Kinetic modelling of in vitro data of PI3K, mTOR1, PTEN enzymes and on-target inhibitors Rapamycin, BEZ235, and LY294002 [PDF]
, 2016 The phosphatidylinositide 3-kinases (PI3K) and mammalian target of rapamycin-1 (mTOR1) are two key targets for anti-cancer therapy. Predicting the response of the PI3K/AKT/mTOR1 signalling pathway to targeted therapy is made difficult because of network ...
Bown, James L. +4 more
core +3 more sources
Journal of Enzyme Inhibition and Medicinal Chemistry, 2023 Phosphoinositide 3-kinases (PI3K) and phosphoinositide 3-kinase-related protein kinases (PIKK) are two structurally related families of kinases that play vital roles in cell growth and DNA damage repair.
Xueqin Huang +11 more
doaj +1 more source
Development of inhibitors for protein tyrosine kinases [PDF]
Oncogene, 2000 In the last 5 years, through combinatorial chemistry, high-throughput screening, computational chemistry, and traditional medicinal chemistry, numerous inhibitors for various protein tyrosine kinases (PTKs) have been developed. The majority of these compounds are small molecules that compete at the ATP binding site of the catalytic domain of the ...
Kit S. Lam, Fahad Al-Obeidi
openaire +3 more sources
The dynamic switch mechanism that leads to activation of LRRK2 is embedded in the DFGψ motif in the kinase domain. [PDF]
, 2019 Leucine-rich repeat kinase 2 (LRRK2) is a large multidomain protein, and LRRK2 mutants are recognized risk factors for Parkinson's disease (PD). Although the precise mechanisms that control LRRK2 regulation and function are unclear, the importance of the
Boassa, Daniela +7 more
core
Resistance is futile: overcoming resistance to targeted therapies in lung adenocarcinoma. [PDF]
, 2017 The advent of genomics has led to the identification of specific "driver" mutations in oncogenic kinases, and the development of targeted small molecule inhibitors to block their tumor-driving functions.
Bivona, Trever G, Neel, Dana S
core +1 more source
Nature Communications, 2020 Cardiotoxic adverse events associated with kinase inhibitors are a growing concern in clinical oncology. Here the authors use cellular transcriptomic responses of human cardiomyocytes treated with protein kinase inhibitors and the associated drug ...
J. G. Coen van Hasselt +16 more
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Aurora Kinase B Inhibition: A Potential Therapeutic Strategy for Cancer
Molecules, 2021 Aurora kinase B (AURKB) is a mitotic serine/threonine protein kinase that belongs to the aurora kinase family along with aurora kinase A (AURKA) and aurora kinase C (AURKC).
Naheed Arfin Borah, Mamatha M. Reddy
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Agrin-induced acetylcholine receptor clustering in mammalian muscle requires tyrosine phosphorylation. [PDF]
, 1996 Agrin is thought to be the nerve-derived factor that initiates acetylcholine receptor (AChR) clustering at the developing neuromuscularjunction. We have investigated the signaling pathway in mouse C2 myotubes and report that agrin induces a rapid but ...
Deiner, M, Ferns, M, Hall, Z
core
Phosphoproteomics data classify hematological cancer cell lines according to tumor type and sensitivity to kinase inhibitors [PDF]
, 2013 This is an open access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work ...
Alcolea, MP +7 more
core +2 more sources
Statistical and Clustering Analysis of Safety Profiles of FDA-Approved Protein Kinase Inhibitors
Applied SciencesProtein kinases are vital regulators in cell biology, modifying protein functions through phosphorylation. Protein kinase inhibitors (PKIs), which impede these kinases’ activities, have broadened their therapeutic scope from cancer treatment to ...
Ioana Lavinia Radulian +3 more
doaj +1 more source