The cysteinome of protein kinases as a target in drug development
Drugs that function through covalent bond formation represent a considerable fraction of our
repository of effective medicines but safety concerns and the complexity of develo** …
repository of effective medicines but safety concerns and the complexity of develo** …
Fluorescence polarization-based bioassays: new horizons
OD Hendrickson, NA Taranova, AV Zherdev… - Sensors, 2020 - mdpi.com
Fluorescence polarization holds considerable promise for bioanalytical systems because it
allows the detection of selective interactions in real time and a choice of fluorophores, the …
allows the detection of selective interactions in real time and a choice of fluorophores, the …
The emerging landscape of small-molecule therapeutics for the treatment of Huntington's disease
S Ahamad, SA Bhat - Journal of medicinal chemistry, 2022 - ACS Publications
Huntington's disease (HD) is a progressive neurodegenerative disorder caused by a CAG
repeat expansion in the huntingtin gene (HTT). The new insights into HD's cellular and …
repeat expansion in the huntingtin gene (HTT). The new insights into HD's cellular and …
Fluorescent kinase inhibitors as probes in cancer
Fluorescent dyes attached to kinase inhibitors (KIs) can be used to probe kinases in vitro, in
cells, and in vivo. Ideal characteristics of the dyes vary with their intended applications …
cells, and in vivo. Ideal characteristics of the dyes vary with their intended applications …
[HTML][HTML] C-Jun N-terminal kinase inhibitors: Structural insight into kinase-inhibitor complexes
MTH Duong, JH Lee, HC Ahn - Computational and structural biotechnology …, 2020 - Elsevier
The activation of c-Jun N-terminal kinases (JNKs) plays an important role in physiological
processes including neuronal function, immune activity, and development, and thus, JNKs …
processes including neuronal function, immune activity, and development, and thus, JNKs …
Tri-and tetrasubstituted pyridinylimidazoles as covalent inhibitors of c-Jun N-terminal kinase 3
F Muth, A El-Gokha, F Ansideri, M Eitel… - Journal of Medicinal …, 2017 - ACS Publications
The concept of covalent inhibition of c-Jun N-terminal kinase 3 (JNK3) was successfully
transferred to our well validated pyridinylimidazole scaffold varying several structural …
transferred to our well validated pyridinylimidazole scaffold varying several structural …
Measurement of (Aptamer–Small Target) KD Using the Competition between Fluorescently Labeled and Unlabeled Targets and the Detection of Fluorescence …
Registration of fluorescence anisotropy (FA) allows for characterizing the interactions of
ligands with aptamers and other receptors under homogeneous conditions without reagent …
ligands with aptamers and other receptors under homogeneous conditions without reagent …
Methods for the comprehensive structural elucidation of constitution and stereochemistry of lipopeptides
H Gerhardt, A Sievers-Engler, G Jahanshah… - … of Chromatography A, 2016 - Elsevier
A panel of methods of general suitability for complete structural elucidation of the
stereochemistry of cyclopeptides, depsipeptides and lipopeptides is presented and …
stereochemistry of cyclopeptides, depsipeptides and lipopeptides is presented and …
Structural Optimization of a Pyridinylimidazole scaffold: shifting the selectivity from p38α mitogen-activated protein kinase to c-Jun N-terminal kinase 3
F Ansideri, JT Macedo, M Eitel, A El-Gokha… - ACS …, 2018 - ACS Publications
Starting from known p38α mitogen-activated protein kinase (MAPK) inhibitors, a series of
inhibitors of the c-Jun N-terminal kinase (JNK) 3 was obtained. Altering the substitution …
inhibitors of the c-Jun N-terminal kinase (JNK) 3 was obtained. Altering the substitution …
A selectivity study of polysubstituted pyridinylimidazoles as dual inhibitors of JNK3 and p38α MAPK based on 3D-QSAR, molecular docking, and molecular dynamics …
L Fu, Y Chen, H Guo, L Xu, M Tan, Y Dong, M Shu… - Structural Chemistry, 2021 - Springer
Within the mitogen-activated protein kinase (MAPK) 1 family, the two kinases of c-Jun N-
terminal kinase 3 (JNK3) and p38α MAPK have emerged in the last decades as particularly …
terminal kinase 3 (JNK3) and p38α MAPK have emerged in the last decades as particularly …