Feng et al., 2013 - Google Patents
A small molecule bidentate-binding dual inhibitor probe of the LRRK2 and JNK kinasesFeng et al., 2013
View PDF- Document ID
- 1523683600176051413
- Author
- Feng Y
- Chambers J
- Iqbal S
- Koenig M
- Park H
- Cherry L
- Hernandez P
- Figuera-Losada M
- LoGrasso P
- Publication year
- Publication venue
- ACS chemical biology
External Links
Snippet
Both JNK and LRRK2 are associated with Parkinson's disease (PD). Here we report a reasonably selective and potent kinase inhibitor (compound 6) that bound to both JNK and LRRK2 (a dual inhibitor). A bidentate-binding strategy that simultaneously utilized the ATP …
- 230000002401 inhibitory effect 0 title abstract description 321
Classifications
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by the preceding groups
- G01N33/48—Investigating or analysing materials by specific methods not covered by the preceding groups biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
- G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
- G01N33/502—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing non-proliferative effects
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by the preceding groups
- G01N33/48—Investigating or analysing materials by specific methods not covered by the preceding groups biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
- G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
- G01N33/5044—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics involving specific cell types
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2500/00—Screening for compounds of potential therapeutic value
- G01N2500/04—Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)
Similar Documents
Publication | Publication Date | Title |
---|---|---|
Yamazoe et al. | Heterobifunctional molecules induce dephosphorylation of kinases–a proof of concept study | |
Urick et al. | Dual screening of BPTF and Brd4 using protein-observed fluorine NMR uncovers new bromodomain probe molecules | |
Koch et al. | Inhibitors of c-Jun N-terminal kinases: an update | |
Millies et al. | Proline-based allosteric inhibitors of Zika and Dengue virus NS2B/NS3 proteases | |
Yin et al. | Terphenyl-based Bak BH3 α-helical proteomimetics as low-molecular-weight antagonists of Bcl-xL | |
Lu et al. | SHAFTS: a hybrid approach for 3D molecular similarity calculation. 2. Prospective case study in the discovery of diverse p90 ribosomal S6 protein kinase 2 inhibitors to suppress cell migration | |
Hartshorn et al. | Fragment-based lead discovery using X-ray crystallography | |
Stebbins et al. | Identification of a new JNK inhibitor targeting the JNK-JIP interaction site | |
Louis et al. | Inhibition of autoprocessing of natural variants and multidrug resistant mutant precursors of HIV-1 protease by clinical inhibitors | |
De et al. | Design, synthesis, and structure− activity relationship of substrate competitive, selective, and in vivo active triazole and thiadiazole inhibitors of the c-Jun N-terminal kinase | |
Yu et al. | Rational design of small-molecule inhibitors for β-catenin/T-cell factor protein–protein interactions by bioisostere replacement | |
Novaroli et al. | Impact of species-dependent differences on screening, design, and development of MAO B inhibitors | |
Wells et al. | SGC-AAK1-1: a chemical probe targeting AAK1 and BMP2K | |
Statsuk et al. | Tuning a three-component reaction for trapping kinase substrate complexes | |
Tomašić et al. | Dual inhibitor of MurD and MurE ligases from Escherichia coli and Staphylococcus aureus | |
Baumli et al. | The CDK9 C-helix exhibits conformational plasticity that may explain the selectivity of CAN508 | |
Stebbins et al. | Design and characterization of a potent and selective dual ATP-and substrate-competitive subnanomolar bidentate c-Jun N-terminal kinase (JNK) inhibitor | |
Allimuthu et al. | 2-Chloropropionamide as a low-reactivity electrophile for irreversible small-molecule probe identification | |
Feng et al. | A small molecule bidentate-binding dual inhibitor probe of the LRRK2 and JNK kinases | |
Tiefenbrunn et al. | Small molecule regulation of protein conformation by binding in the flap of HIV protease | |
Good et al. | Implications of promiscuous Pim-1 kinase fragment inhibitor hydrophobic interactions for fragment-based drug design | |
Stains et al. | A p38α-selective chemosensor for use in unfractionated cell lysates | |
Brandvold et al. | Exquisitely specific bisubstrate inhibitors of c-Src kinase | |
Liu et al. | Development of alkyne-containing pyrazolopyrimidines to overcome drug resistance of Bcr-Abl kinase | |
Xiao et al. | Dynamics of protein kinases: insights from nuclear magnetic resonance |