Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0H4WA)
Name
Myophosphorylase (PYGM)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Glycogen phosphorylase b; Glycogen phosphorylase, muscle form; Glycogen phosphorylase muscle form; Muscle glycogen phosphorylase; Myophosphorylase
Family Transferase (TFase)  >>  Glycosyltransferases (EC 2.4)
Organism
Homo sapiens (Human)
Gene Name PYGM Gene ID
5837
UniProt ID PYGM_HUMAN (click to find more protein-related data of this DBT)
TTD ID T95399 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MSRPLSDQEKRKQISVRGLAGVENVTELKKNFNRHLHFTLVKDRNVATPRDYYFALAHTV
RDHLVGRWIRTQQHYYEKDPKRIYYLSLEFYMGRTLQNTMVNLALENACDEATYQLGLDM
EELEEIEEDAGLGNGGLGRLAACFLDSMATLGLAAYGYGIRYEFGIFNQKISGGWQMEEA
DDWLRYGNPWEKARPEFTLPVHFYGHVEHTSQGAKWVDTQVVLAMPYDTPVPGYRNNVVN
TMRLWSAKAPNDFNLKDFNVGGYIQAVLDRNLAENISRVLYPNDNFFEGKELRLKQEYFV
VAATLQDIIRRFKSSKFGCRDPVRTNFDAFPDKVAIQLNDTHPSLAIPELMRILVDLERM
DWDKAWDVTVRTCAYTNHTVLPEALERWPVHLLETLLPRHLQIIYEINQRFLNRVAAAFP
GDVDRLRRMSLVEEGAVKRINMAHLCIAGSHAVNGVARIHSEILKKTIFKDFYELEPHKF
QNKTNGITPRRWLVLCNPGLAEVIAERIGEDFISDLDQLRKLLSFVDDEAFIRDVAKVKQ
ENKLKFAAYLEREYKVHINPNSLFDIQVKRIHEYKRQLLNCLHVITLYNRIKREPNKFFV
PRTVMIGGKAAPGYHMAKMIIRLVTAIGDVVNHDPAVGDRLRVIFLENYRVSLAEKVIPA
ADLSEQISTAGTEASGTGNMKFMLNGALTIGTMDGANVEMAEEAGEENFFIFGMRVEDVD
KLDQRGYNAQEYYDRIPELRQVIEQLSSGFFSPKQPDLFKDIVNMLMHHDRFKVFADYED
YIKCQEKVSALYKNPREWTRMVIRNIATSGKFSSDRTIAQYAREIWGVEPSRQRLPAPDE
AI
Function
Enzymes from different sources differ in their regulatory mechanisms and in their natural substrates. However, all known phosphorylases share catalytic and structural properties. Phosphorylase is an important allosteric enzyme in carbohydrate metabolism.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Caffeine Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Other agent
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 114000 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID PYGM_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 74900 nM (tested by experiment) [2]
                   Tested Species Oryctolagus cuniculus (Rabbit)
                   UniProt ID PYGM_RABIT
             Experiment (3) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 182000 nM (tested by experiment) [3]
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID PYGM_RAT
References
1 Pentacyclic triterpenes. Part 1: the first examples of naturally occurring pentacyclic triterpenes as a new class of inhibitors of glycogen phosphorylases. Bioorg Med Chem Lett. 2005 Nov 15; 15(22):4944-8.
2 Terpenoids. III: Synthesis and biological evaluation of 23-hydroxybetulinic acid derivatives as novel inhibitors of glycogen phosphorylase. Bioorg Med Chem Lett. 2009 Dec 15; 19(24):6966-9.
3 Discovery of new nanomolar inhibitors of GPa: Extension of 2-oxo-1,2-dihydropyridinyl-3-yl amide-based GPa inhibitors. Eur J Med Chem. 2017 Feb 15; 127:341-356.

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