experiments are generally time-consuming. Here we introduce the use of single-site specifically biotinylated

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15

Tseng, Yu-Kai, Chun-Feng Chen, Chih-Wen Shu, et al. "Effect of EGFR on SQSTM1 Expression in Malignancy and Tumor Progression of Oral Squamous Cell Carcinoma." International Journal of Molecular Sciences 22, no. 22 (2021): 12226. http://dx.doi.org/10.3390/ijms222212226.

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Oral squamous cell carcinoma (OSCC) is one of the most common types of malignant tumor. Sequestosome 1 (SQSTM1) serves as an adaptor of autophagy for degrading protein aggregates. The regulation of autophagy by EGFR and its clinical impacts are indicated in various types of cancer. However, the association of EGFR and SQSTM1 in OSCC is still unknown. Our results show that the expression levels of SQSTM1 and EGFR proteins are higher in tumor tissues than in the corresponding tumor-adjacent (CTAN) tissues of OSCC patients. The expression levels of SQSTM1 were positively associated with the EGFR

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16

Levit, Shani L., Narendar Reddy Gade, Thomas D. Roper, Hu Yang, and Christina Tang. "Self-Assembly of pH-Labile Polymer Nanoparticles for Paclitaxel Prodrug Delivery: Formulation, Characterization, and Evaluation." International Journal of Molecular Sciences 21, no. 23 (2020): 9292. http://dx.doi.org/10.3390/ijms21239292.

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The efficacy of paclitaxel (PTX) is limited due to its poor solubility, poor bioavailability, and acquired drug resistance mechanisms. Designing paclitaxel prodrugs can improve its anticancer activity and enable formulation of nanoparticles. Overall, the aim of this work is to improve the potency of paclitaxel with prodrug synthesis, nanoparticle formation, and synergistic formulation with lapatinib. Specifically, we improve potency of paclitaxel by conjugating it to α-tocopherol (vitamin E) to produce a hydrophobic prodrug (Pro); this increase in potency is indicated by the 8-fold decrease in

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17

Fakhry, Mariam M., Amr A. Mattar, Marwa Alsulaimany, Ebtesam M. Al-Olayan, Sara T. Al-Rashood, and Hatem A. Abdel-Aziz. "New Thiazolyl-Pyrazoline Derivatives as Potential Dual EGFR/HER2 Inhibitors: Design, Synthesis, Anticancer Activity Evaluation and In Silico Study." Molecules 28, no. 21 (2023): 7455. http://dx.doi.org/10.3390/molecules28217455.

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A new series of thiazolyl-pyrazoline derivatives (4a–d, 5a–d 6a, b, 7a–d, 8a, b, and 10a, b) have been designed and synthesized through the combination of thiazole and pyrazoline moieties, starting from the key building blocks pyrazoline carbothioamides (1a–b). These eighteen derivatives have been designed as anticipated EGFR/HER2 dual inhibitors. The efficacy of the developed compounds in inhibiting cell proliferation was assessed using the breast cancer MCF-7 cell line. Among the new synthesized thiazolyl-pyrazolines, compounds 6a, 6b, 10a, and 10b displayed potent anticancer activity toward

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18

Simion, Laurentiu, Iolanda Georgiana Augustin, Simona Ruxandra Volovat, et al. "HER2 Positive Breast Cancer Therapy - A Challenging and Continuously Moving Pathway – A Narrative Literature Review." Archives of Breast Cancer 10, no. 1 (2022): 15–25. http://dx.doi.org/10.32768/abc.202310115-25.

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Background: Alteration of the expression of human epidermal growth factor receptor-2 gene as an oncogenic pathway in breast cancer was first explored in the 1980'. Since then, tremendous progress has been made in treating HER2-positive breast cancer. Methods: We performed a narrative type review of the existing literature using as a starting point the PubMed database, investigated by keywords, later the search being refined and the articles that we considered relevant were selected. The approach to the topic under discussion being variable in the various studies identified convinced us of the

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Imami, Koshi, Naoyuki Sugiyama, Haruna Imamura, et al. "Temporal Profiling of Lapatinib-suppressed Phosphorylation Signals in EGFR/HER2 Pathways." Molecular & Cellular Proteomics 11, no. 12 (2012): 1741–57. http://dx.doi.org/10.1074/mcp.m112.019919.

