Details of the Drug Therapeutic Target (DTT)

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

• DTT Name: Carbonic anhydrase XIV (CA-XIV)
• Synonyms: UNQ690/PRO1335; Carbonic anhydrase 14; Carbonate dehydratase XIV
• Gene Name: CA14
• DTT Type: Successful target; [1]
• BioChemical Class: Alpha-carbonic anhydrase
• UniProt ID: CAH14_HUMAN
• TTD ID: T31992
• EC Number: EC 4.2.1.1
• Sequence:
  MLFSALLLEVIWILAADGGQHWTYEGPHGQDHWPASYPECGNNAQSPIDIQTDSVTFDPD
  LPALQPHGYDQPGTEPLDLHNNGHTVQLSLPSTLYLGGLPRKYVAAQLHLHWGQKGSPGG
  SEHQINSEATFAELHIVHYDSDSYDSLSEAAERPQGLAVLGILIEVGETKNIAYEHILSH
  LHEVRHKDQKTSVPPFNLRELLPKQLGQYFRYNGSLTTPPCYQSVLWTVFYRRSQISMEQ
  LEKLQGTLFSTEEEPSKLLVQNYRALQPLNQRMVFASFIQAGSSYTTGEMLSLGVGILVG
  CLCLLLAVYFIARKIRKKRLENRKSVVFTSAQATTEA
• Function: 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
Sulfamylon	DMIO1K0	Bacterial infection	1A00-1C4Z	Approved	[1]
TRIENTINE	DMD2WPG	Inborn error of metabolism	5C50-5C59	Approved	[2]

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]
PHENOL	DM1QSM3	N. A.	N. A.	Phase 2/3	[3]
Coumate	DMVKW0N	Breast cancer	2C60-2C65	Phase 2	[5]

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	[2]

