4AXA

Structure of PKA-PKB chimera complexed with (1S)-2-amino-1-(4- chlorophenyl)-1-(4-(1H-pyrazol-4-yl)phenyl)ethan-1-ol

Summary for 4AXA

• Entry DOI: 10.2210/pdb4axa/pdb
• Related: 1CMK 1JLU 1KMU 1KMW 1Q24 1Q61 1Q62 1Q8T 1Q8U 1Q8W 1SMH 1STC 1SVE 1SVG 1SVH 1SZM 1VEB 1XH4 1XH5 1XH6 1XH7 1XH8 1XH9 1XHA 1YDR 1YDS 1YDT 2C1A 2C1B 2F7E 2GFC 2GNF 2GNG 2GNH 2GNI 2GNJ 2GNL 2JDS 2JDT 2JDV 2UVX 2UVY 2UVZ 2UW0 2UW3 2UW4 2UW5 2UW6 2UW7 2UW8 2UZT 2UZU 2UZV 2UZW 2VNW 2VNY 2VO0 2VO3 2VO6 2VO7
• Descriptor: CAMP-DEPENDENT PROTEIN KINASE CATALYTIC SUBUNIT ALPHA, CAMP-DEPENDENT PROTEIN KINASE INHIBITOR ALPHA, (2S)-2-(4-chlorophenyl)-2-hydroxy-2-[4-(1H-pyrazol-4-yl)phenyl]ethanaminium, ... (4 entities in total)
• Functional Keywords: transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: BOS TAURUS (CATTLE); More
• Cellular location: Cytoplasm: P00517
• Total number of polymer chains: 2
• Total formula weight: 43371.82

Authors

Davies, T.G.,Yap, T.A.,Walton, M.I.,Grimshaw, K.M.,tePoele, R.H.,Eve, P.D.,Valenti, M.R.,deHavenBrandon, A.K.,Martins, V.,Zetterlund, A.,Heaton, S.P.,Heinzmann, K.,Jones, P.S.,Feltell, R.E.,Reule, M.,Woodhead, S.J.,Lyons, J.F.,Raynaud, F.I.,Eccles, S.A.,Workman, P.,Thompson, N.T.,Garrett, M.D. (deposition date: 2012-06-12, release date: 2012-07-25, Last modification date: 2024-10-23)

Primary citation

Yap, T.A.,Walton, M.I.,Grimshaw, K.M.,Te Poele, R.H.,Eve, P.D.,Valenti, M.R.,De Haven Brandon, A.K.,Martins, V.,Zetterlund, A.,Heaton, S.P.,Heinzmann, K.,Jones, P.S.,Feltell, R.E.,Reule, M.,Woodhead, S.J.,Davies, T.G.,Lyons, J.F.,Raynaud, F.I.,Eccles, S.A.,Workman, P.,Thompson, N.T.,Garrett, M.D.
At13148 is a Novel, Oral Multi-Agc Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity.
Clin.Cancer Res., 18:3912-, 2012

PubMed Abstract: Deregulated phosphatidylinositol 3-kinase pathway signaling through AGC kinases including AKT, p70S6 kinase, PKA, SGK and Rho kinase is a key driver of multiple cancers. The simultaneous inhibition of multiple AGC kinases may increase antitumor activity and minimize clinical resistance compared with a single pathway component.

PubMed: 22781553
DOI: 10.1158/1078-0432.CCR-11-3313

Experimental method

X-RAY DIFFRACTION (1.9 Å)