Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTCFSPE)

• DTT Name: Carbonic anhydrase VI (CA-VI)
• Synonyms: Secreted carbonic anhydrase; Salivary carbonic anhydrase; Carbonic anhydrase 6; Carbonate dehydratase VI
• Gene Name: CA6
• DTT Type: Successful target; [1]
• BioChemical Class: Alpha-carbonic anhydrase
• UniProt ID: CAH6_HUMAN
• TTD ID: T06569
• EC Number: EC 4.2.1.1
• Sequence:
  MRALVLLLSLFLLGGQAQHVSDWTYSEGALDEAHWPQHYPACGGQRQSPINLQRTKVRYN
  PSLKGLNMTGYETQAGEFPMVNNGHTVQISLPSTMRMTVADGTVYIAQQMHFHWGGASSE
  ISGSEHTVDGIRHVIEIHIVHYNSKYKSYDIAQDAPDGLAVLAAFVEVKNYPENTYYSNF
  ISHLANIKYPGQRTTLTGLDVQDMLPRNLQHYYTYHGSLTTPPCTENVHWFVLADFVKLS
  RTQVWKLENSLLDHRNKTIHNDYRRTQPLNHRVVESNFPNQEYTLGSEFQFYLHKIEEIL
  DYLRRALN
• Function: Its role in saliva is unknown. Reversible hydration of carbon dioxide.
• KEGG Pathway: Nitrogen metabolism (hsa00910)
• Reactome Pathway: Reversible hydration of carbon dioxide (R-HSA-1475029)

Molecular Interaction Atlas (MIA) of This DTT

2 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Salicyclic acid	DM2F8XZ	Acne vulgaris	ED80	Approved	[2]
Sulfamylon	DMIO1K0	Bacterial infection	1A00-1C4Z	Approved	[1]

4 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Curcumin	DMQPH29	Solid tumour/cancer	2A00-2F9Z	Phase 3	[3]
PARABEN	DMEW5Z8	N. A.	N. A.	Phase 3	[4]
Coumate	DMVKW0N	Breast cancer	2C60-2C65	Phase 2	[5]
SAR566658	DM6Q295	Solid tumour/cancer	2A00-2F9Z	Phase 2	[6]

1 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
FERULIC ACID	DMJC7NF	Discovery agent	N.A.	Patented	[4]

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SPERMINE	DMD4BFY	N. A.	N. A.	Terminated	[7]

