Target Information
Target General Infomation | |||||
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Target ID |
T92777
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Former ID |
TTDS00291
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Target Name |
Maltase-glucoamylase, intestinal
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Gene Name |
MGAM
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Synonyms |
Alpha-glucosidase; MGAM
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Target Type |
Successful
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Disease | Acquired immune deficiency syndrome [ICD9: 42; ICD10: B20] | ||||
Cardiovascular disorder [ICD10: I00-I99] | |||||
Dengue fever [ICD9: 61; ICD10: A90] | |||||
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1] | |||||
Hyperglycemia [ICD9: 790.29; ICD10: R73.9] | |||||
Muscle disease [ICD10: M60-M63] | |||||
Pompe's disease [ICD10: E74.02] | |||||
Type 2 diabetes [ICD9: 250; ICD10: E11] | |||||
Function |
May 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.
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BioChemical Class |
Glycosylases
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Target Validation |
T92777
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UniProt ID | |||||
EC Number |
EC 3.2.1.3
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Sequence |
MARKKLKKFTTLEIVLSVLLLVLFIISIVLIVLLAKESLKSTAPDPGTTGTPDPGTTGTP
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 |
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Drugs and Mode of Action | |||||
Drug(s) | Acarbose | Drug Info | Approved | Diabetes | [536361], [541872] |
Miglitol | Drug Info | Approved | Diabetes | [468076], [536361] | |
Rh-alphaglucosidase | Drug Info | Approved | Pompe's disease | [551871] | |
Voglibose | Drug Info | Approved | Diabetes | [536361] | |
Acarbose | Drug Info | Phase 3 | Cardiovascular disorder | [536361], [541872] | |
Alpha-glucosidase | Drug Info | Phase 3 | Muscle disease | [523686] | |
Deoxynojirimycin | Drug Info | Phase 3 | Pompe's disease | [530482] | |
PAZ-320 | Drug Info | Phase 2 | Type 2 diabetes | [524644] | |
SC-49483 | Drug Info | Phase 2 | Acquired immune deficiency syndrome | [521416] | |
Celgosivir | Drug Info | Phase 1/2 | Dengue fever | [545627] | |
Maltose | Drug Info | Phase 1/2 | Discovery agent | [523849] | |
SALACINOL | Drug Info | Phase 1/2 | Discovery agent | [521814] | |
A-76202M | Drug Info | Terminated | Acquired immune deficiency syndrome | [526163] | |
Inhibitor | 1,4-dideoxy-1,4-imino-D-arabinito | Drug Info | [526274] | ||
2,5-Dideoxy-2,5-imino-D-mannitol | Drug Info | [526274] | |||
2-Aminomethyl-pyrrolidine-3,4-diol | Drug Info | [526137] | |||
2-Cyclopentylaminomethyl-pyrrolidine-3,4-diol | Drug Info | [526137] | |||
3-(4-(4-hydroxyphenyl)phthalazin-1-ylamino)phenol | Drug Info | [529085] | |||
4'-(p-toluenesulfonamide)-3,4-dihydroxy chalcone | Drug Info | [527781] | |||
De-O-sulfonated kotalanol | Drug Info | [531230] | |||
Deoxynojirimycin | Drug Info | [533823] | |||
Double Oxidized Cysteine | Drug Info | [551393] | |||
GSC-1 | Drug Info | [543667] | |||
KOTALANOL | Drug Info | [531230] | |||
Maltose | Drug Info | [551391] | |||
Miglitol | Drug Info | [538156] | |||
Nicotinamide-Adenine-Dinucleotide | Drug Info | [551393] | |||
PONKORANOL | Drug Info | [531131] | |||
SALACINOL | Drug Info | [531230] | |||
SC-49483 | Drug Info | [534275] | |||
Voglibose | Drug Info | [537567] | |||
Modulator | A-76202M | Drug Info | [526163] | ||
Acarbose | Drug Info | [556264] | |||
Alpha-glucosidase | Drug Info | [543667] | |||
