Assessment of Structural Intolerance and Durability
General Structure Information 3rhk MET crystal structure of the catalytic domain of c-met kinase in complex with arq 197 1.94Å AUTH S.EATHIRAJ,R.PALMA,E.VOLCKOVA,M.HIRSCHI,D.S.FRANCE,AUTH 2 M.A.ASHWELL,T.C.CHANTITL DISCOVERY OF A NOVEL MODE OF PROTEIN KINASE INHIBITIONTITL 2 CHARACTERIZED BY THE MECHANISM OF INHIBITION OF HUMANTITL 3 MESENCHYMAL-EPITHELIAL TRANSITION FACTOR (C-MET) PROTEINTITL 4 AUTOPHOSPHORYLATION BY ARQ 197.REF J.BIOL.CHEM. V. […]
General Structure Information 2x2u RET first two cadherin-like domains from human ret 2.0Å AUTH S.KJAER,S.HANRAHAN,N.TOTTY,N.Q.MCDONALDTITL MAMMAL-RESTRICTED ELEMENTS PREDISPOSE HUMAN RET TOTITL 2 FOLDING IMPAIRMENT BY HSCR MUTATIONS.REF NAT.STRUCT.MOL.BIOL. V. 17 726 2010REFN ISSN 1545-9993PMID 20473317DOI 10.1038/NSMB.1808 Variant Set Distributions Ripley’s K Analysis Plots Variant Set Comparisons Mapped Variants
General Structure Information 3g0f KIT kit kinase domain mutant d816h in complex with sunitinib 2.6Å AUTH K.S.GAJIWALA,J.C.WU,J.CHRISTENSEN,G.D.DESHMUKH,AUTH 2 W.DIEHL,J.P.DINITTO,J.M.ENGLISH,M.J.GREIG,Y.A.HE,AUTH 3 S.L.JACQUES,E.A.LUNNEY,M.MCTIGUE,D.MOLINA,AUTH 4 T.QUENZER,P.A.WELLS,X.YU,Y.ZHANG,A.ZOU,M.R.EMMETT,AUTH 5 A.G.MARSHALL,H.M.ZHANG,G.D.DEMETRITITL KIT KINASE MUTANTS SHOW UNIQUE MECHANISMS OF DRUGTITL 2 RESISTANCE TO IMATINIB AND SUNITINIB INTITL 3 GASTROINTESTINAL STROMAL TUMOR PATIENTS.REF PROC.NATL.ACAD.SCI.USA V. 106 1542 2009REFN ISSN 0027-8424PMID 19164557DOI 10.1073/PNAS.0812413106 Variant […]
General Structure Information 3a4o LYN lyn kinase domain 3.0Å AUTH N.MIYANO,T.KINOSHITA,R.NAKAI,Y.KIRII,K.YOKOTA,AUTH 2 T.TADATITL STRUCTURAL BASIS FOR THE INHIBITOR RECOGNITION OFTITL 2 HUMAN LYN KINASE DOMAINREF BIOORG.MED.CHEM.LETT. V. 19 6557 2009REFN ISSN 0960-894XPMID 19857964DOI 10.1016/J.BMCL.2009.10.038 Variant Set Distributions Ripley’s K Analysis Plots Variant Set Comparisons Pathogenic Proximity Analysis Mapped Variants
General Structure Information 2x2m RET crystal structure of phosphorylated ret tyrosine kinase domain with inhibitor 2.5Å AUTH L.MOLOGNI,R.ROSTAGNO,S.BRUSSOLO,P.P.KNOWLES,AUTH 2 S.KJAER,J.MURRAY-RUST,E.ROSSO,A.ZAMBON,L.SCAPOZZA,AUTH 3 N.Q.MCDONALD,V.LUCCHINI,C.GAMBACORTI-PASSERINITITL SYNTHESIS, STRUCTURE-ACTIVITY RELATIONSHIP ANDTITL 2 CRYSTALLOGRAPHIC STUDIES OF 3-SUBSTITUTED INDOLIN-TITL 3 2-ONE RET INHIBITORS.REF BIOORG.MED.CHEM. V. 18 1482 2010REFN ISSN 0968-0896PMID 20117004DOI 10.1016/J.BMC.2010.01.011 Variant Set Distributions Ripley’s K Analysis Plots Variant Set Comparisons […]
