M00328
type: Enzyme
rlcp: p1162
cath: http://ezcatdb.cbrc.jp/EzCatDB/cath/-.-.-.-
cath: Jelly Rolls
cath: Phosphorylase Kinase; domain 1
cath: Transferase(Phosphotransferase); domain 1
ec: https://purl.uniprot.org/enzyme/2.7.10.1
uniprot: Q9UM73
kegg enzyme: Receptor protein-tyrosine kinase
kegg enzyme: ALK
kegg enzyme: Anaplastic lymphoma kinase
kegg enzyme: ATP:protein-tyrosine O-phosphotransferase (ambiguous)
kegg enzyme: Protein-tyrosine kinase (ambiguous)
kegg enzyme: Protein tyrosine kinase (ambiguous)
kegg enzyme: Receptor protein tyrosine kinase
kegg cofactor: Mg
kegg substrate: ATP
kegg substrate: [protein]-L-tyrosine
kegg product: ADP
kegg product: [protein]-L-tyrosine phosphate
pdb: 2xb7A01
pdb: 2xbaA01
pdb: 2xp2A01
pdb: 2yfxA01
pdb: 2yhvA01
pdb: 2yjrA01
pdb: 2yjsA01
pdb: 3aoxA01
pdb: 3l9pA01
pdb: 3lcsA01
pdb: 3lctA01
pdb: 4dceA01
pdb: 4dceB01
pdb: 4fnwA01
pdb: 4fnxA01
pdb: 4fnyA01
pdb: 4fnzA01
pdb: 4fobA01
pdb: 4focA01
pdb: 4fodA01
pdb: 2xb7A02
pdb: 2xbaA02
pdb: 2xp2A02
pdb: 2yfxA02
pdb: 2yhvA02
pdb: 2yjrA02
pdb: 2yjsA02
pdb: 3aoxA02
pdb: 3l9pA02
pdb: 3lcsA02
pdb: 3lctA02
pdb: 4dceA02
pdb: 4dceB02
pdb: 4fnwA02
pdb: 4fnxA02
pdb: 4fnyA02
pdb: 4fnzA02
pdb: 4fobA02
pdb: 4focA02
pdb: 4fodA02
pdb: 2kupB
pdb: 2ys5B
pdb bound state: Unbound
  compound: ATP
  pdb: 2xb7A01
pdb bound state: Unbound
  compound: ATP
  pdb: 2xbaA01
pdb bound state: Unbound
  compound: ATP
  pdb: 2xp2A01
active site residues resources: Crystal structures of anaplastic lymphoma kinase in complex with ATP competitive inhibitors.
active site residues resources: Q9UM73
references: Identification of anaplastic lymphoma kinase as a receptor for the growth factor pleiotrophin.
references: Midkine binds to anaplastic lymphoma kinase (ALK) and acts as a growth factor for different cell types.
references: Unique substrate specificity of anaplastic lymphoma kinase (ALK): development of phosphoacceptor peptides for the assay of ALK activity.
references: Characterization of some molecular mechanisms governing autoactivation of the catalytic domain of the anaplastic lymphoma kinase.
references: Crystal structure of the ALK (anaplastic lymphoma kinase) catalytic domain.
references: Crystal structures of anaplastic lymphoma kinase in complex with ATP competitive inhibitors.
references: http://ezcatdb.cbrc.jp/EzCatDB/reference/M00328#7
references: CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant.
references: Structure Based Drug Design of Crizotinib (PF-02341066), a Potent and Selective Dual Inhibitor of Mesenchymal-Epithelial Transition Factor (c-MET) Kinase and Anaplastic Lymphoma Kinase (ALK).
references: Rapid development of piperidine carboxamides as potent and selective anaplastic lymphoma kinase inhibitors.
references: The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.
references: The R1275Q neuroblastoma mutant and certain ATP-competitive inhibitors stabilize alternative activation loop conformations of anaplastic lymphoma kinase.
comment: This enzyme is a receptor for growth factors, pleiotrophin (UniProt; P21246) and midkine (UniProt; P21741), which are homologous to each other (see [1] and [2]). This enzyme belongs to the insulin receptor kinase superfamily (see [5]). This enzyme consists of the N-terminal extracellular region, the transmembrane region and the C-terminal cytoplasmic region (see [5]). The extracellular region is composed of an N-terminal region, whose structure has not been elucidated yet, two MAM domains, low-density lipoprotein class A (LDL-A) domain, and a glycine-rich region (see [5]). The cytoplasmic region is composed of a juxtamembrane region, a catalytic domain and a C-terminal region (see [5]). The catalytic domain is homologous to that of insulin receptor kinase (M00129 in EzCatDB).

