LEADER 04752nam 2200661 450 001 9910140801803321 005 20170810183659.0 010 $a1-282-77490-5 010 $a9786612774904 010 $a3-527-64162-9 010 $a3-527-63094-5 010 $a3-527-63095-3 035 $a(CKB)2670000000043896 035 $a(EBL)584982 035 $a(OCoLC)714797092 035 $a(SSID)ssj0000412224 035 $a(PQKBManifestationID)11294106 035 $a(PQKBTitleCode)TC0000412224 035 $a(PQKBWorkID)10366516 035 $a(PQKB)10109589 035 $a(MiAaPQ)EBC584982 035 $a(MiAaPQ)EBC4042285 035 $a(EXLCZ)992670000000043896 100 $a20160331h20102010 uy 0 101 0 $aeng 135 $aur|n|---||||| 181 $ctxt 182 $cc 183 $acr 200 00$aAspartic acid proteases as therapeutic targets /$fedited by Arun K. Ghosh 210 1$aWeinheim, Germany :$cWiley-VCH,$d2010. 210 4$d©2010 215 $a1 online resource (641 p.) 225 1 $aMethods and Principles in Medicinal Chemistry ;$vVolume 45 300 $aDescription based upon print version of record. 311 $a3-527-31811-9 320 $aIncludes bibliographical references at the end of each chapters and index. 327 $aAspartic Acid Proteases as Therapeutic Targets; Contents; List of Contributors; Preface; A Personal Foreword; Part: One Overview of Aspartic Acid Proteases; 1 Introduction to the Aspartic Proteinase Family; 2 Aspartic Proteases: Structure, Function, and Inhibition; 3 Human Aspartic Proteinases; 4 Structure-Based Drug Design Strategies for Inhibition of Aspartic Proteinases; Part Two: HIV-1 Protease as Target for the Treatment of HIV/AIDS; 5 HIV-1 Protease: Role in Viral Replication, Protein-Ligand X-Ray Crystal Structures and Inhibitor Design 327 $a6 First-Generation HIV-1 Protease Inhibitors for the Treatment of HIV/AIDS7 Second-Generation Approved HIV Protease Inhibitors for the Treatment of HIV/AIDS; 8 Darunavir, a New PI with Dual Mechanism: From a Novel Drug Design Concept to New Hope Against Drug-Resistant HIV; 9 Development of HIV-1 Protease Inhibitors, Antiretroviral Resistance, and Current Challenges of HIV/AIDS Management; Part Three: Renin as Target for the Treatment of Hypertension; 10 Discovery and Development of Aliskiren, the First-in-Class Direct Renin Inhibitor for the Treatment of Hypertension 327 $a11 Evolution of Diverse Classes of Renin Inhibitors Through the YearsPart Four: ?-Secretase as Target for the Treatment of Alzheimer""s Disease; 12: ?-Secretase: An Unusual Enzyme with Many Possible Disease Targets, Including Alzheimer""s Disease; 13 ?-Secretase Inhibition: An Overview of Development of Inhibitors for the Treatment of Alzheimer's Disease; Part Five: ß-Secretase as Target for the Treatment of Alzheimer's Disease; 14 BACE: A (Almost) Perfect Target for Staving Off Alzheimer's Disease 327 $a15 The Discovery of ß-Secretase and Development Toward a Clinical Inhibitor for AD: An Exciting Academic Collaboration16 Peptidomimetic BACE1 Inhibitors for Treatment of Alzheimer.s Disease: Design and Evolution; 17 Nonpeptide BACE1 Inhibitors: Design and Synthesis; Part Six: Plasmepsins and Other Aspartic Proteases as Drug Targets; 18 The Plasmepsin Family as Antimalarial Drug Targets; 19 Plasmepsins Inhibitors as Potential Drugs Against Malaria: Starving the Parasite; 20 Fungal Aspartic Proteases as Possible Therapeutic Targets; Index 330 $aIn this ground-breaking practical reference, the family of aspartic acid proteases is described from a drug developer's perspective. The first part provides a general introduction to the family of aspartic acid proteases, their physiological functions, molecular structure and inhibition. Parts two to five present various case studies of successful protease inhibitor drug design and development, as well as current and potential uses of such inhibitors in pharmaceutical medicine, covering the major therapeutic targets HIV-1 protease, renin, beta-secretase, gamma-secretase,plasmepsins and fungal 410 0$aMethods and principles in medicinal chemistry ;$vVolume 45. 606 $aAspartic proteinases 606 $aAspartic proteinases$xInhibitors$xTherapeutic use 608 $aElectronic books. 615 0$aAspartic proteinases. 615 0$aAspartic proteinases$xInhibitors$xTherapeutic use. 676 $a571.9/36 676 $a612.01516 702 $aGhosh$b Arun K.$cProf. Dr., 801 0$bMiAaPQ 801 1$bMiAaPQ 801 2$bMiAaPQ 906 $aBOOK 912 $a9910140801803321 996 $aAspartic acid proteases as therapeutic targets$92016825 997 $aUNINA