Molecular basis of drug design and resistance
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| Sprache: | English |
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Cambridge [u.a.]
Cambridge Univ. Press
1997
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| Schriftenreihe: | British Society for Parasitology: Symposia of the British Society for Parasitology
34 |
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| 245 | 1 | 0 | |a Molecular basis of drug design and resistance |c ed. by G. H. Coombs ... |
| 264 | 1 | |a Cambridge [u.a.] |b Cambridge Univ. Press |c 1997 | |
| 300 | |a VII, 151, VII S. |b Ill. | ||
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| 490 | 0 | |a Parasitology |v 114,Suppl. | |
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| 650 | 4 | |a Antiparasitic agents |v Congresses | |
| 650 | 4 | |a Antiparasitic agents |x Design |v Congresses | |
| 650 | 4 | |a Drug resistance |v Congresses | |
| 650 | 4 | |a Parasitic diseases |x Chemotherapy |v Congresses | |
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Datensatz im Suchindex
| _version_ | 1819779053015531520 |
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| adam_text | PARASITOLOGY SYMPOSIA OF THE BRITISH SOCIETY FOR PARASITOLOGY VOLUME 34
MOLECULAR BASIS OF DRUG DESIGN AND RESISTANCE EDITED BY G. H. COOMBS AND
S. L. CROFT CO-ORDINATING EDITOR L. H. CHAPPELL CAMBRIDGE UNIVERSITY
PRESS CONTENTS LIST OF CONTRIBUTIONS PREFACE THE CURRENT STATUS OF
ANTIPARASITE CHEMOTHERAPY SUMMARY INTRODUCTION CURRENT SITUATION MALARIA
TRYPANOSOMIASIS AND LEISHMANIASIS OTHER COCCIDIAN PARASITES AND
MICROSPORIDIA HELMINTHIASES (OTHER THAN HUMAN FILARIASIS) FILARIASIS
DRUG DESIGN MOLECULAR AND BIOCHEMICAL APPROACHES PHARMACOLOGICAL
APPROACHES REFERENCES VII SI S3 S3 S3 S3 S3 S7 S8 S9 S10 S10 S10 SLL S12
A STRUCTURE-BASED APPROACH TO DRUG DISCOVERY: CRYSTALLOGRAPHY AND
IMPLICATIONS FOR THE DEVELOPMENT OF ANTIPARASITE DRUGS SI7 SUMMARY S17
AN HISTORICAL INTRODUCTION SI7 CHEMISTRY SI 8 CELL AND MOLECULAR BIOLOGY
SI8 STRUCTURE DETERMINATION OF MACROMOLECULES SI9 BIOINFORMATICS AND
COMPUTATIONAL METHODS SI9 STRUCTURE-BASED DRUG DISCOVERY, THE STRATEGY
AND SOME EXAMPLES S20 ECONOMIC CONSIDERATIONS S21 CRYSTALLOGRAPHY
APPLIED TO PROTEINS FROM PARASITES S21 TRYPANOTHIONE REDUCTASE S23 FINAL
COMMENTS S26 ACKNOWLEDGEMENTS S26 REFERENCES S26 VALIDATING TARGETS FOR
ANTIPARASITE CHEMOTHERAPY S31 SUMMARY S31 INTRODUCTION S31 ENZYMES OR
RECEPTORS FOUND ONLY IN PARASITES S33 ENZYMES FOR DIHYDROPTEROATE
SYNTHESIS IN APICOMPLEXAN PARASITES S33 PYRUVATE:FERREDOXIN
OXIDOREDUCTASES IN ANAEROBIC PROTOZOAN PARASITES S34 TRYPANOTHIONE
REDUCTASE IN KINETOPLASTIDA S34 XUCLEOSIDE PHOSPHOTRANSFERASES IN
PROTOZOAN PARASITES S35 GLYCOSOMES IN AFRICAN TRYPANOSOMES S36
INDISPENSABLE ENZYMES OR RECEPTORS IN PARASITES S37 LANOSTEROL C-14A
DEMETHYLASE IN LEISHMANIA AND TRYPANOSOMA CRUZI S37 DIHYDROFOLATE
REDUCTASE-THYMIDYLATE SYNTHETASE BIFUNCTIONAL PROTEINS IN PROTOZOAN
PARASITES S37 PURINE PHOSPHORIBOSYLTRANSFERASES S38 MITOCHONDRIAL
ELECTRON TRANSPORT IN APICOMPLEXAN PARASITES S38 THE MEMBRANE CHLORIDE
ION CHANNELS IN NEMATODE AND ARTHROPOD PARASITES S39 ORNITHINE