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Wang, Jun, Feng-Mei Lv, Dong-Li Wang, et al. "Synergistic Antitumor Effects on Drug-Resistant Breast Cancer of Paclitaxel/Lapatinib Composite Nanocrystals." Molecules 25, no. 3 (2020): 604. http://dx.doi.org/10.3390/molecules25030604.

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Drug resistance presents serious difficulties for cancer treatment. A combination of paclitaxel (PTX) and lapatinib (LAPA) shows potentials in multiple drug resistant cancers in the clinic, but it is almost impossible to deliver these two drugs to the tumor at the same time with the best proportion by simple co-administration of the respective current formualtions for their different pharmacokinetic profiles. Here composite nanocrystals of PTX and LAPA (cNC) were designed with a ratio of 2:1 (w/w), which was their intracellular ratio at the best synergistic efficacy on a drug-resistant cancer

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Uram, Łukasz, Konrad Wróbel, Małgorzata Walczak, Żaneta Szymaszek, Magdalena Twardowska, and Stanisław Wołowiec. "Exploring the Potential of Lapatinib, Fulvestrant, and Paclitaxel Conjugated with Glycidylated PAMAM G4 Dendrimers for Cancer and Parasite Treatment." Molecules 28, no. 17 (2023): 6334. http://dx.doi.org/10.3390/molecules28176334.

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Fulvestrant (F), lapatinib (L), and paclitaxel (P) are hydrophobic, anticancer drugs used in the treatment of estrogen receptor (ER) and epidermal growth factor receptor (EGFR)-positive breast cancer. In this study, glycidylated PAMAM G4 dendrimers, substituted with F, L, and/or P and targeting tumor cells, were synthesized and characterized, and their antitumor activity against glioma U-118 MG and non-small cell lung cancer A549 cells was tested comparatively with human non-tumorogenic keratinocytes (HaCaT). All cell lines were ER+ and EGFR+. In addition, the described drugs were tested in th

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Bello, Martiniano, Concepción Guadarrama-García, and Rolando Alberto Rodriguez-Fonseca. "Dissecting the molecular recognition of dual lapatinib derivatives for EGFR/HER2." Journal of Computer-Aided Molecular Design 34, no. 3 (2019): 293–303. http://dx.doi.org/10.1007/s10822-019-00270-4.

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Bitay, E., A. L. Gergely, I. Balint, et al. "Preparation and characterization of lapatinib-loaded PVP nanofiber amorphous solid dispersion by electrospinning." Express Polymer Letters 15, no. 11 (2021): 1041–50. http://dx.doi.org/10.3144/expresspolymlett.2021.84.

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Dehghankelishadi, Pouya, Ebrahim Saadat, Fatemeh Ravar, et al. "In vitro and in vivo evaluation of paclitaxel–lapatinib-loaded F127 pluronic micelles." Drug Development and Industrial Pharmacy 43, no. 3 (2016): 390–98. http://dx.doi.org/10.1080/03639045.2016.1254238.

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Gao, Huile, Zhi Yang, Shijie Cao, et al. "Behavior and anti-glioma effect of lapatinib-incorporated lipoprotein-like nanoparticles." Nanotechnology 23, no. 43 (2012): 435101. http://dx.doi.org/10.1088/0957-4484/23/43/435101.

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Liu, Yansong, Yiyi Shi, Hang Cheng, et al. "Lapatinib Acts against Biofilm Formation and the Hemolytic Activity of Staphylococcus aureus." ACS Omega 7, no. 10 (2022): 9004–14. http://dx.doi.org/10.1021/acsomega.2c00174.

