Structure of PDB 1o5m Chain A

Receptor sequence
>1o5mA (length=315) Species: 10116 (Rattus norvegicus) [Search protein sequence]
GFLSLDSPTYVLYRDRAEWADIDPVPQNDGPSPVVQIIYSEKFRDVYDYF
RAVLQRDERSERAFKLTRDAIELNAANYTVWHFRRVLLRSLQKDLQEEMN
YITAIIEEQPKNYQVWHHRRVLVEWLKDPSQELEFIADILNQDAKNYHAW
QHRQWVIQEFRLWDNELQYVDQLLKEDVRNNSVWNQRHFVISNTTGYSDR
AVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSRYPNLLNQLLDLQ
PSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRK
EYWRYIGRSLQSKHS
3D structure
PDB1o5m Tricyclic Farnesyl Protein Transferase Inhibitors: Crystallographic and Calorimetric Studies of Structure-Activity Relationships
ChainA
Resolution2.3 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) K164
Catalytic site (residue number reindexed from 1) K111
Enzyme Commision number 2.5.1.58: protein farnesyltransferase.
2.5.1.59: protein geranylgeranyltransferase type I.
Interaction with ligand
Site
#		 Ligand Ligand
chain		 Binding residues on receptor
(original residue number in PDB)		 Binding residues on receptor
(residue number reindexed from 1)		 Binding affinity
BS01 336 A K164 N165 Y166 H201 K111 N112 Y113 H148 PDBbind-CN: -logKd/Ki=8.72,IC50=1.9nM
BindingDB: IC50=1.9nM
Gene Ontology
Molecular Function
GO:0004659 prenyltransferase activity
GO:0004660 protein farnesyltransferase activity
GO:0004661 protein geranylgeranyltransferase activity
GO:0004662 CAAX-protein geranylgeranyltransferase activity
GO:0004663 Rab geranylgeranyltransferase activity
GO:0005515 protein binding
GO:0008017 microtubule binding
GO:0008270 zinc ion binding
GO:0008318 protein prenyltransferase activity
GO:0030971 receptor tyrosine kinase binding
GO:0036094 small molecule binding
GO:0042277 peptide binding
GO:0043014 alpha-tubulin binding
GO:0060090 molecular adaptor activity
GO:1901363 heterocyclic compound binding
Biological Process
GO:0007167 enzyme-linked receptor protein signaling pathway
GO:0008284 positive regulation of cell population proliferation
GO:0014070 response to organic cyclic compound
GO:0018342 protein prenylation
GO:0018343 protein farnesylation
GO:0018344 protein geranylgeranylation
GO:0034097 response to cytokine
GO:0035022 positive regulation of Rac protein signal transduction
GO:0043066 negative regulation of apoptotic process
GO:0045787 positive regulation of cell cycle
GO:0051770 positive regulation of nitric-oxide synthase biosynthetic process
GO:0051771 negative regulation of nitric-oxide synthase biosynthetic process
GO:0090044 positive regulation of tubulin deacetylation
GO:1904395 positive regulation of skeletal muscle acetylcholine-gated channel clustering
Cellular Component
GO:0005737 cytoplasm
GO:0005875 microtubule associated complex
GO:0005953 CAAX-protein geranylgeranyltransferase complex
GO:0005965 protein farnesyltransferase complex

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Molecular Function
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Biological Process
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Cellular Component
External links
PDB RCSB:1o5m, PDBe:1o5m, PDBj:1o5m
PDBsum1o5m
PubMed10377218
UniProtQ04631|FNTA_RAT Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha (Gene Name=Fnta)

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