DECARBOXYLASE IN AFRICAN TRYPANOSOMES S39 CONCLUSION S40 ACKNOWLEDGEMENT
S40 REFERENCES S40 CONTROL OF GENE EXPRESSION IN VIRUSES AND PROTOZOAN
PARASITES BY ANTISENSE OLIGONUCLEOTIDES S45 SUMMARY S45 INTRODUCTION S45
BACKGROUND TO THE DESIGN OF ANTISENSE OLIGONUCLEOTIDES S46
CHEMICALLY-MODIFIED OLIGOMERS S46 MECHANISMS RESPONSIBLE FOR ANTISENSE
EFFECTS S46 SELECTION OF A TARGET SEQUENCE S47 ANTIVIRAL APPLICATIONS
S47 ANTISENSE OLIGONUCLEOTIDES TARGETED TO PARASITE GENES S49 CELL-FREE
TRANSLATION EXPERIMENTS S49 CULTURED PARASITES S50 TARGETING THE
MINI-EXON SEQUENCE OF TRYPANOSOMATIDS WITH ANTISENSE OLIGONUCLEOTIDES
S50 CELL-FREE STUDIES S51 CULTURED PARASITES S51 TARGETING FOLDED RXA
S53 CONCLUSION S54 ACKNOWLEDGEMENTS S54 REFERENCES S54 PARASITE
PROTEINASES AND AMINO ACID METABOLISM: POSSIBILITIES FOR
CHEMOTHERAPEUTIC EXPLOITATION S61 PREAMBLE S61 PROTEINASES AS
ANTIPARASITE DRUG TARGETS: THE RATIONALE AND THE APPROACH S61
PROTEINASES OF PARASITES THAT APPEAR TO OFFER PROMISE AS DRUG TARGETS
S62 CYSTEINE PROTEINASES OF TRYPANOSOMATIDS S62 SURFACE
METALLOPROTEINASES OF TRYPANOSOMATIDS S64 PROTEINASES OF PLASMODIUM
FALCIPARUM S65 PROTEINASES OF HELMINTHS S66 RELEASED AND/OR SURFACE
ENZYMES S67 PROTEINASES INVOLVED IN INVASION BY PARASITES S69 CONFIRMING
PARASITE PROTEINASES AS GOOD DRUG TARGETS S69 TARGET VALIDATION OF
TRYPANOSOMATID CYSTEINE PROTEINASES S70 ATTEMPTS TO VALIDATE TRICHOMONAD
CYSTEINE PROTEINASES USING INHIBITORS S71 PARASITE PROTEINASES AS
ACTIVATORS OF PRO- DRUGS S71 EXPLOITING PARASITE PROTEINASES, HOW TO
PROCEED ? S72 CHEMOTHERAPEUTIC TARGETS IN AMINO ACID METABOLISM S73
SULPHUR AMINO ACID METABOLISM IN PARASITES S73 TRYPANOTHIONE S73
POLYAMINES S73 METHIONINE METABOLISM AND METHIONINE Y-LYASE S74 THE WAY
FORWARD S74 ACKNOWLEDGEMENTS S74 REFERENCES S74 THE MANNITOL CYCLE IN
EIMERIA S81 SUMMARY S81 INTRODUCTION S81 MANNITOL METABOLISM S83
REGULATION OF MANNITOL METABOLISM S83 MANNITOL METABOLISM AS A DRUG
TARGET S86 CONCLUSIONS S87 REFERENCES S87 LIPID BIOSYNTHESIS PATHWAYS AS
CHEMOTHERAPEUTIC TARGETS IN KINETOPLASTID PARASITES S91 SUMMARY S91
INTRODUCTION S91 STEROL BIOSYNTHESIS INHIBITORS S91 D0870 AND OTHER C14A
DEMETHYLASE INHIBITORS S92 J24I2.-O STERO I METHYL TRANSFERASE
INHIBITORS S94 PHOSPHOLIPID BIOSYNTHESIS INHIBITORS S96 CONCLUSIONS S96
ACKNOWLEDGEMENTS S96 REFERENCES S96 NEW APPROACHES TO LEISHMANIA
CHEMOTHERAPY: PTERIDINE REDUCTASE 1 (PTR1) AS A TARGET AND MODULATOR OF
ANTIFOLATE SENSITIVITY SI01 SUMMARY SI 01 INTRODUCTION S101 GROWTH
REQUIREMENTS FOR PTERINS AND FOLATES SI02 UPTAKE AND SALVAGE OF PTERINS
AND FOLATES SI02 MECHANISMS OF ANTIFOLATE RESISTANCE SI02 OVERPRODUCTION
OR MUTATION OF DHFR-TS SI03 H-REGION AMPLIFICATION AND THE DISCOVERY OF
PTR1 S103 ALTERATIONS IN TRANSPORT OR METABOLISM SI03 PTR1 AND PTERIDINE
METABOLISM S104 ENZYMATIC PROPERTIES OF PTR1 S104 COMPARISON OF PTR1
WITH OTHER PTERIDINE REDUCTASES SI 05 THE GROWTH REQUIREMENTS OF PTR1
MUTANTS SUGGEST A KEY ROLE IN PTERIN SALVAGE SI 06 WHAT IS THE ROLE OF
PTERINS IN LEISHMANIA} S106 PTR1 AND OXIDANT RESISTANCE S106 THE ROLE OF
PTR1 IN MODULATING MTX SENSITIVITY AND RESISTANCE SI07 PTR1 AND MTX
RESISTANCE S107 IMPLICATIONS OF PTR1 FOR ANTIFOLATE CHEMOTHERAPY SI 07