66 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2,3-dihydro-1H-indene-5-sulfonamide	DM46MKY	Discovery agent	N.A.	Investigative	[6]
2,4-Disulfamyltrifluoromethylaniline	DM2AW0Z	Discovery agent	N.A.	Investigative	[1]
2-acetamido-2,3-dihydro-1H-indene-5-sulfonic acid	DMIQM4O	Discovery agent	N.A.	Investigative	[6]
2-amino-2,3-dihydro-1H-indene-5-sulfonamide	DMQOCAY	Discovery agent	N.A.	Investigative	[6]
2-Amino-benzenesulfonamide	DMEMANH	Discovery agent	N.A.	Investigative	[1]
2-Amino-indan-5-sulfonic acid	DMCUSH1	Discovery agent	N.A.	Investigative	[6]
2-oxo-2H-chromene-3-carboxylic acid	DMFN769	Discovery agent	N.A.	Investigative	[7]
2-oxo-2H-thiochromene-3-carboxylic acid	DMZTCOM	Discovery agent	N.A.	Investigative	[7]
3-Amino-benzenesulfonamide	DME0TNA	Discovery agent	N.A.	Investigative	[1]
4,4'-thiodipyridine-3-sulfonamide	DM0K5JM	Discovery agent	N.A.	Investigative	[8]
4-(2-AMINOETHYL)BENZENESULFONAMIDE	DMEK6WX	Discovery agent	N.A.	Investigative	[1]
4-(2-Hydroxy-ethyl)-benzenesulfonamide	DM1C5U6	Discovery agent	N.A.	Investigative	[1]
4-(2-Methyl-8-quinolinoxy)-3-pyridinesulfonamide	DME6DHX	Discovery agent	N.A.	Investigative	[8]
4-(2-Propynylthio)pyridine-3-sulfonamide	DMT9RAC	Discovery agent	N.A.	Investigative	[8]
4-(5-Methyl-2-pirazolino)-3-pyridinesulfonamide	DMKT20Q	Discovery agent	N.A.	Investigative	[8]
4-(Allylamino)-3-pyridinesulfonamide	DM6MQCI	Discovery agent	N.A.	Investigative	[8]
4-(Carbamolymethylthio)pyridine-3-sulfonamide	DM12R4M	Discovery agent	N.A.	Investigative	[8]
4-(Cyanomethylthio)pyridine-3-sulfonamide	DMZP20H	Discovery agent	N.A.	Investigative	[8]
4-(hydroxymethyl)benzenesulfonamide	DMR6VWL	Discovery agent	N.A.	Investigative	[1]
4-(Methylhydrazino)-3-pyridinesulfonamide	DM4BPL1	Discovery agent	N.A.	Investigative	[8]
4-(Quinolinoxy)-3-pyridinesulfonamide	DMPNXFA	Discovery agent	N.A.	Investigative	[8]
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-AMINOPHENOL	DMYC1T6	Discovery agent	N.A.	Investigative	[9]
4-Benzythiopyridine-3-sulfonamide	DMI1EFY	Discovery agent	N.A.	Investigative	[8]
4-Ethoxy-3-pyridinesulfonamide	DM8WAOR	Discovery agent	N.A.	Investigative	[8]
4-Hydrazino-3-pyridinesulfonamide	DMSZMQU	Discovery agent	N.A.	Investigative	[8]
4-Hydrazino-benzenesulfonamide	DM49B18	Discovery agent	N.A.	Investigative	[1]
4-Methylthiopyridine-3-sulfonamide	DMEB5XP	Discovery agent	N.A.	Investigative	[8]
6-(aminomethyl)-2H-chromen-2-one	DMJU9TG	Discovery agent	N.A.	Investigative	[7]
6-(hydroxymethyl)-2H-chromen-2-one	DM5TOX2	Discovery agent	N.A.	Investigative	[7]
6-Hydroxy-benzothiazole-2-sulfonic acid amide	DM2B4S5	Discovery agent	N.A.	Investigative	[1]
6-methoxy-2-oxo-2H-chromene-3-carboxylic acid	DM7WH82	Discovery agent	N.A.	Investigative	[7]
6-methyl-2-oxo-2H-chromene-3-carboxylic acid	DMZ6HQL	Discovery agent	N.A.	Investigative	[7]
7-(benzyloxy)-2H-chromen-2-one	DMTKFPW	Discovery agent	N.A.	Investigative	[7]
7-butoxy-2H-chromen-2-one	DM78C5A	Discovery agent	N.A.	Investigative	[7]
7-methoxy-2-oxo-2H-chromene-4-carboxylic acid	DMJITU0	Discovery agent	N.A.	Investigative	[7]
7-phenethoxy-2H-chromen-2-one	DM8Q267	Discovery agent	N.A.	Investigative	[7]
7-propoxy-2H-chromen-2-one	DMD5CB6	Discovery agent	N.A.	Investigative	[7]
8-methoxy-2-oxo-2H-chromene-3-carboxylic acid	DMHCWY8	Discovery agent	N.A.	Investigative	[7]
BENZOLAMIDE	DME5QPX	Discovery agent	N.A.	Investigative	[1]
Beta-D-Mannose	DMHIG9K	Discovery agent	N.A.	Investigative	[10]
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	[11]
COUMARIN	DM0N8ZM	Discovery agent	N.A.	Investigative	[7]
Decane-1,10-diyl disulfamate	DM1ESVR	Discovery agent	N.A.	Investigative	[12]
Decyl sulfamate	DMIERWO	Discovery agent	N.A.	Investigative	[12]
ELLAGIC ACID	DMX8BS5	Discovery agent	N.A.	Investigative	[4]
ETHOXYCOUMARIN	DMSKU4M	Discovery agent	N.A.	Investigative	[7]
Ethyl 7-methoxy-2-oxo-2H-chromene-3-carboxylate	DMWIB0V	Discovery agent	N.A.	Investigative	[7]
GALLICACID	DM6Y3A0	Discovery agent	N.A.	Investigative	[4]
HERNIARIN	DM9UASM	Discovery agent	N.A.	Investigative	[7]
Hexane-1,6-diamine	DMSHF0K	Discovery agent	N.A.	Investigative	[2]
N-propynyl amidebenzenesulphonide	DMWTPJH	Discovery agent	N.A.	Investigative	[13]
N1-(2-aminoethyl)ethane-1,2-diamine	DM6HM5S	Discovery agent	N.A.	Investigative	[2]
N1-(naphthalen-1-yl)ethane-1,2-diamine	DMYGCSV	Discovery agent	N.A.	Investigative	[2]
Octane-1,8-diyl disulfamate	DMBQMGH	Discovery agent	N.A.	Investigative	[12]
Octyl sulfamate	DM40ZCA	Discovery agent	N.A.	Investigative	[12]
P-Coumaric Acid	DMGJSVD	Discovery agent	N.A.	Investigative	[4]
Pentane-1,5-diamine	DMVPZG9	Discovery agent	N.A.	Investigative	[2]
Prop-2-ynyl 4-sulfamoylbenzoate	DM8O41M	Discovery agent	N.A.	Investigative	[13]
RESORCINOL	DMM37C0	Discovery agent	N.A.	Investigative	[9]
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	5.79E-07	-0.09	-0.16

References

• [1] Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides. Bioorg Med Chem Lett. 2005 Sep 1;15(17):3828-33.
• [2] Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. J Med Chem. 2010 Aug 12;53(15):5511-22.
• [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] Indanesulfonamides as carbonic anhydrase inhibitors and anticonvulsant agents: structure-activity relationship and pharmacological evaluation. Eur J Med Chem. 2008 Dec;43(12):2853-60.
• [7] Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins. J Med Chem. 2010 Jan 14;53(1):335-44.
• [8] Carbonic anhydrase inhibitors: synthesis and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associa... Eur J Med Chem. 2010 Jun;45(6):2396-404.
• [9] 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.
• [10] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [11] 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.
• [12] 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.
• [13] Inhibition of membrane-associated carbonic anhydrase isozymes IX, XII and XIV with a library of glycoconjugate benzenesulfonamides. Bioorg Med Chem Lett. 2007 Feb 15;17(4):987-92.