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Wang, Chenghui, Qing Tang, Yunyun Xi, et al. "A Turn-On Supramolecular Fluorescent Probe for Sensing Lapatinib and Its Application in Living Cell Imaging." Chinese Journal of Organic Chemistry 38, no. 6 (2018): 1394. http://dx.doi.org/10.6023/cjoc201711018.

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28

Shi, YeHui, Wei Zhang, Lixin Li, ZhongSheng Tong, and CuiGai Bai. "Design and synthesis of novel triazolo-lapatinib hybrids as inhibitors of breast cancer cells." Medicinal Chemistry Research 27, no. 11-12 (2018): 2437–45. http://dx.doi.org/10.1007/s00044-018-2247-0.

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de Araujo, Gabriel L. B., Matthias Zeller, Daniel Smith, Haichen Nie, and Stephen R. Byrn. "Unexpected Single Crystal Growth Induced by a Wire and New Crystalline Structures of Lapatinib." Crystal Growth & Design 16, no. 10 (2016): 6122–30. http://dx.doi.org/10.1021/acs.cgd.6b01271.

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Athar, Mohd, Prabodh Ranjan, and Prakash C. Jha. "A DFT study of inclusion complexes of substituted calix[n]arenes with dasatinib and lapatinib." Journal of Molecular Graphics and Modelling 84 (September 2018): 160–65. http://dx.doi.org/10.1016/j.jmgm.2018.06.018.

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Vayá, Ignacio, Inmaculada Andreu, Emilio Lence, et al. "Characterization of Locally Excited and Charge‐Transfer States of the Anticancer Drug Lapatinib by Ultrafast Spectroscopy and Computational Studies." Chemistry – A European Journal 26, no. 68 (2020): 15922–30. http://dx.doi.org/10.1002/chem.202001336.

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Guzmán Rodríguez, Andy Guzmán, Marquiza Sablón Sablón Carrazana, Chrislayne Rodríguez Rodríguez Tanty, Martijn J. A. Malessy, Gastón Fuentes, and Luis J. Cruz. "Smart Polymeric Micelles for Anticancer Hydrophobic Drugs." Cancers 15, no. 1 (2022): 4. http://dx.doi.org/10.3390/cancers15010004.

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Cancer has become one of the deadliest diseases in our society. Surgery accompanied by subsequent chemotherapy is the treatment most used to prolong or save the patient’s life. Still, it carries secondary risks such as infections and thrombosis and causes cytotoxic effects in healthy tissues. Using nanocarriers such as smart polymer micelles is a promising alternative to avoid or minimize these problems. These nanostructured systems will be able to encapsulate hydrophilic and hydrophobic drugs through modified copolymers with various functional groups such as carboxyls, amines, hydroxyls, etc.

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Wan, Xu, Xiaoyao Zheng, Xiaoying Pang, Zheming Zhang, and Qizhi Zhang. "Incorporation of lapatinib into human serum albumin nanoparticles with enhanced anti-tumor effects in HER2-positive breast cancer." Colloids and Surfaces B: Biointerfaces 136 (December 2015): 817–27. http://dx.doi.org/10.1016/j.colsurfb.2015.10.018.

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Ghadi, Rohan, Aaradhya Wadikar, Dharshini M., et al. "Advancing apoptosis induction in triple negative breast cancer: Empowering treatment with tyrosine-stapled mixed micelles of lapatinib." Journal of Molecular Liquids 401 (May 2024): 124635. http://dx.doi.org/10.1016/j.molliq.2024.124635.

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Dogan-Topal, Burcu, Burcin Bozal-Palabiyik, Sibel A. Ozkan, and Bengi Uslu. "Investigation of anticancer drug lapatinib and its interaction with dsDNA by electrochemical and spectroscopic techniques." Sensors and Actuators B: Chemical 194 (April 2014): 185–94. http://dx.doi.org/10.1016/j.snb.2013.12.088.