Jelly Rolls
type: Cath
references: http://www.cathdb.info/version/latest/superfamily/2.60.120.-

Phosphorylase Kinase; domain 1
type: Cath
references: http://www.cathdb.info/version/latest/superfamily/3.30.200.20

Transferase(Phosphotransferase); domain 1
type: Cath
references: http://www.cathdb.info/version/latest/superfamily/1.10.510.10
catalytic domain: index.html

Mg
type: KeggCofactor
references: KEGG:C00305
compound type: divalent metal (Ca2+, Mg2+)
references: CHEBI:18420
references: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi

ATP
type: KeggSubstrate
references: KEGG:C00002
compound type: amine group
compound type: nucleotide
references: CHEBI:15422
references: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi

[protein]-L-tyrosine
type: KeggSubstrate
references: KEGG:C00585
compound type: aromatic ring (only carbon atom)
compound type: peptide/protein

ADP
type: KeggProduct
references: KEGG:C00008
compound type: amine group
compound type: nucleotide
references: CHEBI:16761
references: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi

[protein]-L-tyrosine phosphate
type: KeggProduct
references: KEGG:C01167
compound type: aromatic ring (only carbon atom)
compound type: peptide/protein
compound type: phosphate group/phosphate ion

2xb7A01
type: Pdb
references: 2xb7
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:2xb7
comment: invisible 1137-1143

2xbaA01
type: Pdb
references: 2xba
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:2xba
comment: invisible 1123-1129, 1137-1143

2xp2A01
type: Pdb
references: 2xp2
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:2xp2
comment: invisible 1124-1125, 1137-1143

2yfxA01
type: Pdb
references: 2yfx
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:2yfx
comment: invisible 1124-1125, 1136-1143

2yhvA01
type: Pdb
references: 2yhv
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:2yhv
comment: invisible 1123-1125, 1136-1143

2yjrA01
type: Pdb
references: 2yjr
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:2yjr
comment: invisible 1137-1143

2yjsA01
type: Pdb
references: 2yjs
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:2yjs
comment: invisible 1125-1128, 1137-1143

3aoxA01
type: Pdb
references: 3aox
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:3aox
comment: invisible 1124-1127, 1137-1143

3l9pA01
type: Pdb
references: 3l9p
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:3l9p
comment: invisible 1138-1142

4dceA01
type: Pdb
references: 4dce
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:4dce
comment: invisible 1125-1127, 1137-1141

4dceB01
type: Pdb
references: 4dce
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:4dce
comment: invisible 1125-1128, 1137-1142

4fnwA01
type: Pdb
references: 4fnw
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:4fnw
comment: invisible 1124-1127, 1137-1142

4fnxA01
type: Pdb
references: 4fnx
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:4fnx
comment: invisible 1123-1128, 1137-1141

4fnyA01
type: Pdb
references: 4fny
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:4fny
comment: invisible 1125-1127, 1138-1143

4fnzA01
type: Pdb
references: 4fnz
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:4fnz
comment: invisible 1125-1127, 1138-1142

4fobA01
type: Pdb
references: 4fob
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:4fob
comment: invisible 1137-1142

4focA01
type: Pdb
references: 4foc
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:4foc
comment: invisible 1137-1142

4fodA01
type: Pdb
references: 4fod
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:4fod
comment: invisible 1137-1142

2xb7A02
type: Pdb
references: 2xb7
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:2xb7
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
comment: invisible 1275-1288

2xbaA02
type: Pdb
references: 2xba
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:2xba
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
modified residue: TYR 1278(auto-phosphorylation)
comment: invisible 1279-1288

2xp2A02
type: Pdb
references: 2xp2
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:2xp2
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
modified residue: TYR 1278(auto-phosphorylation)
comment: invisible 1281-1289

2yfxA02
type: Pdb
references: 2yfx
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:2yfx
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
modified residue: TYR 1278(auto-phosphorylation)
comment: invisible 1280-1285

2yhvA02
type: Pdb
references: 2yhv
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:2yhv
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
modified residue: TYR 1278(auto-phosphorylation)
comment: invisible 1280-1285

2yjrA02
type: Pdb
references: 2yjr
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:2yjr
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
comment: invisible 1274-1287

2yjsA02
type: Pdb
references: 2yjs
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:2yjs
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
modified residue: TYR 1278(auto-phosphorylation)
comment: invisible 1280-1287

3aoxA02
type: Pdb
references: 3aox
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:3aox
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
modified residue: TYR 1278(auto-phosphorylation)
comment: invisible 1281-1287

3l9pA02
type: Pdb
references: 3l9p
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:3l9p
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
modified residue: TYR 1278(auto-phosphorylation)

3lcsA02
type: Pdb
references: 3lcs
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:3lcs
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
modified residue: TYR 1278(auto-phosphorylation)

