LEADER 05315nam 2200661Ia 450 001 9910146237503321 005 20170816123747.0 010 $a1-280-52070-1 010 $a9786610520701 010 $a3-527-60570-3 010 $a3-527-60191-0 035 $a(CKB)1000000000019371 035 $a(EBL)481752 035 $a(OCoLC)64694613 035 $a(SSID)ssj0000192825 035 $a(PQKBManifestationID)11196305 035 $a(PQKBTitleCode)TC0000192825 035 $a(PQKBWorkID)10215894 035 $a(PQKB)11380954 035 $a(MiAaPQ)EBC481752 035 $a(EXLCZ)991000000000019371 100 $a20031216d2004 uy 0 101 0 $aeng 135 $aur|n|---||||| 181 $ctxt 182 $cc 183 $acr 200 00$aLipases and phospholipases in drug development$b[electronic resource] $efrom biochemistry to molecular pharmacology /$fedited by Gu?nter Mu?ller and Stefan Petry 210 $aWeinheim $cWiley-VCH$dc2004 215 $a1 online resource (356 p.) 300 $aDescription based upon print version of record. 311 $a3-527-30677-3 320 $aIncludes bibliographical references and index. 327 $aLipases and Phospholipases in Drug Development; Contents; Preface; List of Contributors; 1 Purification of Lipase; 1.1 Introduction; 1.2 Pre-purification Steps; 1.3 Chromatographic Steps; 1.4 Unique Purification Strategies; 1.5 Theoretical Modeling; 1.5.1 Model Formulation; 1.5.1.1 Mobile Phase; 1.5.1.2 Stationary Phase; 1.5.1.3 Boundary Conditions; 1.5.2 Solution; 1.5.3 Method of Moments; 1.5.4 Model Evaluation; 1.5.5 Simulation Results; 1.5.5.1 Effect of Feed Angle; 1.5.5.2 Effect of Flow Rate; 1.5.5.3 Effect of Rotation Rate; 1.5.5.4 Effect of Column Height; 1.6 Conclusions 327 $a1.7 Acknowledgements1.8 References; 2 Phospholipase A(1) Structures, Physiological and Patho-physiological Roles in Mammals; 2.1 Introduction; 2.2 Phosphatidylserine-specific Phospholipase A(1) (PS-PLA(1)); 2.2.1 Historical Aspects; 2.2.2 Biochemical Characterization and Tissue Distribution; 2.2.3 Structural Characteristics; 2.2.4 Substrate Specificity; 2.2.5 Possible Functions; 2.3 Membrane-associated Phosphatidic Acid-selective Phospholipase A(1)s (mPA-PLA(1)? and mPA-PLA(1)?); 2.3.1 Historical Aspects; 2.3.2 Characterization and Distribution; 2.3.3 Structural Characteristics 327 $a2.3.4 Function2.4 Phosphatidic Acid-preferring Phospholipase A(1) (PA-PLA(1)); 2.4.1 Historical Aspects; 2.4.2 Characterization and Distribution; 2.4.3 Substrate Specificity; 2.4.4 Function; 2.5 KIAA0725P, a Novel PLA(1) with Sequence Homology to a Mammalian Sec23p-interacting Protein, p125; 2.5.1 Historical Aspects; 2.5.2 Characterization and Distribution; 2.6 References; 3 Rational Design of a Liposomal Drug Delivery System Based on Biophysical Studies of Phospholipase A(2) Activity on Model Lipid Membranes; 3.1 Introduction 327 $a3.2 Role for Secretory Phospholipase A(2) (sPLA(2)) in Liposomal Drug Delivery3.3 Lateral Microstructure of Lipid Bilayers and its Influence on sPLA(2); 3.4 sPLA(2) Degradation of Drug-delivery Liposomes: A New Drug-delivery Principle; 3.4.1 Liposomes Protected by Polymer Coating; 3.4.2 Biophysical Model Drug-delivery System to Study sPLA(2) Activity; 3.4.3 Effect of Lipid Composition on sPLA(2)-triggered Drug Release and Absorption; 3.4.4 Effect of Temperature on Liposomal Drug Release and Absorption by sPLA(2); 3.4.5 Liposomal Drug Release as a Function of sPLA(2) Concentration 327 $a3.5 Conclusion3.6 Acknowledgments; 3.7 References; 4 Phospholipase D; 4.1 Introduction; 4.2 Structure and Catalytic Mechanism of Mammalian Phospholipase D; 4.3 Cellular Locations of PLD1 and PLD2; 4.4 Post-translational Modification of PLD; 4.5 Regulation of PLD1 and PLD2; 4.5.1 Role of PIP(2); 4.5.2 Role of PKC; 4.6 Role of Rho Family GTPases; 4.7 Role of Arf Family GTPases; 4.8 Role of Tyrosine Kinase; 4.9 Role of Ral; 4.10 Cellular Functions of PLD; 4.11 Role of PLD in Growth and Differentiation; 4.12 Role of PLD in Vesicle Trafficking in Golgi 327 $a4.13 Role of PLD in Exocytosis and Endocytosis 330 $aLipases and Phospholipases are key control elements in mammalian metabolism. They share many common features that set them apart from other metabolic enzyme classes, most importantly their association with biological membranes. Their potential as drug targets for the treatment of metabolic diseases is widely recognized, and the first lipase inhibitor drugs have been successfully introduced.Providing drug developers with a firm foundation for lipase-centered drug design, the editors of this volume have assembled experts from different scientific disciplines to create a comprehensive handboo 606 $aLipase 606 $aPhospholipases 606 $aDrug development 608 $aElectronic books. 615 0$aLipase. 615 0$aPhospholipases. 615 0$aDrug development. 676 $a572.75 676 $a572.757 701 $aMu?ller$b Gu?nter$0387918 701 $aPetry$b Stefan$0975549 801 0$bMiAaPQ 801 1$bMiAaPQ 801 2$bMiAaPQ 906 $aBOOK 912 $a9910146237503321 996 $aLipases and phospholipases in drug development$92221368 997 $aUNINA