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Bonomi, Maria, Daniele Spada, Gian Luca Baiocchi, Andrea Celotti, Matteo Brighenti, and Giulia Grizzi. "Targeting HER2 in Gastroesophageal Adenocarcinoma: Molecular Features and Updates in Clinical Practice." International Journal of Molecular Sciences 25, no. 7 (2024): 3876. http://dx.doi.org/10.3390/ijms25073876.

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Gastroesophageal adenocarcinoma (GEA) is one of the principal causes of death related to cancer globally. Human epidermal growth factor receptor 2 (HER2) is a tyrosine kinase receptor which is found to be overexpressed or amplified in approximately 20% of GEA cases. In GEA, the identification of HER2-positive status is crucial to activate a specific anti-HER2 targeted therapy. The landmark ToGA trial demonstrated the superiority of adding trastuzumab to platinum-based chemotherapy, becoming the first-line standard of treatment. However, unlike breast cancer, the efficacy of other anti-HER2 dru

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Fujii, Kiyomu, Rina Fujiwara-Tani, Shota Nukaga, et al. "Involvement of Ferroptosis Induction and Oxidative Phosphorylation Inhibition in the Anticancer-Drug-Induced Myocardial Injury: Ameliorative Role of Pterostilbene." International Journal of Molecular Sciences 25, no. 5 (2024): 3015. http://dx.doi.org/10.3390/ijms25053015.

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Patients with cancer die from cardiac dysfunction second only to the disease itself. Cardiotoxicity caused by anticancer drugs has been emphasized as a possible cause; however, the details remain unclear. To investigate this mechanism, we treated rat cardiomyoblast H9c2 cells with sunitinib, lapatinib, 5-fluorouracil, and cisplatin to examine their effects. All anticancer drugs increased ROS, lipid peroxide, and iron (II) levels in the mitochondria and decreased glutathione peroxidase-4 levels and the GSH/GSSG ratio. Against this background, mitochondrial iron (II) accumulates through the unre

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Shioi, Ryuta, Fumika Karaki, Hiromasa Yoshioka, et al. "Image-based screen capturing misfolding status of Niemann-Pick type C1 identifies potential candidates for chaperone drugs." PLOS ONE 15, no. 12 (2020): e0243746. http://dx.doi.org/10.1371/journal.pone.0243746.

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Niemann-Pick disease type C is a rare, fatal neurodegenerative disorder characterized by massive intracellular accumulation of cholesterol. In most cases, loss-of-function mutations in the NPC1 gene that encodes lysosomal cholesterol transporter NPC1 are responsible for the disease, and more than half of the mutations are considered to interfere with the biogenesis or folding of the protein. We previously identified a series of oxysterol derivatives and phenanthridine-6-one derivatives as pharmacological chaperones, i.e., small molecules that can rescue folding-defective phenotypes of mutated

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Lee, Song Yi, and Hyun-Jong Cho. "Mitochondria Targeting and Destabilizing Hyaluronic Acid Derivative-Based Nanoparticles for the Delivery of Lapatinib to Triple-Negative Breast Cancer." Biomacromolecules 20, no. 2 (2018): 835–45. http://dx.doi.org/10.1021/acs.biomac.8b01449.

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Acconcia, Filippo. "Evaluation of the Sensitivity of Breast Cancer Cell Lines to Cardiac Glycosides Unveils ATP1B3 as a Possible Biomarker for the Personalized Treatment of ERα Expressing Breast Cancers". International Journal of Molecular Sciences 23, № 19 (2022): 11102. http://dx.doi.org/10.3390/ijms231911102.