3lctA02
type: Pdb
references: 3lct
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:3lct
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
modified residue: TYR 1278(auto-phosphorylation)

4dceA02
type: Pdb
references: 4dce
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:4dce
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
comment: invisible 1273-1286

4dceB02
type: Pdb
references: 4dce
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:4dce
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
comment: invisible 1273-1287

4fnwA02
type: Pdb
references: 4fnw
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:4fnw
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
modified residue: TYR 1278(auto-phosphorylation)
comment: invisible 1280-1287

4fnxA02
type: Pdb
references: 4fnx
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:4fnx
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
modified residue: TYR 1278(auto-phosphorylation)
comment: invisible 1279-1287

4fnyA02
type: Pdb
references: 4fny
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:4fny
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
comment: invisible 1216-1219, 1272-1287

4fnzA02
type: Pdb
references: 4fnz
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:4fnz
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
comment: invisible 1273-1287

4fobA02
type: Pdb
references: 4fob
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:4fob
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
modified residue: TYR 1278(auto-phosphorylation)
comment: invisible 1216-1218, 1281-1286

4focA02
type: Pdb
references: 4foc
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:4foc
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
modified residue: TYR 1278(auto-phosphorylation)
comment: invisible 1280-1287

4fodA02
type: Pdb
references: 4fod
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: PDB:4fod
catalytic residue: ASP 1249;ARG 1253
cofactor binding residue: ASN 1254;ASP 1270(Magnesium binding)
modified residue: TYR 1278(auto-phosphorylation)
comment: invisible 1281-1287

Identification of anaplastic lymphoma kinase as a receptor for the growth factor pleiotrophin.
type: BibliographicResource
comment: INTERACTION WITH PTN, FUNCTION.
references: http://www.ncbi.nlm.nih.gov/pubmed/11278720
journal: J Biol Chem
volume: 276
pages: 16772-9
published year: 2001
authors:
  item: Stoica GE
  item: Kuo A
  item: Aigner A
  item: Sunitha I
  item: Souttou B
  item: Malerczyk C
  item: Caughey DJ
  item: Wen D
  item: Karavanov A
  item: Riegel AT
  item: Wellstein A

Midkine binds to anaplastic lymphoma kinase (ALK) and acts as a growth factor for different cell types.
type: BibliographicResource
comment: INTERACTION WITH MDK, FUNCTION.
references: http://www.ncbi.nlm.nih.gov/pubmed/12122009
journal: J Biol Chem
volume: 277
pages: 35990-8
published year: 2002
authors:
  item: Stoica GE
  item: Kuo A
  item: Powers C
  item: Bowden ET
  item: Sale EB
  item: Riegel AT
  item: Wellstein A

Unique substrate specificity of anaplastic lymphoma kinase (ALK): development of phosphoacceptor peptides for the assay of ALK activity.
type: BibliographicResource
comment: SUBSTRATE SPECIFICITY.
references: http://www.ncbi.nlm.nih.gov/pubmed/15938644
journal: Biochemistry
volume: 44
pages: 8533-42
published year: 2005
authors:
  item: Tartari CJ
  item: Mologni L
  item: Scapozza L
  item: Gambacorti-Passerini C
  item: Pinna LA

Characterization of some molecular mechanisms governing autoactivation of the catalytic domain of the anaplastic lymphoma kinase.
type: BibliographicResource
references: http://www.ncbi.nlm.nih.gov/pubmed/18070884
journal: J Biol Chem
volume: 283
pages: 3743-50
published year: 2008
authors:
  item: Tartari CJ
  item: Gunby RH
  item: Coluccia AM
  item: Sottocornola R
  item: Cimbro B
  item: Scapozza L
  item: Donella-Deana A
  item: Pinna LA
  item: Gambacorti-Passerini C

Crystal structure of the ALK (anaplastic lymphoma kinase) catalytic domain.
type: BibliographicResource
comment: X-RAY CRYSTALLOGRAPHY (1.80 ANGSTROMS) OF 1072-1410.
references: http://www.ncbi.nlm.nih.gov/pubmed/20632993
journal: Biochem J
volume: 430
pages: 425-37
published year: 2010
authors:
  item: Lee CC
  item: Jia Y
  item: Li N
  item: Sun X
  item: Ng K
  item: Ambing E
  item: Gao MY
  item: Hua S
  item: Chen C
  item: Kim S
  item: Michellys PY
  item: Lesley SA
  item: Harris JL
  item: Spraggon G
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: Q9UM73

