Limited Offer
Protein Prenylation, Part B
- 1st Edition, Volume 30 - November 8, 2011
- Editors: Christine Hrycyna, Martin Bergo, Fuyuhiko Tamanoi
- Language: English
- Hardback ISBN:9 7 8 - 0 - 1 2 - 4 1 5 9 2 2 - 8
- eBook ISBN:9 7 8 - 0 - 1 2 - 4 1 5 9 6 4 - 8
This volume of The Enzymes features high-caliber thematic articles on the topic of glycosylphosphatidylinositol (GPI) anchoring of protei… Read more
Purchase options
Institutional subscription on ScienceDirect
Request a sales quote- Contributions from leading authorities
- Informs and updates on all the latest developments in the field
Preface
The Enzymology of CAAX Protein Prenylation
I. Abstract
II. Introduction
III. Protein FTase
IV. Protein GGTase-I
V. Conclusions
Acknowledgments
CAAX Processing and Yeast a-Factor Biogenesis
I. Abstract
II. Introduction
III. The a-Factor Mating Pheromone of S. cerevisiae as an Early Prototype for Dissecting the CAAX-Processing Pathway
IV. Biogenesis Pathway of a-Factor: Genetic and Biochemical Analysis of the a-Factor Machinery
V. Progeria—The Role of Prenylation and ZMPSTE24 in Progeroid Disorders
VI. A Prenylated, Secreted Molecule Involved in Drosophila Germ Cell Migration Requires a Pathway Strikingly Similar to That of a-Factor Biogenesis
Acknowledgments
Prenylation and Phosphorylation of Ras Superfamily Small GTPases
I. Abstract
II. Introduction
III. Small GTPase Prenylation
IV. C-Terminal Phosphorylation of Prenylated Ras Family Small GTPases
V. C-Terminal Phosphorylation of Prenylated Rho Family Small GTPases
VI. C-Terminal Phosphorylation of Prenylated Rab Family Small GTPases
VII. Conclusions
Acknowledgments
Biochemical and Biological Functions of Isoprenylcysteine Carboxyl Methyltransferase
I. Abstract
II. Introduction
III. Icmt: Structure and Biological Function
IV. ICMT Substrate Specificity
V. Effect of Methylation by Icmt on Substrate Function: In Vitro Studies
VI. ICMT Effect on Substrate Function: In Vivo Studies
VII. Conclusions
Chemical Probes of Protein Prenylation
I. Abstract
II. Introduction
III. Prenyl Analogs as FTase Inhibitors (FTIs)
IV. Prenyl Analogs as Mechanistic and Structural Probes
V. Substrate Specificity Studies
VI. Prenyl Proteomics Studies
VII. Future Directions
Geranylgeranyltransferase-1 Inhibitors
I. Abstract
II. Introduction
III. Biochemistry of Protein Prenylation
IV. Validation of GGT-1 as a Target in a Genetic Mouse Model
V. Design of CaaX Peptidomimetics as PTIs and Identification of PTIs from High-Throughput Screens (HTS)
VI. FTIs as Anticancer Drugs
VII. GGTI Effects in Cultured Cells and In Vivo
VIII. GGTIs in the Clinic
IX. The Use of PTIs in Other Diseases
X. Future Directions and Challenges
Acknowledgments
Small-Molecule Inhibitors of GGTase-I from the Heterocycle Library Derived from Phosphine Catalysis
I. Abstract
II. Introduction
III. Phosphine Catalysis-Based Chemical Compound Library and Identification of Initial GGTI Compounds P3-E5 and P5-H6
IV. Cell Active Compound P61-A6
V. Tumor Growth Inhibition by P61-A6
VI. Long Plasma Half Life of P61-A6 and Pharmacokinetic Parameters
VII. Identification of Dual Specificity Inhibitors of GGTase-I and RabGGTase
VIII. Identification of Specific Inhibitors of RabGGTase from the Library
IX. Conclusion and Future Prospects
Acknowledgment
Inhibition of Rab Prenylation
I. Abstract
II. Introduction
III. RabGGTase Inhibitors
IV. Summary and Outlook
Inhibitors of Postprenylation CAAX Processing Enzymes
I. Abstract
II. Introduction
III. Inhibitors of Rce1
IV. Inhibitors of Icmt
V. Conclusion
The Ras Converting Enzyme (Rce1p)
I. Abstract
II. Introduction
III. Identification of Rce1p and Its Orthologs
IV. The Basis for Rce1p as a Therapeutic Target for Disease
V. Rce1p and Ste24p Have Different Target Specificities
VI. The Recognition of Specific CaaX Motifs is Influenced by Protein Context
VII. Rce1p Influences the Localization of Some But Not All of Its Targets
VIII. Rce1p Inhibitors Can Be Assay Independent and Assay Dependent
IX. Structural Chemistry and Proposed Mechanism
X. Conclusions and Future Directions
Acknowledgments
Cysmethynil, a Specific Small-Molecule Inhibitor of Isoprenylcysteine Carboxylmethyl Transferase (Icmt)
I. Abstract
II. Prenylation Process
III. Rationale for Targeting Icmt
IV. Icmt and Its Functional Importance in Biology
V. Development of Icmt Inhibitors
VI. Cysmethynil, a Nonstructure Analog Small-Molecule Inhibitor of Icmt
VII. Inhibition of Icmt by Cysmethynil Induces Autophagy and Cell Death, Potential for Cancer Therapy
VIII. Cysmethynil Inhibition of Icmt Results in Reduction of Rho-Mediated Cell Migration, Suggesting a Potential Role in Cancer Metastasis
IX. Current and Future Work to Identify Better Icmt Inhibitors Through Medicinal Chemistry
The Isoprenoid Biosynthetic Pathway and Statins
I. Abstract
II. The Isoprenoid Biosynthetic Pathway
III. Statins
IV. Statins and the IBP
V. Future Directions
Inhibition of Farnesyl and Geranylgeranyl Diphosphate Synthases
I. Abstract
II. The Isoprenoid Biosynthetic Pathway
III. Nitrogenous Bisphosphonates
IV. GGDPS Inhibitors
V. Future Directions
- No. of pages: 372
- Language: English
- Edition: 1
- Volume: 30
- Published: November 8, 2011
- Imprint: Academic Press
- Hardback ISBN: 9780124159228
- eBook ISBN: 9780124159648
CH
Christine Hrycyna
MB
Martin Bergo
FT