The Resource Phosphodiesterases and Their Inhibitors : Phosphodiesterases and Their Inhibitors

Phosphodiesterases and Their Inhibitors : Phosphodiesterases and Their Inhibitors

Label
Phosphodiesterases and Their Inhibitors : Phosphodiesterases and Their Inhibitors
Title
Phosphodiesterases and Their Inhibitors
Title remainder
Phosphodiesterases and Their Inhibitors
Creator
Contributor
Subject
Genre
Language
eng
Summary
Written by the pioneers of Viagra, the first blockbuster PDE inhibitor drug. Beginning with a review of the first wave of phosphodiesterase (PDE) inhibitors, this book focuses on new and emerging PDE targets and their inhibitors. Drug development options for all major human PDE families are discussed and cover diverse therapeutic fields, such as neurological/psychiatric, cardiovascular/metabolic, pain, and allergy/respiratory diseases. Finally, emerging chemotherapeutic applications of PDE inhibitors against malaria and other tropical diseases are discussed
Member of
Cataloging source
MiAaPQ
http://library.link/vocab/creatorName
Mannhold, Raimund
LC call number
QP609.C92 -- .P467 2014eb
Literary form
non fiction
Nature of contents
dictionaries
http://library.link/vocab/relatedWorkOrContributorName
  • Kubinyi, Hugo
  • Folkers, Gerd
  • Liras, Spiros
  • Bell, Andrew S
  • ProQuest (Firm)
Series statement
Methods and Principles in Medicinal Chemistry Ser.
Series volume
v.61
http://library.link/vocab/subjectName
  • Cyclic nucleotide phosphodiesterases
  • Phosphodiesterases -- Inhibitors -- Therapeutic use
  • Phosphodiesterases -- Inhibitors
Label
Phosphodiesterases and Their Inhibitors : Phosphodiesterases and Their Inhibitors
Link
http://ebookcentral.proquest.com/lib/multco/detail.action?docID=1650854
Instantiates
Publication
Copyright
Carrier category
online resource
Carrier category code
cr
Carrier MARC source
rdacarrier
Color
multicolored
Content category
text
Content type code
txt
Content type MARC source
rdacontent
Contents
  • Phosphodiesterases and Their Inhibitors -- Contents -- List of Contributors -- Preface -- A Personal Foreword -- 1 Introduction -- 2 Toward a New Generation of PDE5 Inhibitors through Advances in Medicinal Chemistry -- 2.1 Introduction -- 2.2 The First-Generation Agents -- 2.3 PDE5 as a Mechanism and Alternative Indications Beyond MED -- 2.4 A Summary of PDE5 Chemotypes Reported Post-2010 -- 2.5 Second-Generation PDE5 Inhibitors from Pfizer: Pyrazolopyrimidines -- 2.6 Second-Generation PDE5 Inhibitors from Pfizer: Pyridopyrazinones -- 2.7 Conclusions -- References -- 3 PDE4: New Structural Insights into the Regulatory Mechanism and Implications for the Design of Selective Inhibitors -- 3.1 Introduction -- 3.2 Isoforms, Domain Organization, and Splice Variants -- 3.3 Structural Features of the Catalytic Site -- 3.4 Regulation of PDE4 Activity -- 3.5 Crystal Structure of Regulatory Domains of PDE4 -- 3.6 UCR2 Interaction and Selectivity -- 3.7 Conclusions -- References -- 4 PDE4: Recent Medicinal Chemistry Strategies to Mitigate Adverse Effects -- 4.1 Introduction -- 4.2 Brief Summary of pan-PDE4 Inhibitors -- 4.2.1 Rolipram -- 4.2.2 Roflumilast -- 4.2.3 Cilomilast -- 4.2.4 Apremilast -- 4.3 PDE4 Strategies to Avoid Gastrointestinal Events -- 4.3.1 Allosteric Modulation -- 4.3.2 PDE4D Selectivity -- 4.3.3 Pfizer -- 4.3.4 Novartis -- 4.3.5 Merck-Frosst -- 4.3.6 GEBR-7b -- 4.3.7 PDE4B Selectivity -- 4.3.8 Asahi Kasei -- 4.3.9 GlaxoSmithKline -- 4.3.10 Pfizer -- 4.3.11 Tissue Targeting -- 4.3.12 Polypharmacology -- 4.3.13 Olanzapine Derivatives -- 4.4 Conclusions -- References -- 5 The Function, Enzyme Kinetics, Structural Biology, and Medicinal Chemistry of PDE10A -- 5.1 Enzymology and Protein Structure -- 5.2 Papaverine-Related PDE10A Inhibitors -- 5.3 MP-10/PF-2545920 Class of Inhibitors -- 5.4 PF-2545920/MP-Inspired Inhibitors
  • 5.5 PF-2545920/Papaverine/Quinazoline Hybrid Series of Inhibitors -- 5.6 PET Ligand Development -- 5.7 Summary and Future -- References -- 6 The State of the Art in Selective PDE2A Inhibitor Design -- 6.1 Introduction -- 6.2 Selective PDE2A Inhibitors -- 6.2.1 Bayer -- 6.2.2 Altana AG -- 6.2.3 Biotie Therapies -- 6.2.4 Boehringer Ingelheim -- 6.2.5 Janssen -- 6.2.6 Lundbeck -- 6.2.7 Merck -- 6.2.8 Neuro3d -- 6.2.9 Pfizer -- 6.3 Methods -- 6.4 Conclusions -- References -- 7 Crystal Structures of Phosphodiesterase 9A and Insight into Inhibitor Discovery -- 7.1 Introduction -- 7.2 Subtle Asymmetry of the PDE9 Dimer in the Crystals -- 7.3 The Structure of the PDE9 Catalytic Domain -- 7.4 Interaction of Inhibitors with PDE9 -- 7.5 Implication on Inhibitor Selectivity -- References -- 8 PDEs as CNS Targets: PDE9 Inhibitors for Cognitive Deficit Diseases -- 8.1 PDE9A Enzymology and Pharmacology -- 8.2 Crystal Structures of PDE9A Inhibitors -- 8.3 Medicinal Chemistry Efforts toward Identifying PDE9A Inhibitors for Treating Cognitive Disorders -- 8.3.1 Bayer -- 8.3.2 Pfizer -- 8.3.3 Boehringer Ingelheim -- 8.3.4 Sun Yat-Sen University, China -- 8.3.5 Envivo Pharmaceuticals -- 8.4 Analysis of CNS Desirability of PDE9A Inhibitors -- 8.5 Conclusions -- References -- 9 Phosphodiesterase 8B -- 9.1 Introduction -- 9.2 Identification -- 9.3 Properties -- 9.4 Expression and Tissue Distribution -- 9.5 Functions of PDE8B -- 9.5.1 Thyroid -- 9.5.2 Adrenal Gland -- 9.5.3 Pancreatic Islets -- 9.6 Inhibitors and Potential Therapeutic Uses -- References -- 10 Selective New Small-Molecule Inhibitors of Phosphodiesterase 1 -- 10.1 Introduction -- 10.2 PDE1 Enzymology -- 10.3 PDE1 Inhibitors -- 10.3.1 Non-Selective PDE1 Inhibitors -- 10.3.2 Selective PDE1 inhibitors -- 10.4 Conclusion -- References -- 11 Recent Advances in the Development of PDE7 Inhibitors