39 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2,4-Disulfamyltrifluoromethylaniline	DM2AW0Z	Discovery agent	N.A.	Investigative	[1]
2-Amino-benzenesulfonamide	DMEMANH	Discovery agent	N.A.	Investigative	[1]
2-hydrazinylbenzenesulfonamide	DMCNXZM	Discovery agent	N.A.	Investigative	[1]
4-(2-aminopyrimidin-4-ylamino)benzenesulfonamide	DMWG706	Discovery agent	N.A.	Investigative	[1]
4-(2-Hydroxy-ethyl)-benzenesulfonamide	DM1C5U6	Discovery agent	N.A.	Investigative	[1]
4-(hydroxymethyl)benzenesulfonamide	DMR6VWL	Discovery agent	N.A.	Investigative	[1]
4-Amino-3-bromo-benzenesulfonamide	DMVUCZK	Discovery agent	N.A.	Investigative	[1]
4-Amino-3-chloro-benzenesulfonamide	DMERTQ4	Discovery agent	N.A.	Investigative	[1]
4-Amino-3-fluoro-benzenesulfonamide	DMIQ3VR	Discovery agent	N.A.	Investigative	[1]
4-Amino-3-iodo-benzenesulfonamide	DMCOYHR	Discovery agent	N.A.	Investigative	[1]
4-amino-6-chlorobenzene-1,3-disulfonamide	DMIWGZS	Discovery agent	N.A.	Investigative	[1]
4-amino-N-(4-sulfamoylbenzyl)benzenesulfonamide	DMJZNX6	Discovery agent	N.A.	Investigative	[1]
4-CYANOPHENOL	DMN12EX	Discovery agent	N.A.	Investigative	[2]
4-Hydrazino-benzenesulfonamide	DM49B18	Discovery agent	N.A.	Investigative	[1]
6-(aminomethyl)-2H-chromen-2-one	DMJU9TG	Discovery agent	N.A.	Investigative	[8]
6-(hydroxymethyl)-2H-chromen-2-one	DM5TOX2	Discovery agent	N.A.	Investigative	[8]
6-Hydroxy-benzothiazole-2-sulfonic acid amide	DM2B4S5	Discovery agent	N.A.	Investigative	[1]
7-butoxy-2H-chromen-2-one	DM78C5A	Discovery agent	N.A.	Investigative	[8]
7-propoxy-2H-chromen-2-one	DMD5CB6	Discovery agent	N.A.	Investigative	[8]
BENZOLAMIDE	DME5QPX	Discovery agent	N.A.	Investigative	[1]
Carzenide	DMVD481	Discovery agent	N.A.	Investigative	[1]
CATECHIN	DMY38SB	Discovery agent	N.A.	Investigative	[3]
CL-5343	DM9AFZ3	Solid tumour/cancer	2A00-2F9Z	Investigative	[9]
COUMARIN	DM0N8ZM	Discovery agent	N.A.	Investigative	[8]
Decane-1,10-diyl disulfamate	DM1ESVR	Discovery agent	N.A.	Investigative	[10]
Decyl sulfamate	DMIERWO	Discovery agent	N.A.	Investigative	[10]
ELLAGIC ACID	DMX8BS5	Discovery agent	N.A.	Investigative	[4]
Ethyl 7-methoxy-2-oxo-2H-chromene-3-carboxylate	DMWIB0V	Discovery agent	N.A.	Investigative	[8]
GALLICACID	DM6Y3A0	Discovery agent	N.A.	Investigative	[4]
HERNIARIN	DM9UASM	Discovery agent	N.A.	Investigative	[8]
Hexane-1,6-diamine	DMSHF0K	Discovery agent	N.A.	Investigative	[7]
N1-(2-aminoethyl)ethane-1,2-diamine	DM6HM5S	Discovery agent	N.A.	Investigative	[7]
N1-(naphthalen-1-yl)ethane-1,2-diamine	DMYGCSV	Discovery agent	N.A.	Investigative	[7]
Octane-1,8-diyl disulfamate	DMBQMGH	Discovery agent	N.A.	Investigative	[10]
Octyl sulfamate	DM40ZCA	Discovery agent	N.A.	Investigative	[10]
P-Coumaric Acid	DMGJSVD	Discovery agent	N.A.	Investigative	[4]
P-toluenesulfonamide	DMPEKTO	Discovery agent	N.A.	Investigative	[1]
Pentane-1,5-diamine	DMVPZG9	Discovery agent	N.A.	Investigative	[7]
Syringic Acid	DM802V7	Discovery agent	N.A.	Investigative	[4]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Breast cancer	2C82	Breast tissue	3.64E-10	-0.17	-0.37

References

• [1] Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV. J Med Chem. 2009 Feb 12;52(3):646-54.
• [2] 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.
• [3] Carbonic anhydrase inhibitors. Antioxidant polyphenols effectively inhibit mammalian isoforms I-XV. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5050-3.
• [4] Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids. Bioorg Med Chem. 2010 Mar 15;18(6):2159-2164.
• [5] Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-r... Bioorg Med Chem Lett. 2008 Aug 1;18(15):4282-6.
• [6] An Antibody-Drug Conjugate Targeting MUC1-Associated Carbohydrate CA6 Shows Promising Antitumor Activities. Mol Cancer Ther. 2020 Aug;19(8):1660-1669.
• [7] Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. J Med Chem. 2010 Aug 12;53(15):5511-22.
• [8] Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins. J Med Chem. 2010 Jan 14;53(1):335-44.
• [9] Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a l... Bioorg Med Chem Lett. 2010 Aug 1;20(15):4376-81.
• [10] Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-bi... J Med Chem. 2009 Oct 8;52(19):5990-8.