p38α mapk  (Carna Inc)

Journal: Biochemical and biophysical research communications

Article Title: Identification of a novel target site for ATP-independent ERK2 inhibitors.

doi: 10.1016/j.bbrc.2022.01.035

Figure Lengend Snippet: Fig. 2. Enlarged views of the ERK2-compound 1 complex. (a) Ribbon and stick representation of the main chain and selected side chains, respectively. Residue names of p38a and JNK1 are shown in parentheses, respectively. (b) Molecular surface representation of the binding site from different views. Compound 1 is shown in green. The dotted-line circle in the figure on the right shows the remaining residual space. (For interpretation of the references to colour in this figure legend, the reader is referred to the Web version of this article.)

Article Snippet: The inhibitory activities of a test compound for ERK2, p38a and JNK1 were determined using human recombinant GST-fused ERK2, p38a, or JNK1 (Carna Biosciences, Inc.), and 1 mM FITC-labeled substrate peptide in the presence of the test compound in assay buffer containing 20 mMHEPES (pH 7.5), 0.01% Triton X-100, 5 mM DTT, 5 mM MgCl2 and ATP (50 mM, 150 mM, or 100 mM for ERK2, p38a or JNK1, respectively) at room temperature for 1 h. The reaction was terminated by adding of termination buffer (QuickScout Screening Assist MSA; Carna Biosciences, Inc.).

Techniques: Residue, Binding Assay

Journal: Biochemical and biophysical research communications

Article Title: Identification of a novel target site for ATP-independent ERK2 inhibitors.

doi: 10.1016/j.bbrc.2022.01.035

Figure Lengend Snippet: Fig. 3. Root mean square fluctuation (RMSF) diagrams from molecular dynamics simulations of MAPKs. (a) ERK2. (b) p38a. (c) JNK1. The circles, triangles, and squares denote aC-helix, TXY-motif in the A-loop, and L16 loop, respectively. Yellow and red shaded areas signify the b-sheet and a-helix. The gray bars represent the standard errors of the RMSFs. (For interpretation of the references to colour in this figure legend, the reader is referred to the Web version of this article.)

Article Snippet: The inhibitory activities of a test compound for ERK2, p38a and JNK1 were determined using human recombinant GST-fused ERK2, p38a, or JNK1 (Carna Biosciences, Inc.), and 1 mM FITC-labeled substrate peptide in the presence of the test compound in assay buffer containing 20 mMHEPES (pH 7.5), 0.01% Triton X-100, 5 mM DTT, 5 mM MgCl2 and ATP (50 mM, 150 mM, or 100 mM for ERK2, p38a or JNK1, respectively) at room temperature for 1 h. The reaction was terminated by adding of termination buffer (QuickScout Screening Assist MSA; Carna Biosciences, Inc.).

Techniques:

Journal: Cell Reports Methods

Article Title: Motif-centric phosphoproteomics to target kinase-mediated signaling pathways

doi: 10.1016/j.crmeth.2021.100138

Figure Lengend Snippet:

Article Snippet: p38α(MAPK14) , Carna Biosciences , Catalog:04-152.

Techniques: Recombinant, Bicinchoninic Acid Protein Assay, Sequencing, Modification, Software