The structures of salt-inducible kinase 3 in complex with inhibitors reveal determinants for binding and selectivity

Keywords

salt-inducible kinase

isoform selectivity

crystallization chaperones

AMPK related kinase

drug design

crystal structure

protein purification

protein expression

protein kinase

protein crystallization

Abbreviations2TYAG

2TY+ ampicillin + glucose

ABL

Abelson murine leukemia viral oncogene

AMPK

AMP-activated protein kinase

BCR

breakpoint cluster region

BIS-TRIS propane

1,3-bis(tris(hydroxymethyl)methylamino)propane

BRSK2

BR serine/threonine kinase 2

CDR

complementarity determining region

CREB

cAMP-response element binding protein

CRTCs

CREB-regulated transcriptional coactivators

Fab

fragment antigen-binding

GST

glutathione S-transferase

HEK

human embryonic kidney

IEX

ion exchange chromatography

IMAC

immobilized metal ion affinity chromatography

IPTG

isopropyl β-d-1-thiogalactopyranoside

MARK

MAP/microtubule affinity-regulating kinase

MEF2

Myosite Enhancer Factor 2

MELK

maternal embryonic leucine zipper kinase

MMS

microseed matrix screening

MPD

2-methyl-2,4-pentanediol

MST

mammalian STE20-like protein kinase

NCS

non-crystallographic symmetry

NUAK

SNF1/AMP kinase-related kinase

PAGE

polyacrylamide gel electrophoresis

r.m.s.d.

root-mean-square deviation

ScFv

single-chain variable fragment

SER

surface-entrope reducing

SPR

surface plasmon resonance

Src

Proto-oncogene tyrosine-protein kinase

TCEP

tris(2-ccarboxyethyl)phosphine

TEV

tobacco etch virus nuclear-inclusion-a endopeptidase

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