Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0KC5P)
Name
Arachidonate 5-lipoxygenase (ALOX5)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Arachidonate 5-lipoxygenase; 5-LO; 5-lipoxygenase; LOG5
Family Oxidoreductase (ORase)  >>  Oxygen single donor oxidoreductase (EC 1.13)
Organism
Homo sapiens (Human)
Gene Name ALOX5 Gene ID
240
UniProt ID LOX5_HUMAN (click to find more protein-related data of this DBT)
TTD ID T00140 (click to find more therapeutic target data of this DBT)
INTEDE ID DME0201 (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
MPSYTVTVATGSQWFAGTDDYIYLSLVGSAGCSEKHLLDKPFYNDFERGAVDSYDVTVDE
ELGEIQLVRIEKRKYWLNDDWYLKYITLKTPHGDYIEFPCYRWITGDVEVVLRDGRAKLA
RDDQIHILKQHRRKELETRQKQYRWMEWNPGFPLSIDAKCHKDLPRDIQFDSEKGVDFVL
NYSKAMENLFINRFMHMFQSSWNDFADFEKIFVKISNTISERVMNHWQEDLMFGYQFLNG
CNPVLIRRCTELPEKLPVTTEMVECSLERQLSLEQEVQQGNIFIVDFELLDGIDANKTDP
CTLQFLAAPICLLYKNLANKIVPIAIQLNQIPGDENPIFLPSDAKYDWLLAKIWVRSSDF
HVHQTITHLLRTHLVSEVFGIAMYRQLPAVHPIFKLLVAHVRFTIAINTKAREQLICECG
LFDKANATGGGGHVQMVQRAMKDLTYASLCFPEAIKARGMESKEDIPYYFYRDDGLLVWE
AIRTFTAEVVDIYYEGDQVVEEDPELQDFVNDVYVYGMRGRKSSGFPKSVKSREQLSEYL
TVVIFTASAQHAAVNFGQYDWCSWIPNAPPTMRAPPPTAKGVVTIEQIVDTLPDRGRSCW
HLGAVWALSQFQENELFLGMYPEEHFIEKPVKEAMARFRKNLEAIVSVIAERNKKKQLPY
YYLSPDRIPNSVAI
Function
Catalyzes the first step in leukotriene biosynthesis, and thereby plays a role in inflammatory processes.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Ethyl isovalerate 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
Flavoring agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 35000 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID LOX5_HUMAN
          DIG Name: Propyl gallate 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
Antimicrobial preservative; Antioxidant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 0.43 uM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID LOX5_HUMAN
          DIG Name: Cinnamaldehyde 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
Flavoring agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 35000 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID LOX5_HUMAN
          DIG Name: Ethyl vanillate 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
Flavoring agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 270 uM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID LOX5_HUMAN
          DIG Name: Gentisic acid 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
Antioxidant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 75000 nM (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID LOX5_HUMAN
          DIG Name: Stearic hydrazide 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
Emulsifying agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 6000 nM (estimated based on the structural similarity with CHEMBL25790 ) [4]
                   Structural Similarity Tanimoto coefficient = 0.75
                   Tested Species Homo sapiens (Human)
                   UniProt ID LOX5_HUMAN
References
1 5-Lipoxygenase as a drug target: A review on trends in inhibitors structural design, SAR and mechanism based approach. Bioorg Med Chem. 2019 Sep 1; 27(17):3745-3759.
2 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
3 Identifying chelators for metalloprotein inhibitors using a fragment-based approach. J Med Chem. 2011 Jan 27; 54(2):591-602.
4 Structure-activity relationships of the pyridazinone series of 5-lipoxygenase inhibitors. Bioorg Med Chem Lett. (1992) 2:1357-1360.

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