Structure of PDB 4lts Chain A

Receptor sequence
>4ltsA (length=472) Species: 9606 (Homo sapiens) [Search protein sequence]
EFNILLATDSYKVTHYKQYPPNTSKVYSYFECREKKVKYEETVFYGLQYI
LNKYLKGKVVTKEKIQEAKDVYKEHFQDDVFNEKGWNYILEKYDGHLPIE
IKAVPEGFVIPRGNVLFTVENTDPECYWLTNWIETILVQSWYPITVATNS
REQKKILAKYLLETSGNLDGLEYKLHDFGYRGVSSQETAGIGASAHLVNF
KGTDTVAGLALIKKYYGTKDPVPGYSVPAAEHSTITAWGKDHEKDAFEHI
VTQFSSVPVSVVSDSYDIYNACEKIWGEDLRHLIVSRSTQAPLIIRPDSG
NPLDTVLKVLEILGKKFPVTENSKGYKLLPPYLRVIQGDGVDINTLQEIV
EGMKQKMWSIENIAFGSGGGLLQKLTRDLLNCSFKCSYVVTNGLGINVFK
DPVADPNKRSKKGRLSLHRTPAGNFVTLEEGKGDLEEYGQDLLHTVFKNG
KVTKSYSFDEIRKNAQLNIELE
3D structure
PDB4lts Discovery of potent and efficacious cyanoguanidine-containing nicotinamide phosphoribosyltransferase (Nampt) inhibitors.
ChainA
Resolution1.692 Å
3D
structure
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Enzymatic activity
Enzyme Commision number 2.4.2.12: nicotinamide phosphoribosyltransferase.
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 LTS A Y188 H191 F193 R196 D219 Y240 S241 V242 A244 S275 R311 I351 Y173 H176 F178 R181 D204 Y225 S226 V227 A229 S260 R296 I336 MOAD: ic50=4.4nM
PDBbind-CN: -logKd/Ki=8.36,IC50=4.4nM
BindingDB: IC50=6.20nM
Gene Ontology
Molecular Function
GO:0005125 cytokine activity
GO:0005515 protein binding
GO:0016757 glycosyltransferase activity
GO:0042802 identical protein binding
GO:0047280 nicotinamide phosphoribosyltransferase activity
Biological Process
GO:0007165 signal transduction
GO:0007267 cell-cell signaling
GO:0007623 circadian rhythm
GO:0008284 positive regulation of cell population proliferation
GO:0008286 insulin receptor signaling pathway
GO:0009435 NAD biosynthetic process
GO:0019363 pyridine nucleotide biosynthetic process
GO:0032922 circadian regulation of gene expression
GO:0034356 NAD biosynthesis via nicotinamide riboside salvage pathway
GO:0045944 positive regulation of transcription by RNA polymerase II
GO:0048511 rhythmic process
GO:0051770 positive regulation of nitric-oxide synthase biosynthetic process
GO:0060612 adipose tissue development
Cellular Component
GO:0005576 extracellular region
GO:0005615 extracellular space
GO:0005634 nucleus
GO:0005737 cytoplasm
GO:0005829 cytosol
GO:0016607 nuclear speck
GO:0030054 cell junction
GO:0070062 extracellular exosome

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Molecular Function
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Biological Process
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Cellular Component
External links
PDB RCSB:4lts, PDBe:4lts, PDBj:4lts
PDBsum4lts
PubMed24279990
UniProtP43490|NAMPT_HUMAN Nicotinamide phosphoribosyltransferase (Gene Name=NAMPT)

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