Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00291

Target Information
NameMaltase-glucoamylase, intestinal    
Type of targetSuccessful target    
SynonymsAlpha-glucosidase    
DiseaseDiabetes mellitus
[ICD9: 250   ICD10: E08-E13]
[1]
Drug(s)AcarboseApprovedDiabetes mellitus[2][3]
MiglitolApprovedDiabetes mellitus[1]
VogliboseApprovedDiabetes mellitus[4]
AcarbosePhase IIICardiovascular Disorders[4][2]
BioChemical ClassTransmembrane protein    
EC NumberEC 3.2.1.20
PathwayGalactose metabolism
Metabolic pathways
Starch and sucrose metabolism
UniProt IDO43451
PDB Structure2QLY; 2QMJ; 3CTT; 3L4T; 3L4U; 3L4V; 3L4W; 3L4X; 3L4Y; 3L4Z; 3TON; 3TOP.    
FunctionMay serve as an alternate pathway for starch digestion when luminal alpha-amylase activity is reduced because of immaturity or malnutrition. May play a unique role in the digestion of malted dietary oligosaccharides used in food manufacturing.    
SequenceMARKKLKKFTTLEIVLSVLLLVLFIISIVLIVLLAKESLKSTAPDPGTTGTPDPGTTGTP DPGTTGTTHARTTGPPDPGTTGTTPVSAECPVVNELERINCIPDQPPTKATCDQRGCCWN PQGAVSVPWCYYSKNHSYHVEGNLVNTNAGFTARLKNLPSSPVFGSNVDNVLLTAEYQTS NRFHFKLTDQTNNRFEVPHEHVQSFSGNAAASLTYQVEISRQPFSIKVTRRSNNRVLFDS SIGPLLFADQFLQLSTRLPSTNVYGLGEHVHQQYRHDMNWKTWPIFNRDTTPNGNGTNLY GAQTFFLCLEDASGLSFGVFLMNSNAMEVVLQPAPAITYRTIGGILDFYVFLGNTPEQVV QEYLELIGRPALPSYWALGFHLSRYEYGTLDNMREVVERNRAAQLPYDVQHADIDYMDER RDFTYDSVDFKGFPEFVNELHNNGQKLVIIVDPAISNNSSSSKPYGPYDRGSDMKIWVNS SDGVTPLIGEVWPGQTVFPDYTNPNCAVWWTKEFELFHNQVEFDGIWIDMNEVSNFVDGS VSGCSTNNLNNPPFTPRILDGYLFCKTLCMDAVQHWGKQYDIHNLYGYSMAVATAEAAKT VFPNKRSFILTRSTFAGSGKFAAHWLGDNTATWDDLRWSIPGVLEFNLFGIPMVGPDICG FALDTPEELCRRWMQLGAFYPFSRNHNGQGYKDQDPASFGADSLLLNSSRHYLNIRYTLL PYLYTLFFRAHSRGDTVARPLLHEFYEDNSTWDVHQQFLWGPGLLITPVLDEGAEKVMAY VPDAVWYDYETGSQVRWRKQKVEMELPGDKIGLHLRGGYIFPTQQPNTTTLASRKNPLGL IIALDENKEAKGELFWDNGETKDTVANKVYLLCEFSVTQNRLEVNISQSTYKDPNNLAFN EIKILGTEEPSNVTVKHNGVPSQTSPTVTYDSNLKVAIITDIDLLLGEAYTVEWSIKIRD EEKIDCYPDENGASAENCTARGCIWEASNSSGVPFCYFVNDLYSVSDVQYNSHGATADIS LKSSVYANAFPSTPVNPLRLDVTYHKNEMLQFKIYDPNKNRYEVPVPLNIPSMPSSTPEG QLYDVLIKKNPFGIEIRRKSTGTIIWDSQLLGFTFSDMFIRISTRLPSKYLYGFGETEHR SYRRDLEWHTWGMFSRDQPPGYKKNSYGVHPYYMGLEEDGSAHGVLLLNSNAMDVTFQPL PALTYRTTGGVLDFYVFLGPTPELVTQQYTELIGRPVMVPYWSLGFQLCRYGYQNDSEIA SLYDEMVAAQIPYDVQYSDIDYMERQLDFTLSPKFAGFPALINRMKADGMRVILILDPAI SGNETQPYPAFTRGVEDDVFIKYPNDGDIVWGKVWPDFPDVVVNGSLDWDSQVELYRAYV AFPDFFRNSTAKWWKREIEELYNNPQNPERSLKFDGMWIDMNEPSSFVNGAVSPGCRDAS LNHPPYMPHLESRDRGLSSKTLCMESQQILPDGSLVQHYNVHNLYGWSQTRPTYEAVQEV TGQRGVVITRSTFPSSGRWAGHWLGDNTAAWDQLKKSIIGMMEFSLFGISYTGADICGFF QDAEYEMCVRWMQLGAFYPFSRNHNTIGTRRQDPVSWDVAFVNISRTVLQTRYTLLPYLY TLMHKAHTEGVTVVRPLLHEFVSDQVTWDIDSQFLLGPAFLVSPVLERNARNVTAYFPRA RWYDYYTGVDINARGEWKTLPAPLDHINLHVRGGYILPWQEPALNTHLSRQKFMGFKIAL DDEGTAGGWLFWDDGQSIDTYGKGLYYLASFSASQNTMQSHIIFNNYITGTNPLKLGYIE IWGVGSVPVTSVSISVSGMVITPSFNNDPTTQVLSIDVTDRNISLHNFTSLTWISTL
Related US Patent6,299,911
6,455,573
Target ValidationClick to Find Target Validation Information.    
Inhibitor1,4-dideoxy-1,4-imino-D-arabinito[5]
