abbott compound (a-769662) Search Results


compound a769662  (Abbott Laboratories)
90
Abbott Laboratories compound a769662
Activation of purified, recombinant AMPK. A, activity dose-response curves determined by radioactive kinase assays using the ACC-based SAMS peptide as substrate. n = 3; error bars, S.D. B, effects of 20 μm R734, R739, or <t>A769662</t> or 200 μm AMP on protection against activation loop dephosphorylation. The indicated AMPK proteins were incubated with protein phosphatase 2Cα (PP2C; left blot) or with λ-phosphatase (λ-pp; right blot) for the indicated length of time. Protein phosphatase 2Cα was chosen for AMPK α1β2γ1 as the activation loop phosphate of this isoform was inefficiently removed by λ-phosphatase. Phospho-AMPK was visualized by immunoblotting. ΔST, deletion of the ST loop in the α-subunit (amino acids 476–529).
Compound A769662, supplied by Abbott Laboratories, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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Activation of purified, recombinant AMPK. A, activity dose-response curves determined by radioactive kinase assays using the ACC-based SAMS peptide as substrate. n = 3; error bars, S.D. B, effects of 20 μm R734, R739, or A769662 or 200 μm AMP on protection against activation loop dephosphorylation. The indicated AMPK proteins were incubated with protein phosphatase 2Cα (PP2C; left blot) or with λ-phosphatase (λ-pp; right blot) for the indicated length of time. Protein phosphatase 2Cα was chosen for AMPK α1β2γ1 as the activation loop phosphate of this isoform was inefficiently removed by λ-phosphatase. Phospho-AMPK was visualized by immunoblotting. ΔST, deletion of the ST loop in the α-subunit (amino acids 476–529).

Journal: The Journal of Biological Chemistry

Article Title: Structures of AMP-activated protein kinase bound to novel pharmacological activators in phosphorylated, non-phosphorylated, and nucleotide-free states

doi: 10.1074/jbc.RA118.004883

Figure Lengend Snippet: Activation of purified, recombinant AMPK. A, activity dose-response curves determined by radioactive kinase assays using the ACC-based SAMS peptide as substrate. n = 3; error bars, S.D. B, effects of 20 μm R734, R739, or A769662 or 200 μm AMP on protection against activation loop dephosphorylation. The indicated AMPK proteins were incubated with protein phosphatase 2Cα (PP2C; left blot) or with λ-phosphatase (λ-pp; right blot) for the indicated length of time. Protein phosphatase 2Cα was chosen for AMPK α1β2γ1 as the activation loop phosphate of this isoform was inefficiently removed by λ-phosphatase. Phospho-AMPK was visualized by immunoblotting. ΔST, deletion of the ST loop in the α-subunit (amino acids 476–529).

Article Snippet: In 2006, Abbot Laboratories developed compound A769662 ( 36 ), the first example of a group of small molecules that activate AMPK with high specificity by binding the ADaM site at the KD/CBM interface ( 22 ).

Techniques: Activation Assay, Purification, Recombinant, Activity Assay, De-Phosphorylation Assay, Incubation, Western Blot

R734, R739, 991, and A769662 increase phosphorylation of AMPK, Raptor, and ACC in cells. A–D, dose-dependent phosphorylation increases in the presence of R734 (A), R739 (B), 991 (C), and A769662 (D). HepG2 cells were treated with increasing doses of R734, R739, 991, and A769662 for 1 h. Phosphorylated and total proteins were visualized by immunoblotting with the indicated antibodies. Target bands are indicated by arrows. Higher order phosphorylation of AMPKα due to autophosphorylation is marked by asterisks. Bands above the phosphorylated Raptor bands are cross-reacting bands. β-Actin is shown as loading control.

Journal: The Journal of Biological Chemistry

Article Title: Structures of AMP-activated protein kinase bound to novel pharmacological activators in phosphorylated, non-phosphorylated, and nucleotide-free states

doi: 10.1074/jbc.RA118.004883

Figure Lengend Snippet: R734, R739, 991, and A769662 increase phosphorylation of AMPK, Raptor, and ACC in cells. A–D, dose-dependent phosphorylation increases in the presence of R734 (A), R739 (B), 991 (C), and A769662 (D). HepG2 cells were treated with increasing doses of R734, R739, 991, and A769662 for 1 h. Phosphorylated and total proteins were visualized by immunoblotting with the indicated antibodies. Target bands are indicated by arrows. Higher order phosphorylation of AMPKα due to autophosphorylation is marked by asterisks. Bands above the phosphorylated Raptor bands are cross-reacting bands. β-Actin is shown as loading control.

Article Snippet: In 2006, Abbot Laboratories developed compound A769662 ( 36 ), the first example of a group of small molecules that activate AMPK with high specificity by binding the ADaM site at the KD/CBM interface ( 22 ).

Techniques: Western Blot