Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00141

Target Information
NameHexokinase D    
Type of targetClinical trial target    
SynonymsGCK    
Glucokinase    
HK IV    
HK4    
Hexokinase type IV    
DiseaseBenign prostatic hyperplasia
[ICD9: 600   ICD10: N40]
[1][2][3]
Diabetes Mellitus Type 1 and 2
[ICD9: 250   ICD10: E08-E13]
[4]
Noninsulin-dependent diabetes mellitus
[ICD9: 250   ICD10: E08-E13]
[5][6]
Prostate Disorders[1][2][3]
Drug(s)AMG 151Phase IIType 2 diabetes
AZD1656Phase IIType 2 Diabetes Mellitus[7]
R7201Phase IIType 2 diabetes[8]
GK1-399Phase I/IIType 2 diabetes
AZD6370Phase I completedType 2 Diabetes[7]
AZD5658Phase IObesity, Diabetes[9]
DS-7309Phase IDiabetes
PSN-101Phase IDiabetes Mellitus Type 1 and 2[4]
TAK-329Phase IDiabetes mellitus
TAK-329Phase IType 1 diabetes
TTP355Phase IType 2 diabetes
LonidamineTerminated in Phase IIIBenign Prostatic Hyperplasia, Prostate Disorders[1][2][3]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.1
PathwayAmino sugar and nucleotide sugar metabolism
Glycolysis / Gluconeogenesis
Insulin signaling pathway
Maturity onset diabetes of the young
Metabolic pathways
Starch and sucrose metabolism
Type II diabetes mellitus
UniProt IDP35557
PDB Structure1GLK; 1V4S; 1V4T; 3A0I; 3F9M; 3FGU; 3FR0; 3GOI; 3H1V; 3ID8; 3IDH; 3IMX; 3QIC; 3S41; 3VEV; 3VEY; 3VF6; 4DCH; 4DHY; 4ISE; 4ISF; 4ISG; 4IWV; 4IXC.    
FunctionCatalyzes the initial step in utilization of glucose by the beta-cell and liver at physiological glucose concentration. Glucokinase has a high km for glucose, and so it is effective only when glucose is abundant.    
SequenceMLDDRARMEAAKKEKVEQILAEFQLQEEDLKKVMRRMQKEMDRGLRLETHEEASVKMLPT YVRSTPEGSEVGDFLSLDLGGTNFRVMLVKVGEGEEGQWSVKTKHQMYSIPEDAMTGTAE MLFDYISECISDFLDKHQMKHKKLPLGFTFSFPVRHEDIDKGILLNWTKGFKASGAEGNN VVGLLRDAIKRRGDFEMDVVAMVNDTVATMISCYYEDHQCEVGMIVGTGCNACYMEEMQN VELVEGDEGRMCVNTEWGAFGDSGELDEFLLEYDRLVDESSANPGQQLYEKLIGGKYMGE LVRLVLLRLVDENLLFHGEASEQLRTRGAFETRFVSQVESDTGDRKQIYNILSTLGLRPS TTDCDIVRRACESVSTRAAHMCSAGLAGVINRMRESRSEDVMRITVGVDGSVYKLHPSFK ERFHASVRRLTPSCEITFIESEEGSGRGAALVSAVACKKACMLGQ
Related US Patent6,320,050
6,353,111
6,369,232
6,384,220
6,388,071
6,388,088
6,433,188
6,441,180
6,441,184
6,448,399
6,482,951
6,486,184
6,489,485
6,545,155
6,583,288
6,608,218
6,610,846
Target ValidationClick to Find Target Validation Information.    
InhibitorBeta-D-Glucose[10]
Lonidamine[1][2][3]
ActivatorAZD1656[7]
AZD5658[9]
AZD6370[7]
GKA1[6]
GKA2[6]
PSN-101[4]
R7201[8]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Development of a Yeast Bio-Assay to Screen Anti-Mitochondrial Drugs. Curr Drug Discov Technol. 2009 Sep 1. [Epub ahead of print] To Reference
Ref 2Human cytomegalovirus US9 protein contains an N-terminal signal sequence and a C-terminal mitochondrial localization domain, and does not alter cellular sensitivity to apoptosis. J Gen Virol. 2009 May;90(Pt 5):1172-82. Epub 2009 Mar 4. To Reference
Ref 3The anti-trypanosomal agent lonidamine inhibits Trypanosoma brucei hexokinase 1. Mol Biochem Parasitol. 2008 Apr;158(2):202-7. Epub 2008 Jan 3. To Reference
Ref 4CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008. To Reference
Ref 5Insights into the biochemical and genetic basis of glucokinase activation from naturally occurring hypoglycemia mutations. Diabetes. 2003 Sep;52(9):2433-40. To Reference
Ref 6Stimulation of hepatocyte glucose metabolism by novel small molecule glucokinase activators. Diabetes. 2004 Mar;53(3):535-41. To Reference
Ref 7AstraZeneca. Product Development Pipeline. January 29 2009. To Reference
Ref 8Roche. Product Development Pipeline. July 29 2009. To Reference
Ref 92011 Pipeline of AstraZeneca. To Reference
Ref 10Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference



 

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