Results 41 to 50 of about 4,906,436 (344)

Activation of tyrosine kinases by mutation of the gatekeeper threonine. [PDF]

, 2008
Protein kinases targeted by small-molecule inhibitors develop resistance through mutation of the gatekeeper threonine residue of the active site. Here we show that the gatekeeper mutation in the cellular forms of c-ABL, c-SRC, platelet-derived growth ...
Azam, Mohammad, Daley, George, Gray, Nathanael, KURIYAN, John, Seeliger, Markus   +4 more
core   +1 more source

Analysis of Tumor Heterogeneity Through AXL Activation in Primary Resistance to EGFR Tyrosine Kinase Inhibitors

JTO Clinical and Research Reports, 2023
Introduction: EGFR tyrosine kinase inhibitors are standard therapeutic agents for patients with advanced NSCLC harboring EGFR mutations. Nevertheless, some patients exhibit primary resistance to EGFR tyrosine kinase inhibitors in the first-line treatment
Ryota Nakamura, MD, Hiroyuki Fujii, MD, Tadaaki Yamada, MD, PhD, Yohei Matsui, MD, Takeshi Yaoi, MS, Mizuki Honda, MD, Noriyuki Tanaka, MD, PhD, Aya Miyagawa-Hayashino, MD, PhD, Akihiro Yoshimura, MD, PhD, Kenji Morimoto, MD, PhD, Masahiro Iwasaku, MD, PhD, Shinsaku Tokuda, MD, PhD, Young Hak Kim, MD, PhD, Eiichi Konishi, MD, PhD, Kyoko Itoh, MD, PhD, Koichi Takayama, MD, PhD   +15 more
doaj   +1 more source

Computerized Protein Modeling and Molecular Docking Analysis of Human Proto Oncogene Tyrosine Protein Kinase YES for Discovery of Novel Lead Molecules [PDF]

, 2010
Human proto-oncogene tyrosine-protein kinase YES (YES) is a non receptor kinase belongs to Src family. This gene lies in close proximity to thymidylate synthase gene on chromosome 18, and a corresponding pseudogene has been found on chromosome 22.
Amineni Umamaheswari, Dibyabhaba Pradhan, Karuna J. Jaya Sai   +2 more
core   +2 more sources

Marine-derived protein kinase inhibitors for neuroinflammatory diseases

BioMedical Engineering OnLine, 2018
Neuroinflammation is primarily characterized by overexpression of proinflammatory mediators produced by glial activation or immune cell infiltration. Several kinases have been shown to be critical mediators in neuroinflammation. One of the largest groups
Chong Ning, Hui-Min David Wang, Rong Gao, Yu-Chia Chang, Fengqing Hu, Xianjun Meng, Shi-Ying Huang   +6 more
doaj   +1 more source

Recent advances on anti-angiogenesis receptor tyrosine kinase inhibitors in cancer therapy

Journal of Hematology & Oncology, 2019
Angiogenesis has always been the topic of major scientific interest in the field of malignant tumors. Nowadays, targeting angiogenesis has achieved success in various carcinomas by several mechanisms, including the use of anti-angiogenic small molecule ...
Shuang Qin, Anping Li, Ming Yi, Shengnan Yu, Mingsheng Zhang, Kongming Wu   +5 more
semanticscholar   +1 more source

Targeting phosphoinositide 3-kinase (PI3K) in head and neck squamous cell carcinoma (HNSCC). [PDF]

, 2018
The landscape of head and neck squamous cell carcinoma (HNSCC) has been changing rapidly due to growing proportion of HPV-related disease and development of new therapeutic agents.
Jung, Kyungsuk, Kang, Hyunseok, Mehra, Ranee   +2 more
core   +2 more sources

Properties of FDA-approved small molecule protein kinase inhibitors: a 2024 update.

Pharmacological Research
Owing to the dysregulation of protein kinase activity in many diseases including cancer, this enzyme family has become one of the most important drug targets in the 21st century.
R. Roskoski
semanticscholar   +1 more source

Non-linear Deep Neural Network for Rapid and Accurate Prediction of Phenotypic Responses to Kinase Inhibitors

iScience, 2020
Summary: Protein kinase inhibitors are one of the most successful targeted therapies to date. Despite this progress, additional kinase inhibitors are needed to expand the target space as well as overcome drug resistance that has emerged in clinical ...
Siddharth Vijay, Taranjit S. Gujral
doaj   +1 more source

SnapShot: Kinase Inhibitors I

Molecular Cell, 2015
Selective small-molecule inhibitors of protein kinases can serve as powerful tools to elucidate biological function. Efforts to develop potential drug candidates have yielded a wealth of kinase inhibitors. However, selecting the optimal kinase inhibitor for a particular application can be challenging.
Wang, Jinhua, Gray, Nathanael S.
openaire   +3 more sources

Kinase profiling of liposarcomas using RNAi and drug screening assays identified druggable targets. [PDF]

, 2017
BackgroundLiposarcoma, the most common soft tissue tumor, is understudied cancer, and limited progress has been made in the treatment of metastatic disease.
Doan, Ngan B, Forscher, Charles, Garg, Manoj, Kanojia, Deepika, Koeffler, H Phillip, Luty, Samuel B, M T, Anand, Martinez, Jacqueline, Said, Jonathan W, Tyner, Jeffrey W   +9 more
core   +2 more sources