BMN-103 | Drug Info | [543667] | |||
Celgosivir | Drug Info | ||||
Imino sugars | Drug Info | [543667] | |||
PAZ-320 | Drug Info | [544481] | |||
Rh-alphaglucosidase | Drug Info | [528715] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Galactose metabolism | ||||
Starch and sucrose metabolism | |||||
Metabolic pathways | |||||
Carbohydrate digestion and absorption | |||||
PathWhiz Pathway | Starch and Sucrose Metabolism | ||||
WikiPathways | Metabolism of carbohydrates | ||||
References | |||||
Ref 468076 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4842). | ||||
Ref 521416 | ClinicalTrials.gov (NCT00000791) A Phase II Double-Blind Study of Two Doses of SC-49483 in Combination With Zidovudine (ZDV) Versus ZDV. U.S. National Institutes of Health. | ||||
Ref 521814 | ClinicalTrials.gov (NCT00306072) Effect of Different Doses of Salacinol Extract on Glycemic and Insulinemic Response in Patients With Type 2 Diabetes. U.S. National Institutes of Health. | ||||
Ref 523686 | ClinicalTrials.gov (NCT01468181) A Study of LY2189265 in Japanese Participants With Type 2 Diabetes Mellitus. U.S. National Institutes of Health. | ||||
Ref 523849 | ClinicalTrials.gov (NCT01562626) Phase I/II Study of APS001F With Flucytosine and Maltose in Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 524644 | ClinicalTrials.gov (NCT02060916) Study to Evaluate the Safety and Efficacy of PAZ320 in Patients With Type 2 Diabetes. U.S. National Institutes of Health. | ||||
Ref 526163 | Synthesis and biological activity of 4',8-dihydroxyisoflavon-7-yl D-hexopyranosides. Carbohydr Res. 2001 Oct 15;335(4):283-9. | ||||
Ref 530482 | The pharmacological chaperone 1-deoxynojirimycin increases the activity and lysosomal trafficking of multiple mutant forms of acid alpha-glucosidase. Hum Mutat. 2009 Dec;30(12):1683-92. | ||||
Ref 536361 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
Ref 541872 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6791). | ||||
Ref 526137 | Bioorg 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. | ||||
Ref 526163 | Synthesis and biological activity of 4',8-dihydroxyisoflavon-7-yl D-hexopyranosides. Carbohydr Res. 2001 Oct 15;335(4):283-9. | ||||
Ref 526274 | J Nat Prod. 2002 Feb;65(2):198-202.New sugar-mimic alkaloids from the pods of Angylocalyx pynaertii. | ||||
Ref 527781 | Bioorg Med Chem Lett. 2005 Dec 15;15(24):5514-6. Epub 2005 Oct 3.Sulfonamide chalcone as a new class of alpha-glucosidase inhibitors. | ||||
Ref 529085 | Bioorg 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. | ||||
Ref 531131 | Bioorg 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 |A-glucosidase inhibitor. | ||||
Ref 531230 | Bioorg 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 asix-membered ring nitrogen analogue of kotalanol and its de-O-sulfonated derivative. | ||||
Ref 533823 | J Med Chem. 1994 Oct 28;37(22):3701-6.Nitrogen-in-the-ring pyranoses and furanoses: structural basis of inhibition of mammalian glycosidases. | ||||
Ref 534275 | Pathology of perbutylated-N-butyl-1-deoxynojiromycin (an alpha-glucosidase-1 inhibitor) in Sprague-Dawley rats. Toxicol Pathol. 1996 Sep-Oct;24(5):531-8. | ||||
Ref 537567 | Effects 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. | ||||
Ref 543667 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2627). | ||||
Ref 544481 | Treatment With Novel Galactomannan Derivative Reduces 2-Hour Postprandial Glucose Excursions in Individuals With Type 2 Diabetes Treated With Oral Medications and/or Insulin. J Diabetes Sci Technol. 2014 September; 8(5): 1018-1022. |
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