General Structure Information 2c0o HCK src family kinase hck with bound inhibitor a-770041 2.85Å AUTH A.BURCHAT,D.W.BORHANI,D.J.CALDERWOOD,G.C.HIRST,B.LI,AUTH 2 R.F.STACHLEWITZTITL DISCOVERY OF A-770041, A SRC-FAMILY SELECTIVE ORALLY ACTIVETITL 2 LCK INHIBITOR THAT PREVENTS ORGAN ALLOGRAFT REJECTION.REF BIOORG.MED.CHEM.LETT. V. 16 118 2006REFN ISSN 0960-894XPMID 16216497DOI 10.1016/J.BMCL.2005.09.039 Variant Set Distributions Ripley’s K Analysis Plots Variant Set Comparisons Pathogenic Proximity […]
General Structure Information 3gt8 EGFR crystal structure of the inactive egfr kinase domain in complex with amp-pnp 2.96Å AUTH N.JURA,N.F.ENDRES,K.ENGEL,S.DEINDL,R.DAS,AUTH 2 M.H.LAMERS,D.E.WEMMER,X.ZHANG,J.KURIYANTITL MECHANISM FOR ACTIVATION OF THE EGF RECEPTORTITL 2 CATALYTIC DOMAIN BY THE JUXTAMEMBRANE SEGMENT.REF CELL(CAMBRIDGE,MASS.) V. 137 1293 2009REFN ISSN 0092-8674PMID 19563760DOI 10.1016/J.CELL.2009.04.025 Variant Set Distributions Ripley’s K Analysis Plots Variant Set Comparisons […]
General Structure Information 2uzp PRKCG crystal structure of the c2 domain of human protein kinase c gamma. 2.0Å AUTH A.C.W.PIKE,A.AMOS,C.JOHANSSON,F.SOBOTT,P.SAVITSKY,AUTH 2 G.BERRIDGE,O.FEDOROV,C.UMEANO,F.GORREC,G.BUNKOCZI,AUTH 3 J.DEBRECZENI,F.VON DELFT,C.H.ARROWSMITH,A.EDWARDS,J.WEIGELT,AUTH 4 M.SUNDSTROM,S.KNAPPTITL CRYSTAL STRUCTURE OF C2 DOMAIN OF PROTEIN KINASE C GAMMAREF TO BE PUBLISHEDREFN Variant Set Distributions Ripley’s K Analysis Plots Variant Set Comparisons Pathogenic Proximity Analysis Mapped Variants
General Structure Information 2v3s OXSR1 structural insights into the recognition of substrates and activators by the osr1 kinase 1.7Å AUTH F.VILLA,J.GOEBEL,F.H.RAFIQI,M.DEAK,J.THASTRUP,AUTH 2 D.R.ALESSI,D.M.F.VAN AALTENTITL STRUCTURAL INSIGHTS INTO THE RECOGNITION OFTITL 2 SUBSTRATES AND ACTIVATORS BY THE OSR1 KINASEREF EMBO REP. V. 8 839 2007REFN ISSN 1469-3178PMID 17721439DOI 10.1038/SJ.EMBOR.7401048 Variant Set Distributions Mapped Variants
General Structure Information 3i6w CHEK2 structure and activation mechanism of the chk2 dna-damage checkpoint kinase 3.25Å AUTH Z.CAI,N.H.CHEHAB,N.P.PAVLETICHTITL STRUCTURE AND ACTIVATION MECHANISM OF THE CHK2 DNA DAMAGETITL 2 CHECKPOINT KINASE.REF MOL.CELL V. 35 818 2009REFN ISSN 1097-2765PMID 19782031DOI 10.1016/J.MOLCEL.2009.09.007 Variant Set Distributions Ripley’s K Analysis Plots Variant Set Comparisons Pathogenic Proximity Analysis Mapped Variants