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Drug-Target Interaction

Drug

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PubChem ID:5987
Structure:
Synonyms:
07401_RIEDEL
13770-89-3
13770-89-3 (nickel(+2)[2:1] salt)
13770-90-6
13770-90-6 (zinc[2:1] salt)
13770-91-7
13770-91-7 (magnesium[2:1] salt)
13823-50-2
13823-50-2 (mono-potassium salt)
18653-83-3
18653-83-3 (Sn(+2) salt)
242772_SIAL
242780_SIAL
383120_SIAL
481505_ALDRICH
5329-14-6
66027-93-8
66027-93-8 (In(+3) salt)
7773-06-0
7773-06-0 (mono-ammonium salt)
86040_FLUKA
AB1003508
AC1L1LJX
AC1Q55HO
AG-F-82632
AI3-15024
AIDS-018413
AIDS018413
amidohydroxidodioxidosulfur
Amidoschwefelsaeure
Amidosulfonic acid
Amidosulfuric acid
Aminosulfonic acid
Aminosulfuric acid
Caswell No. 809
CHEBI:9330
CHEMBL68253
EINECS 226-218-8
EPA Pesticide Chemical Code 078101
HSDB 795
Imidosulfonic acid
Jumbo
Kyselina amidosulfonova
Kyselina amidosulfonova [Czech]
Kyselina sulfaminova
Kyselina sulfaminova [Czech]
LS-147664
LTBB002877
NCGC00090927-01
NCGC00090927-02
NCIOpen2_000675
NSC 1871
NSC1871
SO3
Sulfamic acid
Sulfamic acid [UN2967] [Corrosive]
Sulfamic acid [UN2967] [Corrosive]
SULFAMIC ACID, ACS
SULFAMIC ACID, REAG
Sulfamidic acid
Sulfamidsaeure
Sulfaminic acid
sulfuramidic acid
Sulphamic acid
Sulphamidic acid
UN2967
WLN: ZSWQ
[S(NH2)O2(OH)]

Target

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Uniprot ID:STS_HUMAN
Synonyms:
Arylsulfatase C
ASC
Steroid sulfatase
Steryl-sulfatase
Steryl-sulfate sulfohydrolase
EC-Numbers:3.1.6.2
Organism:Homo sapiens
Human
PDB IDs:1P49
Structure:
1P49

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

15478125
Sulfamates and their therapeutic potential.. Jean-Yves Winum; Andrea Scozzafava; Jean-Louis Montero; Claudiu T Supuran (2005) Medicinal research reviews display abstract
Starting from the very simple molecule sulfamic acid, O-substituted-, N-substituted-, or di-/tri-substituted sulfamates may be obtained, which show specific biological activities which were or started to be exploited for the design of many types of therapeutic agents. Among them, sulfamate inhibitors of aminoacyl-tRNA synthetases (aaRSs) were recently reported, constituting completely new classes of antibiotics, useful in the fight of drug-resistant infections. Anti-viral agents incorporating sulfamate moieties have also been obtained, with at least two types of such derivatives investigated: the nucleoside/nucleotide human immunodeficiency virus (HIV) reverse transcriptase inhibitors, and the HIV protease inhibitors (PIs). In the increasing armamentarium of anti-cancer drugs, the sulfamates occupy a special position, with at least two important targets evidenced so far: the steroid sulfatases (STSs) and the carbonic anhydrases (CAs). An impressing number of inhibitors of STSs of the sulfamate type have been reported in the last years, with several compounds, such as 667COUMATE among others, progressing to clinical trials for the treatment of hormone-dependent tumors (breast and prostate cancers). This field is rapidly evolving, with many types of new inhibitors being constantly reported and designed in such a way as to increase their anti-tumor properties, and decrease undesired features (for example, estrogenicity, a problem encountered with the first generation such inhibitors, such as EMATE). Among the many isozymes of CAs, at least two, CA IX and CA XII, are highly overexpressed in tumors, being generally absent in the normal tissues. Inhibition of tumor-associated CAs was hypothesized to lead to novel therapeutic approaches for the treatment of cancer. Many sulfamates act as very potent (low nanomolar) CA inhibitors. The X-ray crystal structure of the best-studied isozyme, CA II, with three sulfamates (sulfamic acid, topiramate, and EMATE) has recently been reported, which allowed for a rationale drug design of new inhibitors. Indeed, low nanomolar CA IX inhibitors of the sulfamate type have been reported, although such compounds also act as efficient inhibitors of isozymes CA I and II, which are not associated with tumors. A large number of anti-convulsant sulfamates have been described, with one such compound, topiramate, being widely used clinically as anti-epileptic drug. By taking into consideration a side effect of topiramate, an anti-epileptic drug leading to weight loss in some patients, it has recently been proposed to use this drug and related sulfamates for the treatment of obesity. The rationale of this use is based on the inhibition of the mitochondrial CA isozyme, CA V, involved in lipogenesis. Some sulfamates were also shown to possess potent inhibitory activity against acyl coenzyme A:cholesterol acyltransferase, an enzyme involved in cholesterol metabolism. One such agent, avasimibe, is in advanced clinical trials for the treatment of hyperlipidemia and atherosclerosis. Thus, the sulfamate moiety offers very attractive possibilities for the drug design of various pharmacological agents, which are on one hand due to the relative ease with which such compounds are synthesized, and on the other one, due to the fact that biological activity of most of them is impressive.