Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET00FYL)
Name
Squalene synthase (FDFT1)
Synonyms    Click to Show/Hide the Synonyms of This DBT
FPP:FPP farnesyltransferase; Farnesyl-diphosphate farnesyltransferase; Farnesyl-diphosphate farnesyltransferase 1; SQS; SS
Family Transferase (TFase)  >>  Alkyl/aryl transferase (EC 2.5)
Organism
Homo sapiens (Human)
Gene Name FDFT1 Gene ID
2222
UniProt ID FDFT_HUMAN (click to find more protein-related data of this DBT)
TTD ID T81850 (click to find more therapeutic target data of this DBT)
INTEDE ID DME0571 (click to find more drug-metabolizing enzyme data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MEFVKCLGHPEEFYNLVRFRIGGKRKVMPKMDQDSLSSSLKTCYKYLNQTSRSFAAVIQA
LDGEMRNAVCIFYLVLRALDTLEDDMTISVEKKVPLLHNFHSFLYQPDWRFMESKEKDRQ
VLEDFPTISLEFRNLAEKYQTVIADICRRMGIGMAEFLDKHVTSEQEWDKYCHYVAGLVG
IGLSRLFSASEFEDPLVGEDTERANSMGLFLQKTNIIRDYLEDQQGGREFWPQEVWSRYV
KKLGDFAKPENIDLAVQCLNELITNALHHIPDVITYLSRLRNQSVFNFCAIPQVMAIATL
AACYNNQQVFKGAVKIRKGQAVTLMMDATNMPAVKAIIYQYMEEIYHRIPDSDPSSSKTR
QIISTIRTQNLPNCQLISRSHYSPIYLSFVMLLAALSWQYLTTLSQVTEDYVQTGEH
Function
Catalyzes the condensation of 2 farnesyl pyrophosphate (FPP) moieties to form squalene. Proceeds in two distinct steps. In the first half-reaction, two molecules of FPP react to form the stable presqualene diphosphate intermediate (PSQPP), with concomitant release of a proton and a molecule of inorganic diphosphate. In the second half-reaction, PSQPP undergoes heterolysis, isomerization, and reduction with NADPH or NADH to form squalene. It is the first committed enzyme of the sterol biosynthesis pathway.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Monostearyl citrate 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
Emollient
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 9000 nM (estimated based on the structural similarity with CHEMBL78764 ) [1]
                   Structural Similarity Tanimoto coefficient = 0.835820896
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID FDFT_RAT
References
1 Isolation, structure determination and squalene synthase activity of L-731,120 and L-731,128, alkyl citrate analogs of zaragozic acids A and B. Bioorg Med Chem Lett. (1995) 5:2403-2408.

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