  • 11.1 Introduction -- 11.1.1 PDE7: Subtypes and Distribution -- 11.1.2 Rationale for PDE7 as a Therapeutic Target -- 11.2 Historical Development of PDE7 Inhibitors -- 11.2.1 Early Examples of Nonselective and Selective Lead Matter -- 11.2.2 Developing Selective Lead Matter from Nonselective Hits -- 11.2.3 Targeting PDE4/7 Dual Inhibitors -- 11.3 Recent Advances in the Discovery of PDE7 Inhibitors for Peripheral Therapeutic Benefit -- 11.3.1 PDE7 Inhibitors for the Treatment of T Cell-Related Disorders -- 11.3.1.1 Developments in PDE7 Inhibitors for the Treatment of Airway-Related Disorders -- 11.3.1.2 Developments in PDE7 Inhibitors for the Treatment of Nonairway- Related Disorders -- 11.3.1.3 Summary of T-Cell-Related Research -- 11.3.2 PDE7 Inhibitors for the Treatment of Neuropathic Pain -- 11.4 Recent Advances in the Discovery of PDE7 Inhibitors for CNS-Related Disorders -- 11.4.1 Creating PDE7 Inhibitors by Ligand-Based Virtual Screening Methods -- 11.4.2 Repositioning PDE7 Inhibitors Designed for the Treatment of Peripheral Diseases -- 11.5 Recent Advances in the Discovery of Dual PDE7 Inhibitors -- 11.5.1 Dual PDE4/7 Inhibitors -- 11.5.2 Dual PDE7/8 Inhibitors -- 11.6 Identifying Next-Generation PDE7 Inhibitors -- 11.6.1 Emerging Chemotypes as Novel PDE7 Inhibitors -- 11.6.2 Novel Methods to Identify PDE7 Inhibitors -- 11.6.2.1 Computational Methods to Identify New PDE7 Inhibitors -- 11.6.2.2 Fission Yeast-Based HTS to Identify New PDE7 Inhibitors -- 11.7 Summary -- References -- 12 Inhibitors of Protozoan Phosphodiesterases as Potential Therapeutic Approaches for Tropical Diseases -- 12.1 Introduction -- 12.2 Malaria -- 12.2.1 PfPDE Inhibition Studies -- 12.3 Chagas Disease -- 12.4 Leishmaniasis -- 12.5 Human African Trypanosomiasis -- 12.6 Conclusion -- References -- Index
Control code
EBC1650854
Dimensions
unknown
Edition
1st ed.
Extent
1 online resource (238 pages)
Form of item
online
Isbn
9783527682355
Media category
computer
Media MARC source
rdamedia
Media type code
c
Note
Electronic reproduction. Ann Arbor, Michigan : ProQuest Ebook Central, 2017. Available via World Wide Web. Access may be limited to ProQuest Ebook Central affiliated libraries.
Sound
unknown sound
Specific material designation
remote
System control number
  • (MiAaPQ)EBC1650854
  • (Au-PeEL)EBL1650854
  • (CaPaEBR)ebr10849214
  • (CaONFJC)MIL584446
  • (OCoLC)874321908
Label
Phosphodiesterases and Their Inhibitors : Phosphodiesterases and Their Inhibitors
Link
http://ebookcentral.proquest.com/lib/multco/detail.action?docID=1650854
Publication
Copyright
Carrier category
online resource
Carrier category code
cr
Carrier MARC source
rdacarrier
Color
multicolored
Content category
text
Content type code
txt
Content type MARC source
rdacontent
Contents
