Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0PG6J)
Name
Carbonic anhydrase IX (CA9)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Carbonate dehydratase IX; Carbonic anhydrase IX; CA-IX; CAIX; Membrane antigen MN; P54/58N; Renal cell carcinoma-associated antigen G250; RCC-associated antigen G250; pMW1; PMW1; MN; G250 antigen (MN/CA IX/G250); G250; Carbonic anhydrase 9
Family Lyase/isomerase/ligase (L/I/G)  >>  Carbon-oxygen lyase (EC 4.2)
Organism
Homo sapiens (Human)
Gene Name CA9 Gene ID
768
UniProt ID CAH9_HUMAN (click to find more protein-related data of this DBT)
TTD ID T64567 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MAPLCPSPWLPLLIPAPAPGLTVQLLLSLLLLVPVHPQRLPRMQEDSPLGGGSSGEDDPL
GEEDLPSEEDSPREEDPPGEEDLPGEEDLPGEEDLPEVKPKSEEEGSLKLEDLPTVEAPG
DPQEPQNNAHRDKEGDDQSHWRYGGDPPWPRVSPACAGRFQSPVDIRPQLAAFCPALRPL
ELLGFQLPPLPELRLRNNGHSVQLTLPPGLEMALGPGREYRALQLHLHWGAAGRPGSEHT
VEGHRFPAEIHVVHLSTAFARVDEALGRPGGLAVLAAFLEEGPEENSAYEQLLSRLEEIA
EEGSETQVPGLDISALLPSDFSRYFQYEGSLTTPPCAQGVIWTVFNQTVMLSAKQLHTLS
DTLWGPGDSRLQLNFRATQPLNGRVIEASFPAGVDSSPRAAEPVQLNSCLAAGDILALVF
GLLFAVTSVAFLVQMRRQHRRGTKGGVSYRPAEVAETGA
Function
Participates in pH regulation. May be involved in the control of cell proliferation and transformation. Appears to be a novel specific biomarker for a cervical neoplasia. Reversible hydration of carbon dioxide.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Acesulfame 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 = 2400 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CAH9_HUMAN
          DIG Name: Benzosulfimide 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 = 100 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CAH9_HUMAN
          DIG Name: Calcium carbonate 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
Binding agent; Buffering agent; Diluent; Opacifying agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 8600 nM (estimated based on the structural similarity with CHEMBL1161632 ) [3]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Homo sapiens (Human)
                   UniProt ID CAH9_HUMAN
          DIG Name: methylparaben 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
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 5500 nM (tested by experiment) [4]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CAH9_HUMAN
          DIG Name: Sucralose 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 = 2200 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CAH9_HUMAN
          DIG Name: Compressible sugar 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
Binding agent; Diluent; Flavoring agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki > 20000 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CAH9_HUMAN
          DIG Name: Ethylparaben 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
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 8200 nM (tested by experiment) [4]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CAH9_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 Ki = 6600 nM (tested by experiment) [4]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CAH9_HUMAN
          DIG Name: Hydroquinone 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 Ki = 32500 nM (tested by experiment) [5]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CAH9_HUMAN
          DIG Name: Phenol 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
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 8800 nM (tested by experiment) [6]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CAH9_HUMAN
          DIG Name: Sodium cyclamate 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 = 81.3 nM (tested by experiment) [7]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CAH9_HUMAN
References
1 Sweet Binders: Carbonic Anhydrase IX in Complex with Sucralose. ACS Med Chem Lett. 2018 May 10; 9(7):657-661.
2 Seriously Sweet: Acesulfame K Exhibits Selective Inhibition Using Alternative Binding Modes in Carbonic Anhydrase Isoforms. J Med Chem. 2018 Feb 8; 61(3):1176-1181.
3 Carbonic anhydrase inhibitors. Inhibition of isozymes I, II, IV, V, and IX with anions isosteric and isoelectronic with sulfate, nitrate, and carbonate. Bioorg Med Chem Lett. 2005 Feb 1; 15(3):567-71.
4 Mono-/dihydroxybenzoic acid esters and phenol pyridinium derivatives as inhibitors of the mammalian carbonic anhydrase isoforms I, II, VII, IX, XII and XIV. Bioorg Med Chem. 2013 Mar 15; 21(6):1564-9.
5 Carbonic anhydrase inhibitors: inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid. Bioorg Med Chem. 2008 Aug 1; 16(15):7424-8.
6 Salen and tetrahydrosalen derivatives act as effective inhibitors of the tumor-associated carbonic anhydrase XII--a new scaffold for designing isoform-selective inhibitors. Bioorg Med Chem Lett. 2013 Dec 15; 23(24):6759-63.
7 Sulfamide derivatives with selective carbonic anhydrase VII inhibitory action. Bioorg Med Chem. 2016 Feb 15; 24(4):894-901.

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