Results 51 to 60 of about 21,933 (136)

Kinetic Fingerprints as Mechanistic and Clinical Roadmaps Across KIT Activation States

ChemMedChem, Volume 21, Issue 11, 15 June 2026.
Kinetic profiling of 172 compounds across KIT conformations—including D816V—reveals kinetic fingerprints that predict efficacy, selectivity, resistance, and inhibitors’ ability to stabilize key regulatory elements. Far from a secondary metric, binding kinetics provide mechanistic insights beyond affinity, offering a powerful framework for rational drug
Ana Corrionero, Niall Prendiville, Tatiana Cazorla, Maria Baena‐Nuevo, Röhm Sandra, Emilio Camafeita, Stefan Knapp, Patricia Alfonso   +7 more
wiley   +1 more source

Abcg2 overexpression represents a novel mechanism for acquired resistance to the multi-kinase inhibitor Danusertib in BCR-ABL-positive cells in vitro. [PDF]

, 2011
The success of Imatinib (IM) therapy in chronic myeloid leukemia (CML) is compromised by the development of IM resistance and by a limited IM effect on hematopoietic stem cells.
Carsten Bokemeyer, Balabanov, S., Moll, J., Tessa L. Holyoake, Edgar Jost, Braig, Melanie, Stefan Balabanov, Moll, Jürgen, Rohe, Imke, Gontarewicz, A., Gunhild Keller, von Amsberg, Gunhild, Braig, M., Holyoake, Tessa L., Jost, E., Rohe, I., Jost, Edgar, Bosotti, Roberta, Tim H Brümmendorf, Bosotti, R., Balabanov, Stefan, Barett, Christine, Artur Gontarewicz, Holyoake, T.L., Laura Raddrizzani, Brümmendorf, T.H., Gontarewicz, Artur, Roberta Bosotti, Barett, C., Raddrizzani, Laura, Melanie Braig, Raddrizzani, L., Bokemeyer, C., Jürgen Moll, Tessa L Holyoake, Keller, G., Tim H. Brümmendorf, Bokemeyer, Carsten, Brümmendorf, Tim Henrik, Imke Rohe, Christine Barett   +40 more
core   +2 more sources

Hepatic metastasis with heterologous rhabdomyoblastic differentiation in a patient with gastrointestinal stromal tumor treated with imatinib

Indian Journal of Pathology and Microbiology, 2013
Gastrointestinal stromal tumors (GISTs) are the most common mesenchymal tumors of the intestinal tract. In patients with locally advanced and/or metastatic GIST, the introduction of tyrosine kinase inhibitor, imatinib mesylate, has transformed the ...
Mukul Vij, Susama Patra, Mohamed Rela
doaj   +1 more source

Lethal and Sub-Lethal Effects and Modulation of Gene Expression Induced by T Kinase Inhibitors in Zebrafish (Danio Rerio) Embryos

Toxics, 2021
Tyrosine kinase inhibitors (TKIs) are designed for targeted cancer therapy. The consumption of these drugs during the last 20 years has been constantly rising.
Tina Elersek, Matjaž Novak, Mateja Mlinar, Igor Virant, Nika Bahor, Karin Leben, Bojana Žegura, Metka Filipič   +7 more
doaj   +1 more source

Integrating Single‐Cell and Spatial Transcriptomes in HGSOC to Decipher the Metastasis‐Associated Biomarkers

iNew Medicine, Volume 2, Issue 2, June 2026.
ABSTRACT High‐grade serous ovarian cancer (HGSOC) is the most common and lethal histological subtype of ovarian cancer. This study aimed to identify peritoneal metastasis‐associated biomarkers of HGSOC to provide directions for subsequent treatment. Transcriptome data were extracted from the GEO database and literature. Differential expression analysis,
Jing Zhu, Zhicheng Yu, Yang Zhang, Hui Hong, Xiaoli Wang, Shan Jiang, Ying Zhou, Cheng Peng, Hongbo Chen   +8 more
wiley   +1 more source

Treatment of gastrointestinal stromal tumor: focus on imatinib mesylate [PDF]

, 2008
Omar S Din, Penella J WollAcademic Department of Clinical Oncology, University of Sheffield, Weston Park Hospital, Sheffield, UKAbstract: Gastrointestinal stromal tumor (GIST) is a rare primary neoplasm of the gastrointestinal tract, mesentery, or ...
Woll, P.J., Din, O.S., Omar S Din, Penella J Woll   +3 more
core   +1 more source

Hyperpigmentation of the hard palate mucosa in a patient with chronic myeloid leukaemia taking imatinib

Maxillofacial Plastic and Reconstructive Surgery, 2017
Background Imatinib mesylate is an inhibitor of the tyrosine kinase Bcr–Abl and a first-line treatment for Philadelphia chromosome-positive chronic myeloid leukaemia (CML).
Gian Paolo Bombeccari, Umberto Garagiola, Francesco Pallotti, Margherita Rossi, Massimo Porrini, Aldo Bruno Giannì, Francesco Spadari   +6 more
doaj   +1 more source

Formulation and in vitro, in vivo evaluation of effervescent floating sustained-release imatinib mesylate tablet. [PDF]

PLoS ONE, 2015
Imatinib mesylate is an antineoplastic agent which has high absorption in the upper part of the gastrointestinal tract (GIT). Conventional imatinib mesylate (Gleevec) tablets produce rapid and relatively high peak blood levels and requires frequent ...
Ali Kadivar, Behnam Kamalidehghan, Hamid Akbari Javar, Ehsan Taghizadeh Davoudi, Nurul Dhania Zaharuddin, Bahareh Sabeti, Lip Yong Chung, Mohamed Ibrahim Noordin   +7 more
doaj   +1 more source

Uveitis – A side effect of imatinib mesylate

Indian Journal of Ophthalmology. Case Reports, 2023
Imatinib mesylate, a BCR-ABL tyrosine kinase inhibitor, is widely used in the management of chronic myeloid leukemia (CML). Although there are a few studies documenting ocular side effects of imatinib, there have been no reports of uveitis caused by ...
BN Kalpana, Akhila Mathew, BC Hemalatha, YD Shilpa   +3 more
doaj   +1 more source

The Dual Role of Autophagy in Cancer: Mechanisms and Therapeutic Strategies

MedComm – Oncology, Volume 5, Issue 2, June 2026.
Autophagy is a conserved cellular process degrading dysfunctional organelles and protein aggregates to maintain cell homeostasis, and it exhibits context‐dependent duality in cancer. Autophagy functions as a critical tumor‐suppressive mechanism by preventing DNA damage and mutation during tumor initiation.
Xiang‐Zheng Gao, Yuheng Qin, Haoyu Wan, Guang Lu, Han‐Ming Shen   +4 more
wiley   +1 more source