Content: Virus-receptor interactions / Bernard N. Fields and Mark I. Greene --
Design of peptide superagonists and antagonists : conformational and dynamic considerations / Victor J. Hruby --
Localization and synthesis of protein antigenic sites : use of free synthetic peptides for the preparation of antibodies and T-cells of preselected specificities / M. Zouhair Atassi --
Studies on new microbial secondary metabolites with potential usefulness : antibiotics, enzyme inhibitors, and immunomodifiers / Hamao Umezawa --
Conformation of nucleic acids and their interactions with drugs / Andrew H.-J. Wang --
Substrate analog inhibitors of highly specific proteases / James Burton --
Structure-behavioral activity relationships of peptides derived from ACTH : some stereochemical considerations / J.W. Van Nispen and H.M. Greven --
Design of novel cyclic hexapeptide somatostatin analogs from a model of the bioactive conformation / Roger M. Freidinger and Daniel F. Veber --
Design of kinase inhibitors : conformational and mechanistic considerations / George L. Kenyon and Rebecca E. Reddick --
Design and discovery of aspartyl protease inhibitors : mechanistic and clinical implications / Daniel H. Rich, Francesco G. Salituro, Mark W. Holladay, and Paul G. Schmidt --
Design of peptide analogs : theoretical simulation of conformation, energetics, and dynamics / R.S. Struthers, A.T. Hagler, and J. Rivier.
Author(s): Julius A. Vida and Maxwell Gordon (Eds.)
Series: ACS Symposium Series 251
Publisher: American Chemical Society
Year: 1984
Language: English
Pages: 268
City: Washington, D.C
Title Page......Page 1
Half Title Page......Page 3
Copyright......Page 4
ACS Symposium Series......Page 5
FOREWORD......Page 6
PdftkEmptyString......Page 0
PREFACE......Page 7
1 Virus-Receptor Interactions......Page 9
Hemagglutinin topography......Page 10
Monoclonal anti-idiotypes resemble ligand......Page 13
Literature Cited......Page 15
2 Design of Peptide Superagonists and Antagonists Conformational and Dynamic Considerations......Page 16
Development of Conformationally Constrained α-Melanotropin Superagonists......Page 18
Development of Cyclic Enkephalin Analogs with High Receptor Specificity......Page 21
Development of Conformationally Constrained Oxytocin Antagonists with Prolonged in Vivo Activities......Page 25
Development of α-Melanotropin Analogs with Prolonged In Vitro and In Vivo Biological Activities......Page 27
Literature Cited......Page 31
3 Localization and Synthesis of Protein Antigenic Sites Use of Free Synthetic Peptides for the Preparation of Antibodies and T-Cells of Preselected Specificities......Page 35
Introduction......Page 36
a. General Chemical Strategy......Page 37
b. Comprehensive Synthetic Approach for Continuous Antigenic Sites......Page 38
Comparative Analysis of Protein Antigenic Structures......Page 39
Comments on attempts to predict location of protein antigenic sites.......Page 50
Regions outside the Antigenic Sites......Page 52
Antibodies were preselected submolecu!ar specificities evoked by immunization with FREE peptides......Page 57
Other parameters of antibody response to free peptides.......Page 61
Production of monoclonal antibodies with preselected specificities......Page 62
(a) Monoclonal antibodies against the antigenic sites......Page 63
Remarks on antibody production by free small peptides......Page 65
Preparation of T-lymphocyte lines and clones with specificities to preselected protein sites.......Page 68
Induction of tolerance to preselected protein antigenic sites by free synthetic peptides......Page 69
Literature Cited......Page 74
Studies on Antimicrobial Antibiotics: Kanamycin and Derivatives of Aminoglycoside Antibiotics......Page 78
Studies on Antitumor Antibiotics, Their Derivatives and Analogs......Page 82
Low Molecular Weight Enzyme Inhibitors - Microbial Secondary Metabolites with Various Pharmacological Activity......Page 95
Low Molecular Weight Immunomodifiers......Page 97
Conclusion......Page 103
Literature Cited......Page 104
5 Conformation of Nucleic Acids and Their Interactions with Drugs......Page 109
Right-handed DNA Conformation......Page 110
A Modified A-DNA Conformation......Page 112
Conformation of a DNA-RNA Hybrid......Page 114
Lattice Interactions......Page 115
Left-Handed Z-DNA......Page 119
Methylation of Cytosine Stabilizes Z-DNA......Page 122
Adenine-Thymine Base Pairs in Z-DNA......Page 124
The Double Helix Changes Conformation Upon Intercalation......Page 127
Interaction between Daunomycin and DNA......Page 128
Specificity of Drugs through Anchoring Function......Page 132
Triostin A can Bis-intercalate into DNA......Page 134
Conclusion......Page 137
Literature Cited......Page 138
6 Substrate Analog Inhibitors of Highly Specific Proteases......Page 141
Renin......Page 142
IgA1 Protease......Page 146
Literature Cited......Page 153
7 Structure-Behavioral Activity Relationships of Peptides Derived from ACTH Some Stereochemical Considerations......Page 156
Strategy and results of the structure-behavioural activity studies......Page 157
Biological and physico-chemical properties of ACTH-(4-10) and Org 2766......Page 161
Suggestion for conformation at the receptor site for pole-jumping activity......Page 165
Literature Cited......Page 167
8 Design of Novel Cyclic Hexapeptide Somatostatin Analogs from a Model of the Bioactive Conformation......Page 171
Conformational Approach to Peptide Analog Design......Page 172
Retro Peptides......Page 174
Nα-Methyl Lysine Somatostatin Analogs......Page 182
Literature Cited......Page 187
9 Design of Kinase Inhibitors Conformational and Mechanistic Considerations......Page 190
ATP: The Common Substrate......Page 191
Nucleic Acids As Cosubstrates......Page 197
Proteins and Other Polypeptides as Cosubstrate......Page 198
Small Molecules as Cosubstrates......Page 199
Affinity Labeling of Creatine Kinase: Rationale for the Design of Epoxycreatine......Page 201
Literature Cited......Page 206
10 Design and Discovery of Aspartyl Protease Inhibitors Mechanistic and Clinical Implications......Page 211
Is Pepstatin a Transition-State Analog Inhibitor?......Page 214
Statine is an Analog of a Dipeptide......Page 218
Specificity......Page 224
Other Types of Inhibitors of Aspartyl Proteases......Page 229
The Catalytic Mechanism of Aspartyl Proteases......Page 230
Literature Cited......Page 235
11 Design of Peptide Analogs Theoretical Simulation of Conformation, Energetics, and Dynamics......Page 238
CALCULATION OF PEPTIDE CONFORMATION......Page 240
ANALOG DESIGN......Page 252
Literature Cited......Page 258
Author Index......Page 261
A......Page 262
C......Page 263
G......Page 264
L......Page 265
P......Page 266
S......Page 267
V......Page 268
