LEADER 04820nam 2200709Ia 450 001 9911018822903321 005 20200520144314.0 010 $a9786612774904 010 $a9781282774902 010 $a1282774905 010 $a9783527641628 010 $a3527641629 010 $a9783527630943 010 $a3527630945 010 $a9783527630950 010 $a3527630953 035 $a(CKB)2670000000043896 035 $a(EBL)584982 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(OCoLC)714797092 035 $a(Perlego)1010613 035 $a(EXLCZ)992670000000043896 100 $a20100427d2010 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 $aWeinheim $cWiley-VCH$d2010 215 $a1 online resource (641 p.) 225 1 $aMethods and principles in medicinal chemistry ;$vv. 45 300 $aDescription based upon print version of record. 311 08$a9783527318117 311 08$a3527318119 320 $aIncludes bibliographical references 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 ;$vv. 45. 606 $aAspartic proteinases 606 $aAspartic proteinases$xInhibitors$xTherapeutic use 615 0$aAspartic proteinases. 615 0$aAspartic proteinases$xInhibitors$xTherapeutic use. 676 $a571.9/36 676 $a612.01516 701 $aGhosh$b Arun K.$cProf. Dr.$01636192 801 0$bMiAaPQ 801 1$bMiAaPQ 801 2$bMiAaPQ 906 $aBOOK 912 $a9911018822903321 996 $aAspartic acid proteases as therapeutic targets$94416016 997 $aUNINA