  • Phosphodiesterases and Their Inhibitors -- Contents -- List of Contributors -- Preface -- A Personal Foreword -- 1 Introduction -- 2 Toward a New Generation of PDE5 Inhibitors through Advances in Medicinal Chemistry -- 2.1 Introduction -- 2.2 The First-Generation Agents -- 2.3 PDE5 as a Mechanism and Alternative Indications Beyond MED -- 2.4 A Summary of PDE5 Chemotypes Reported Post-2010 -- 2.5 Second-Generation PDE5 Inhibitors from Pfizer: Pyrazolopyrimidines -- 2.6 Second-Generation PDE5 Inhibitors from Pfizer: Pyridopyrazinones -- 2.7 Conclusions -- References -- 3 PDE4: New Structural Insights into the Regulatory Mechanism and Implications for the Design of Selective Inhibitors -- 3.1 Introduction -- 3.2 Isoforms, Domain Organization, and Splice Variants -- 3.3 Structural Features of the Catalytic Site -- 3.4 Regulation of PDE4 Activity -- 3.5 Crystal Structure of Regulatory Domains of PDE4 -- 3.6 UCR2 Interaction and Selectivity -- 3.7 Conclusions -- References -- 4 PDE4: Recent Medicinal Chemistry Strategies to Mitigate Adverse Effects -- 4.1 Introduction -- 4.2 Brief Summary of pan-PDE4 Inhibitors -- 4.2.1 Rolipram -- 4.2.2 Roflumilast -- 4.2.3 Cilomilast -- 4.2.4 Apremilast -- 4.3 PDE4 Strategies to Avoid Gastrointestinal Events -- 4.3.1 Allosteric Modulation -- 4.3.2 PDE4D Selectivity -- 4.3.3 Pfizer -- 4.3.4 Novartis -- 4.3.5 Merck-Frosst -- 4.3.6 GEBR-7b -- 4.3.7 PDE4B Selectivity -- 4.3.8 Asahi Kasei -- 4.3.9 GlaxoSmithKline -- 4.3.10 Pfizer -- 4.3.11 Tissue Targeting -- 4.3.12 Polypharmacology -- 4.3.13 Olanzapine Derivatives -- 4.4 Conclusions -- References -- 5 The Function, Enzyme Kinetics, Structural Biology, and Medicinal Chemistry of PDE10A -- 5.1 Enzymology and Protein Structure -- 5.2 Papaverine-Related PDE10A Inhibitors -- 5.3 MP-10/PF-2545920 Class of Inhibitors -- 5.4 PF-2545920/MP-Inspired Inhibitors
  • 5.5 PF-2545920/Papaverine/Quinazoline Hybrid Series of Inhibitors -- 5.6 PET Ligand Development -- 5.7 Summary and Future -- References -- 6 The State of the Art in Selective PDE2A Inhibitor Design -- 6.1 Introduction -- 6.2 Selective PDE2A Inhibitors -- 6.2.1 Bayer -- 6.2.2 Altana AG -- 6.2.3 Biotie Therapies -- 6.2.4 Boehringer Ingelheim -- 6.2.5 Janssen -- 6.2.6 Lundbeck -- 6.2.7 Merck -- 6.2.8 Neuro3d -- 6.2.9 Pfizer -- 6.3 Methods -- 6.4 Conclusions -- References -- 7 Crystal Structures of Phosphodiesterase 9A and Insight into Inhibitor Discovery -- 7.1 Introduction -- 7.2 Subtle Asymmetry of the PDE9 Dimer in the Crystals -- 7.3 The Structure of the PDE9 Catalytic Domain -- 7.4 Interaction of Inhibitors with PDE9 -- 7.5 Implication on Inhibitor Selectivity -- References -- 8 PDEs as CNS Targets: PDE9 Inhibitors for Cognitive Deficit Diseases -- 8.1 PDE9A Enzymology and Pharmacology -- 8.2 Crystal Structures of PDE9A Inhibitors -- 8.3 Medicinal Chemistry Efforts toward Identifying PDE9A Inhibitors for Treating Cognitive Disorders -- 8.3.1 Bayer -- 8.3.2 Pfizer -- 8.3.3 Boehringer Ingelheim -- 8.3.4 Sun Yat-Sen University, China -- 8.3.5 Envivo Pharmaceuticals -- 8.4 Analysis of CNS Desirability of PDE9A Inhibitors -- 8.5 Conclusions -- References -- 9 Phosphodiesterase 8B -- 9.1 Introduction -- 9.2 Identification -- 9.3 Properties -- 9.4 Expression and