Btk SH2-kinase interface is critical for allosteric kinase activation and its targeting inhibits B-cell neoplasms

Duarte D, Lamontanara A, La Sala G, Jeong S, Sohn Y, Panjkovich A, Georgeon S, Kükenshöner T, Marcaida M, Pojer F, De Vivo M, Svergun D, Kim H, Dal Peraro M, Hantschel O
Nature Communications 11(1) (2020 May 8)

doi: 10.1038/s41467-020-16128-5

Submitted to SASBDB: 2019 Feb 20 Published in SASBDB: 2020 Jan 8

SASDF53 – Bruton's Tyrosine Kinase - kinase domain Sample: Bruton's tyrosine kinase, kinase domain monomer, 32 kDa Homo sapiens protein Buffer: 20mM Tris, 150mM NaCl, 1mM TCEP, 5% glycerol, pH: 7.5 Experiment: SAXS data collected at BM29, ESRF on 2018 May 11 RgGuinier 2.1 nm Dmax 6.8 nm VolumePorod 52 nm3

SASDF63 – Bruton's Tyrosine Kinase - SH2-kinase domain Sample: Bruton's tyrosine kinase - Src homolgy domain 2 - kinase domain monomer, 46 kDa Homo sapiens protein Buffer: 20mM Tris, 150mM NaCl, 1mM TCEP, 5% glycerol, pH: 7.5 Experiment: SAXS data collected at BM29, ESRF on 2018 Nov 3 RgGuinier 2.8 nm Dmax 9.4 nm VolumePorod 64 nm3

SASDF73 – Bruton's Tyrosine Kinase - SH3-SH2-kinase domain Sample: Bruton's tyrosine kinase - Src homology 3-2 kinase domain monomer, 52 kDa Homo sapiens protein Buffer: 20mM Tris, 150mM NaCl, 1mM TCEP, 5% glycerol, pH: 7.5 Experiment: SAXS data collected at BM29, ESRF on 2018 Nov 2 RgGuinier 2.6 nm Dmax 8.3 nm VolumePorod 72 nm3

SASDF83 – Bruton's Tyrosine Kinase - Full-length Sample: Bruton's tyrosine kinase - full length monomer, 77 kDa Homo sapiens protein Buffer: 20mM Tris, 150mM NaCl, 1mM TCEP, 5% glycerol, pH: 7.5 Experiment: SAXS data collected at BM29, ESRF on 2018 Nov 3 RgGuinier 4.0 nm Dmax 15.6 nm VolumePorod 114 nm3