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The molecular classification of breast cancer (BC) dictates pharmacological treatment. Estrogen receptor α (ERα) expressing tumors are treated with 4OH-tamoxifen or fulvestrant, which inhibits the receptor, or with aromatase inhibitors (i.e., anastrozole, letrozole, and exemestane) that reduce the 17β-estradiol (E2) circulating blood levels. Besides such endocrine therapy (ET) drugs, ERα-positive BCs can be treated with epidermal growth factor receptor (EGF-R) inhibitors (i.e., gefitinib, erlotinib, and lapatinib) according to HER2 expression. Notwithstanding these anti-BC drugs, novel persona

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Chang, Kai-Tun, Hsing-Ju Wu, Chien-Wei Liu, Chia-Ying Li, and Hung-Yu Lin. "A Novel Role of Arrhythmia-Related Gene KCNQ1 Revealed by Multi-Omic Analysis: Theragnostic Value and Potential Mechanisms in Lung Adenocarcinoma." International Journal of Molecular Sciences 23, no. 4 (2022): 2279. http://dx.doi.org/10.3390/ijms23042279.

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The early diagnosis, prognostic prediction, and personalized therapy of lung adenocarcinoma (LUAD) remains a challenging issue. KCNQ1 (potassium voltage-gated channel subfamily Q Member 1) is implicated in long QT syndrome (LQTS) and cardiac arrhythmia, while its significance in LUAD remains unclear. In this study, we aimed to explore the significance of KCNQ1 in terms of clinical value, tumor immunity, underlying mechanisms, and a precision medicine approach by means of multi-omics analysis. The association of KCNQ1 with LUAD was first explored. Both altered variants and high expression of KC

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Chi, Weiru, Bingqiu Xiu, Min Xiong, et al. "MNX1 Promotes Anti-HER2 Therapy Sensitivity via Transcriptional Regulation of CD-M6PR in HER2-Positive Breast Cancer." International Journal of Molecular Sciences 25, no. 1 (2023): 221. http://dx.doi.org/10.3390/ijms25010221.

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Although targeted therapy for human epidermal growth factor receptor 2 (HER2)-positive breast cancer has significantly prolonged survival time and improved patients’ quality of life, drug resistance has gradually emerged. This study explored the mechanisms underlying the effect of the motor neuron and pancreatic homeobox 1 (MNX1) genes on drug sensitivity in HER2-positive breast cancer. From July 2017 to 2018, core needle biopsies of HER2-positive breast cancer were collected from patients who received paclitaxel, carboplatin, and trastuzumab neoadjuvant therapy at our center. Based on treatme

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Xu, Shiyao, Yan Xiong, Rui Yao, et al. "A Novel ERK2 Degrader Z734 Induces Apoptosis of MCF–7 Cells via the HERC3/p53 Signaling Pathway." Molecules 27, no. 14 (2022): 4337. http://dx.doi.org/10.3390/molecules27144337.

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Breast cancer is one of the leading causes of death worldwide, and synthetic chemicals targeting specific proteins or various molecular pathways for tumor suppression, such as ERK inhibitors and degraders, have been intensively investigated. The targets of ERK participate in the regulation of critical cellular mechanisms and underpin the progression of anticancer therapy. In this study, we identified a novel small molecule, which we named Z734, as a new mitogen–activated protein kinase 1 (ERK2) degrader and demonstrated that Z734 inhibits cell growth by inducing p53–mediated apoptotic pathways

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Basuli, Falguni, Haitao Wu, Changhui Li, Zhen-Dan Shi, Agnieszka Sulima, and Gary L. Griffiths. "A first synthesis of 18F-radiolabeled lapatinib: a potential tracer for positron emission tomographic imaging of ErbB1/ErbB2 tyrosine kinase activity." Journal of Labelled Compounds and Radiopharmaceuticals 54, no. 9 (2011): 633–36. http://dx.doi.org/10.1002/jlcr.1898.

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Yang, Zehui, Danfeng Shao, and Guoquan Zhou. "Dissolution behavior and thermodynamic properties of lapatinib ditosylate in pure and mixed organic solvents from T = (283.15–323.15) K." Fluid Phase Equilibria 486 (May 2019): 91–97. http://dx.doi.org/10.1016/j.fluid.2019.01.005.