2,5-Dideoxy-2,5-imino-D-mannitol[5]
2-Aminomethyl-pyrrolidine-3,4-diol[6]
2-Cyclopentylaminomethyl-pyrrolidine-3,4-diol[6]
3- (4-[7]
4'- (p-toluenesulfonamide)-3,4-dihydroxy chalcone[8]
Acarbose[2][3]
Acarbose[4][2]
DEOXYNOJIRIMYCIN[9]
Double Oxidized Cysteine[10]
KOTALANOL[11]
Maltose[12]
Miglitol[1]
Nicotinamide-Adenine-Dinucleotide[10]
PONKORANOL[13]
SALACINOL[11]
Voglibose[4]
de-O-sulfonated kotalanol[11]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Drug therapy of postprandial hyperglycaemia. Drugs. 1999 Jan;57(1):19-29. To Reference
Ref 2Cardiovascular benefits of acarbose in impaired glucose tolerance and type 2 diabetes. Int J Cardiol. 2006 Feb 8;107(1):11-20. To Reference
Ref 3Nat Rev Drug Discov. 2003 Jan;2(1):38-51.Knockouts model the 100 best-selling drugs--will they model the next 100? To Reference
Ref 4Effects of changeover from voglibose to acarbose on postprandial triglycerides in type 2 diabetes mellitus patients. Adv Ther. 2009 Jun;26(6):660-6. Epub 2009 Jun 30. To Reference
Ref 5J Nat Prod. 2002 Feb;65(2):198-202.New sugar-mimic alkaloids from the pods of Angylocalyx pynaertii. To Reference
Ref 6Bioorg Med Chem Lett. 2001 Sep 17;11(18):2489-93.Derivatives of (2R,3R,4S)-2-aminomethylpyrrolidine-3,4-diol are selective alpha-mannosidase inhibitors. To Reference
Ref 7Bioorg Med Chem. 2008 Jan 1;16(1):284-92. Epub 2007 Sep 22.Discovery of novel alpha-glucosidase inhibitors based on the virtual screening with the homology-modeled protein structure. To Reference
Ref 8Bioorg Med Chem Lett. 2005 Dec 15;15(24):5514-6. Epub 2005 Oct 3.Sulfonamide chalcone as a new class of alpha-glucosidase inhibitors. To Reference
Ref 9J Med Chem. 1994 Oct 28;37(22):3701-6.Nitrogen-in-the-ring pyranoses and furanoses: structural basis of inhibition of mammalian glycosidases. 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
Ref 11Bioorg Med Chem. 2010 Nov 15;18(22):7794-8. Epub 2010 Sep 29.Probing the active-site requirements of human intestinal N-terminal maltase-glucoamylase: Synthesis and enzyme inhibitory activities of a six-membered ring nitrogen analogue of kotalanol and its de-O-sulfonated derivative. To Reference
Ref 12Nucleic Acids Res. 2011 January; 39(Database issue): D1035¨CD1041. DrugBank 3.0: a comprehensive resource for ¡®Omics¡¯ research on drugs To Reference
Ref 13Bioorg Med Chem Lett. 2010 Oct 1;20(19):5686-9. Epub 2010 Aug 11.Probing the active-site requirements of human intestinal N-terminal maltase glucoamylase: the effect of replacing the sulfate moiety by a methyl ether in ponkoranol, a naturally occurring ¦Á-glucosidase inhibitor. To Reference



 

Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.


Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore


All rights reserved.

   
 
 
Computer-aided Drug Design
about BIDD |  databases |  software |  teaching |  research |  links

 

Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543