Crystal structures of anaplastic lymphoma kinase in complex with ATP competitive inhibitors.
type: BibliographicResource
comment: X-RAY CRYSTALLOGRAPHY (1.95 ANGSTROMS) OF 1094-1407 IN COMPLEX WITH INHIBITOR.
references: http://www.ncbi.nlm.nih.gov/pubmed/20695522
journal: Biochemistry
volume: 49
pages: 6813-25
published year: 2010
authors:
  item: Bossi RT
  item: Saccardo MB
  item: Ardini E
  item: Menichincheri M
  item: Rusconi L
  item: Magnaghi P
  item: Orsini P
  item: Avanzi N
  item: Borgia AL
  item: Nesi M
  item: Bandiera T
  item: Fogliatto G
  item: Bertrand JA
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: Q9UM73

http://ezcatdb.cbrc.jp/EzCatDB/reference/M00328#7
type: BibliographicResource
references: http://www.ncbi.nlm.nih.gov/pubmed/20454865
journal: J Struct Funct Genomics
volume: 11
pages: 125-41
published year: 2010
authors:
  item: Koshiba S
  item: Li H
  item: Motoda Y
  item: Tomizawa T
  item: Kasai T
  item: Tochio N
  item: Yabuki T
  item: Harada T
  item: Watanabe S
  item: Tanaka A
  item: Shirouzu M
  item: Kigawa T
  item: Yamamoto T
  item: Yokoyama S
title: Structural basis for the recognition of nucleophosmin-anaplastic lymphoma kinase oncoprotein by the phosphotyrosine binding domain of Suc1-associated neurotrophic factor-induced tyrosine-phosphorylated target-2.
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl

CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant.
type: BibliographicResource
comment: X-RAY CRYSTALLOGRAPHY (1.75 ANGSTROMS) OF 1069-1411 IN COMPLEX WITH INHIBITOR, ENZYME REGULATION.
references: http://www.ncbi.nlm.nih.gov/pubmed/21575866
journal: Cancer Cell
volume: 19
pages: 679-90
published year: 2011
authors:
  item: Sakamoto H
  item: Tsukaguchi T
  item: Hiroshima S
  item: Kodama T
  item: Kobayashi T
  item: Fukami TA
  item: Oikawa N
  item: Tsukuda T
  item: Ishii N
  item: Aoki Y
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: Q9UM73

Structure Based Drug Design of Crizotinib (PF-02341066), a Potent and Selective Dual Inhibitor of Mesenchymal-Epithelial Transition Factor (c-MET) Kinase and Anaplastic Lymphoma Kinase (ALK).
type: BibliographicResource
references: http://www.ncbi.nlm.nih.gov/pubmed/21812414
journal: J Med Chem
volume: 54
pages: 6342-6363
published year: 2011
authors:
  item: Cui JJ
  item: Tran-Dube? M
  item: Shen H
  item: Nambu M
  item: Kung PP
  item: Pairish M
  item: Jia L
  item: Meng J
  item: Funk L
  item: Botrous I
  item: McTigue M
  item: Grodsky N
  item: Ryan K
  item: Padrique E
  item: Alton G
  item: Timofeevski S
  item: Yamazaki S
  item: Li Q
  item: Zou H
  item: Christensen J
  item: Mroczkowski B
  item: Bender S
  item: Kania RS
  item: Edwards MP
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl
references: Q9UM73

Rapid development of piperidine carboxamides as potent and selective anaplastic lymphoma kinase inhibitors.
type: BibliographicResource
references: http://www.ncbi.nlm.nih.gov/pubmed/22263917
journal: J Med Chem
volume: 55
pages: 1698-705
published year: 2012
authors:
  item: Bryan MC
  item: Whittington DA
  item: Doherty EM
  item: Falsey JR
  item: Cheng AC
  item: Emkey R
  item: Brake RL
  item: Lewis RT
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl

The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.
type: BibliographicResource
references: http://www.ncbi.nlm.nih.gov/pubmed/22734674
journal: J Med Chem
volume: 55
pages: 6523-40
published year: 2012
authors:
  item: Lewis RT
  item: Bode CM
  item: Choquette DM
  item: Potashman M
  item: Romero K
  item: Stellwagen JC
  item: Teffera Y
  item: Moore E
  item: Whittington DA
  item: Chen H
  item: Epstein LF
  item: Emkey R
  item: Andrews PS
  item: Yu VL
  item: Saffran DC
  item: Xu M
  item: Drew A
  item: Merkel P
  item: Szilvassy S
  item: Brake RL
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl

The R1275Q neuroblastoma mutant and certain ATP-competitive inhibitors stabilize alternative activation loop conformations of anaplastic lymphoma kinase.
type: BibliographicResource
references: http://www.ncbi.nlm.nih.gov/pubmed/22932897
journal: J Biol Chem
volume: 287
pages: 37447-57
published year: 2012
authors:
  item: Epstein LF
  item: Chen H
  item: Emkey R
  item: Whittington DA
references: http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl