FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2100386666> ?p ?o ?g. }

• W2100386666 endingPage "228" @default.
• W2100386666 startingPage "186" @default.
• W2100386666 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." @default.
• W2100386666 created "2016-06-24" @default.
• W2100386666 creator A5012797490 @default.
• W2100386666 creator A5035013697 @default.
• W2100386666 creator A5083642064 @default.
• W2100386666 creator A5090525653 @default.
• W2100386666 date "2004-01-01" @default.
• W2100386666 modified "2023-10-12" @default.
• W2100386666 title "Sulfamates and their therapeutic potential" @default.
• W2100386666 cites W13946816 @default.
• W2100386666 cites W1509732336 @default.
• W2100386666 cites W1549224984 @default.
• W2100386666 cites W1843300456 @default.
• W2100386666 cites W1964408420 @default.
• W2100386666 cites W1966899798 @default.
• W2100386666 cites W1966971943 @default.
• W2100386666 cites W1969665073 @default.
• W2100386666 cites W1973109666 @default.
• W2100386666 cites W1973813358 @default.
• W2100386666 cites W1976375282 @default.
• W2100386666 cites W1976752852 @default.
• W2100386666 cites W1978887142 @default.
• W2100386666 cites W1980866137 @default.
• W2100386666 cites W1982063637 @default.
• W2100386666 cites W1982074106 @default.
• W2100386666 cites W1982891950 @default.
• W2100386666 cites W1985029412 @default.
• W2100386666 cites W1985043270 @default.
• W2100386666 cites W1986466656 @default.
• W2100386666 cites W1989250669 @default.
• W2100386666 cites W1989276141 @default.
• W2100386666 cites W1990938350 @default.
• W2100386666 cites W1991080894 @default.
• W2100386666 cites W1993706660 @default.
• W2100386666 cites W1993924528 @default.
• W2100386666 cites W1994991797 @default.
• W2100386666 cites W1996208375 @default.
• W2100386666 cites W2001070076 @default.
• W2100386666 cites W2001861941 @default.
• W2100386666 cites W2002973513 @default.
• W2100386666 cites W2004028476 @default.
• W2100386666 cites W2005643164 @default.
• W2100386666 cites W2005989077 @default.
• W2100386666 cites W2011101734 @default.
• W2100386666 cites W2012713167 @default.
• W2100386666 cites W2013720878 @default.
• W2100386666 cites W2016681412 @default.
• W2100386666 cites W2017436619 @default.
• W2100386666 cites W2017505758 @default.
• W2100386666 cites W2021796609 @default.
• W2100386666 cites W2023991964 @default.
• W2100386666 cites W2024162717 @default.
• W2100386666 cites W2024703446 @default.
• W2100386666 cites W2025001185 @default.
• W2100386666 cites W2026161126 @default.
• W2100386666 cites W2028713603 @default.
• W2100386666 cites W2029154177 @default.
• W2100386666 cites W2029953509 @default.
• W2100386666 cites W2030838926 @default.
• W2100386666 cites W2031808408 @default.
• W2100386666 cites W2033078718 @default.
• W2100386666 cites W2034207827 @default.
• W2100386666 cites W2034233153 @default.
• W2100386666 cites W2035391529 @default.
• W2100386666 cites W2035720137 @default.
• W2100386666 cites W2036035252 @default.
• W2100386666 cites W2037894465 @default.
• W2100386666 cites W2039078428 @default.
• W2100386666 cites W2040073841 @default.
• W2100386666 cites W2041143470 @default.
• W2100386666 cites W2041368906 @default.
• W2100386666 cites W2042116997 @default.
• W2100386666 cites W2042685194 @default.
• W2100386666 cites W2042983666 @default.
• W2100386666 cites W2044347375 @default.
• W2100386666 cites W2044356885 @default.
• W2100386666 cites W2046292937 @default.
• W2100386666 cites W2046895642 @default.
• W2100386666 cites W2052933595 @default.
• W2100386666 cites W2053531428 @default.
• W2100386666 cites W2053611922 @default.
• W2100386666 cites W2055432912 @default.
• W2100386666 cites W2055548299 @default.
• W2100386666 cites W2055875149 @default.
• W2100386666 cites W2056719400 @default.
• W2100386666 cites W2061066255 @default.
• W2100386666 cites W2061419229 @default.
• W2100386666 cites W2064865290 @default.
• W2100386666 cites W2065461165 @default.
• W2100386666 cites W2066863172 @default.
• W2100386666 cites W2067284991 @default.
• W2100386666 cites W2070866396 @default.
• W2100386666 cites W2071674869 @default.
• W2100386666 cites W2077224086 @default.
• W2100386666 cites W2078830969 @default.
• W2100386666 cites W2080398125 @default.
• W2100386666 cites W2080520986 @default.
• W2100386666 cites W2080845610 @default.

• next