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Chang, Wei-Ting, Ping-Yen Liu, Kaisen Lee, Yin-Hsun Feng, and Sheng-Nan Wu. "Differential Inhibitory Actions of Multitargeted Tyrosine Kinase Inhibitors on Different Ionic Current Types in Cardiomyocytes." International Journal of Molecular Sciences 21, no. 5 (2020): 1672. http://dx.doi.org/10.3390/ijms21051672.

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Lapatinib (LAP) and sorafenib (SOR) are multitargeted tyrosine kinase inhibitors (TKIs) with antineoplastic properties. In clinical observations, LAP and SOR may contribute to QTc prolongation, but the detailed mechanism for this has been largely unexplored. In this study, we investigated whether LAP and SOR affect the activities of membrane ion channels. Using a small animal model and primary cardiomyocytes, we studied the impact of LAP and SOR on Na+ and K+ currents. We found that LAP-induced QTc prolongation in mice was reversed by isoproterenol. LAP or SOR suppressed the amplitude of the s

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Nishiguch, Yukiko, Rina Fujiwara-Tani, Shota Nukaga, et al. "Pterostilbene Induces Apoptosis from Endoplasmic Reticulum Stress Synergistically with Anticancer Drugs That Deposit Iron in Mitochondria." International Journal of Molecular Sciences 25, no. 5 (2024): 2611. http://dx.doi.org/10.3390/ijms25052611.

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Anticancer agents are playing an increasing role in the treatment of gastric cancer (GC); however, novel anticancer agents have not been fully developed. Therefore, it is important to investigate compounds that improve sensitivity to the existing anticancer drugs. We have reported that pterostilbene (PTE), a plant stilbene, enhances the antitumor effect of low doses of sunitinib in gastric cancer cells accumulating mitochondrial iron (II) (mtFe) at low doses. In this study, we investigated the relationship between the mtFe deposition and the synergistic effect of PTE and different anticancer d

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Mathad, Ayyapayya S., J. Seetharamappa та Shankara S. Kalanur. "β-Cyclodextrin anchored neem carbon dots for enhanced electrochemical sensing performance of an anticancer drug, lapatinib via host-guest inclusion". Journal of Molecular Liquids 350 (березень 2022): 118582. http://dx.doi.org/10.1016/j.molliq.2022.118582.

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Canino, Fabio, Federico Piacentini, Claudia Omarini, et al. "Role of Intrinsic Subtype Analysis with PAM50 in Hormone Receptors Positive HER2 Negative Metastatic Breast Cancer: A Systematic Review." International Journal of Molecular Sciences 23, no. 13 (2022): 7079. http://dx.doi.org/10.3390/ijms23137079.

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Endocrine therapy (ET), associated with CDK 4/6 inhibitors, represents the first choice of treatment for HR+/HER2- metastatic breast cancer (mBC). Primary or secondary endocrine resistance could develop; however validated biomarkers capable of predicting such a conditions are not available. Several studies have shown that HR+/HER2- mBC comprises five intrinsic subtypes. The purpose of this systematic review was to analyze the potential correlations between intrinsic subtype, efficacy of treatment, and patient outcome. Five papers that analyzed the intrinsic subtype with PAM50 assay in patients

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Tullemans, Bibian, Alicia Veninga, Delia Fernandez, et al. "Multiparameter Evaluation of the Platelet-Inhibitory Effects of Tyrosine Kinase Inhibitors Used for Cancer Treatment." International Journal of Molecular Sciences 22, no. 20 (2021): 11199. http://dx.doi.org/10.3390/ijms222011199.

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Current antiplatelet drugs for the treatment of arterial thrombosis often coincide with increased bleeding risk. Several tyrosine kinase inhibitors (TKIs) for cancer treatment inhibit platelet function, with minor reported bleeding symptoms. The aim of this study was to compare the antiplatelet properties of eight TKIs to explore their possible repurposing as antiplatelet drugs. Samples of whole blood, platelet-rich plasma (PRP), or isolated platelets from healthy donors were treated with TKI or the vehicle. Measurements of platelet aggregation, activation, intracellular calcium mobilization,

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