Tissue Distribution -- 9.5 Functions of PDE8B -- 9.5.1 Thyroid -- 9.5.2 Adrenal Gland -- 9.5.3 Pancreatic Islets -- 9.6 Inhibitors and Potential Therapeutic Uses -- References -- 10 Selective New Small-Molecule Inhibitors of Phosphodiesterase 1 -- 10.1 Introduction -- 10.2 PDE1 Enzymology -- 10.3 PDE1 Inhibitors -- 10.3.1 Non-Selective PDE1 Inhibitors -- 10.3.2 Selective PDE1 inhibitors -- 10.4 Conclusion -- References -- 11 Recent Advances in the Development of PDE7 Inhibitors
  • 11.1 Introduction -- 11.1.1 PDE7: Subtypes and Distribution -- 11.1.2 Rationale for PDE7 as a Therapeutic Target -- 11.2 Historical Development of PDE7 Inhibitors -- 11.2.1 Early Examples of Nonselective and Selective Lead Matter -- 11.2.2 Developing Selective Lead Matter from Nonselective Hits -- 11.2.3 Targeting PDE4/7 Dual Inhibitors -- 11.3 Recent Advances in the Discovery of PDE7 Inhibitors for Peripheral Therapeutic Benefit -- 11.3.1 PDE7 Inhibitors for the Treatment of T Cell-Related Disorders -- 11.3.1.1 Developments in PDE7 Inhibitors for the Treatment of Airway-Related Disorders -- 11.3.1.2 Developments in PDE7 Inhibitors for the Treatment of Nonairway- Related Disorders -- 11.3.1.3 Summary of T-Cell-Related Research -- 11.3.2 PDE7 Inhibitors for the Treatment of Neuropathic Pain -- 11.4 Recent Advances in the Discovery of PDE7 Inhibitors for CNS-Related Disorders -- 11.4.1 Creating PDE7 Inhibitors by Ligand-Based Virtual Screening Methods -- 11.4.2 Repositioning PDE7 Inhibitors Designed for the Treatment of Peripheral Diseases -- 11.5 Recent Advances in the Discovery of Dual PDE7 Inhibitors -- 11.5.1 Dual PDE4/7 Inhibitors -- 11.5.2 Dual PDE7/8 Inhibitors -- 11.6 Identifying Next-Generation PDE7 Inhibitors -- 11.6.1 Emerging Chemotypes as Novel PDE7 Inhibitors -- 11.6.2 Novel Methods to Identify PDE7 Inhibitors -- 11.6.2.1 Computational Methods to Identify New PDE7 Inhibitors -- 11.6.2.2 Fission Yeast-Based HTS to Identify New PDE7 Inhibitors -- 11.7 Summary -- References -- 12 Inhibitors of Protozoan Phosphodiesterases as Potential Therapeutic Approaches for Tropical Diseases -- 12.1 Introduction -- 12.2 Malaria -- 12.2.1 PfPDE Inhibition Studies -- 12.3 Chagas Disease -- 12.4 Leishmaniasis -- 12.5 Human African Trypanosomiasis -- 12.6 Conclusion -- References -- Index
Control code
EBC1650854
Dimensions
unknown
Edition
1st ed.
Extent
1 online resource (238 pages)
Form of item
online
Isbn
9783527682355
Media category
computer
Media MARC source
rdamedia
Media type code
c
Note
Electronic reproduction. Ann Arbor, Michigan : ProQuest Ebook Central, 2017. Available via World Wide Web. Access may be limited to ProQuest Ebook Central affiliated libraries.
Sound
unknown sound
Specific material designation
remote
System control number
  • (MiAaPQ)EBC1650854
  • (Au-PeEL)EBL1650854
  • (CaPaEBR)ebr10849214
  • (CaONFJC)MIL584446
  • (OCoLC)874321908

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