LEADER 04198nam  22006255  450 
001 9910337943803321
005 20200703104525.0
010   $a3-030-12780-X
024 7 $a10.1007/978-3-030-12780-0
035   $a(CKB)4100000008280448
035   $a(MiAaPQ)EBC5779998
035   $a(DE-He213)978-3-030-12780-0
035   $a(PPN)236525212
035   $a(EXLCZ)994100000008280448
100   $a20190521d2019      u|         0
101 0 $aeng
135   $aurcnu||||||||
181   $ctxt$2rdacontent
182   $cc$2rdamedia
183   $acr$2rdacarrier
200 10$aCarbonic Anhydrase as Drug Target $eThermodynamics and Structure of Inhibitor Binding /$fedited by Daumantas Matulis
205   $a1st ed. 2019.
210  1$aCham :$cSpringer International Publishing :$cImprint: Springer,$d2019.
215   $a1 online resource (358 pages)
311   $a3-030-12778-8 
320   $aIncludes bibliographical references and index.
327   $aFinal ToC tbd. 1) Description of human carbonic anhydrases (12 catalytically active human isoforms; isoforms as drug targets, enzymatic activity, catalytic mechanism, thermodynamics of protonation of the water molecule in the active site) -- 2) Thermal stabilities of all isoform CA catalytic domains -- Thermodynamics of inhibitor binding to CAs (incl. intrinsic thermodynamics - not mentioned important subject in most CA literature) -- 3) Comparison of methods to determine inhibitor binding to CAs (ITC, FTSA, enzymatic activity assays) -- 4) Chemical synthesis of CA inhibitors -- 5) X-ray crystallographic structures of CAs and their complexes with inhibitors -- 6) Antibodies against CAs.
330   $aThis book offers deep insights into the thermodynamics and molecular structures of the twelve catalytically active isoforms of human carbonic anhydrase (CA) with a particular focus on inhibitor binding for drug design. X-ray crystallographic structures in combination with enzyme kinetic testing provide information on the interaction of CAs and their inhibitors, knowledge which is crucial for rational drug design. CAs are zinc carrying enzymes that catalyse the reversible interconversion of carbon dioxide and bicarbonate and are involved in numerous cellular processes. They are therefore a common target for drugs. The suppression of CA activities through inhibitory compounds has found application for example in diuretics and in glaucoma therapy. In this book methods used to determine binding thermodynamics of inhibitory compounds (Isothermal titration calorimetry, Fluorescent thermal shift assay/differential scanning fluorimetry and others) will be compared in detail. Also types and chemical synthesis of CA inhibitors, the use of antibodies against CAs as well as inhibitor application in animals are discussed. .
606   $aMolecular biology
606   $aMedical biochemistry
606   $aProteins 
606   $aMedicinal chemistry
606   $aPharmaceutical technology
606   $aMolecular Medicine$3https://scigraph.springernature.com/ontologies/product-market-codes/B1700X
606   $aMedical Biochemistry$3https://scigraph.springernature.com/ontologies/product-market-codes/H35005
606   $aProtein-Ligand Interactions$3https://scigraph.springernature.com/ontologies/product-market-codes/L14060
606   $aMedicinal Chemistry$3https://scigraph.springernature.com/ontologies/product-market-codes/C28000
606   $aPharmaceutical Sciences/Technology$3https://scigraph.springernature.com/ontologies/product-market-codes/B21010
615  0$aMolecular biology.
615  0$aMedical biochemistry.
615  0$aProteins .
615  0$aMedicinal chemistry.
615  0$aPharmaceutical technology.
615 14$aMolecular Medicine.
615 24$aMedical Biochemistry.
615 24$aProtein-Ligand Interactions.
615 24$aMedicinal Chemistry.
615 24$aPharmaceutical Sciences/Technology.
676   $a572.79
676   $a611.01816
702   $aMatulis$b Daumantas$4edt$4http://id.loc.gov/vocabulary/relators/edt
906   $aBOOK
912   $a9910337943803321
996   $aCarbonic Anhydrase as Drug Target$91945683
997   $aUNINA