ACKNOWLEDGEMENTS SI 08 REFERENCES SI 08 TARGET SITES OF ANTHELMINTICS
SILL SUMMARY SILL INTRODUCTION SILL NICOTINIC ACETYLCHOLINE RECEPTORS SI
12 STRUCTURE OF THE NICOTINIC ACETYLCHOLINE RECEPTOR ION-CHANNEL (NACHR)
SI 13 GABA AGONIST: PIPERAZINE SI 15 AVERMECTINS SI 15 CALCIUM
PERMEABILITY: PRAZIQUANTEL SI 17 BENZIMIDAZOLES: /J-TUBULIN SI 17
STRUCTURE AND FUNCTION OF MICROTUBULES SI 18 PROTON IONOPHORES SI21
MALATE METABOLISM SI21 PHOSPHOGLYCERATE KINASE AND MUTASE INHIBITION SI
21 ARACHIDONIC ACID METABOLISM AND INNATE IMMUNITY S121 FUTURE
DEVELOPMENT OF ANTHELMINTICS SI22 ACKNOWLEDGEMENTS SI 22 REFERENCES SI
22 QUINOLINE RESISTANCE MECHANISMS IN PLASMODIUM FALCIPARUM : THE DEBATE
GOES ON SI25 SUMMARY SI 25 INTRODUCTION SI 25 CHLOROQUINE, THE DRUG SI25
MECHANISMS OF CHLOROQUINE ACTION SI26 CHLOROQUINE RESISTANCE SI26 THE
BIOCHEMICAL BASIS OF CHLOROQUINE RESISTANCE SI 27 THE MOLECULAR EVIDENCE
OF CHLOROQUINE RESISTANCE SI 30 WHAT IS THE STRUCTURAL BASIS FOR
CHLOROQUINE RESISTANCE? SI 32 WHAT FUTURE FOR THE AMINOQUINOLINES ? SI
33 REFERENCES SI 33 THE ROLE OF DRUGS IN THE CONTROL OF PARASITIC
NEMATODE INFECTIONS: MUST WE DO WITHOUT? SI37 SUMMARY SI 37 INTRODUCTION
SI 37 CONTROL OF HELMINTH INFECTIONS SI38 ANTHELMINTIC DRUGS SI38
DEVELOPMENT OF DRUG RESISTANCE SI 39 MOLECULAR MECHANISMS OF
BENZIMIDAZOLE RESISTANCE IN THE SHEEP NEMATODE H. CONTORTUS SI40 ROLE OF
MUTATIONS IN /?-TUBULIN IN BZ RESISTANCE CONCLUSIONS ACKNOWLEDGEMENTS
REFERENCES DESIGNER DRUGS: PIPE DREAMS OR REALITIES ? SUMMARY
INTRODUCTION CRITIQUE OF THE RATIONAL APPROACH TO ANTIPARASITE DRUG
DESIGN S141 S142 S142 S142 S145 S145 S145 S145 IT REQUIRES MASSIVE
INITIAL INVESTMENT OF RESOURCES BEFORE THE PROCESS CAN BEGIN SI46 TO
DATE, TOO FEW POTENTIAL TARGETS IN PARASITES HAVE BEEN PROPERLY
VALIDATED FOR THE APPROACH TO BE JUSTIFIED SI47 NO REGISTERED
ANTIPARASITE DRUG HAS BEEN DESIGNED TOTALLY RATIONALLY SI47 APPROPRIATE
CHARACTERISTICS OF ABSORPTION, DISTRIBUTION, METABOLISM AND EXCRETION
(ADME) CANNOT BE DESIGNED TOTALLY RATIONALLY S147 IT DOES NOT ALLOW
EXPLOITATION OF ALL POTENTIAL MECHANISMS OF SELECTIVE TOXICITY SI47 IT
MAY REQUIRE ONLY LIMITED CHEMICAL SYNTHESIS AND BIOLOGICAL TESTING, BUT
THE COST SAVINGS HERE ARE OFFSET BY HIGH EXPENDITURE ON PHYSICAL
SCIENCES SI48 IT WILL BE OVERTAKEN BY THE COMBINATORIAL CHEMISTRY
REVOLUTION SI48 THIS DEBATE IS ACADEMIC, AS THERE ARE NO PHARMACEUTICAL
COMPANIES LEFT IN THE ANTIPARASITE DRUG DEVELOPMENT BUSINESS SI50
CONCLUSIONS SI 50 ACKNOWLEDGEMENTS S151 REFERENCES SI 51
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| id | DE-604.BV012160945 |
| illustrated | Illustrated |
| indexdate | 2024-12-23T14:57:19Z |
| institution | BVB |
| isbn | 0521626692 |
| language | English |
| oai_aleph_id | oai:aleph.bib-bvb.de:BVB01-008237653 |
| oclc_num | 37799160 |
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| physical | VII, 151, VII S. Ill. |
| publishDate | 1997 |
| publishDateSearch | 1997 |
| publishDateSort | 1997 |
| publisher | Cambridge Univ. Press |
| record_format | marc |
| series | British Society for Parasitology: Symposia of the British Society for Parasitology |
| series2 | British Society for Parasitology: Symposia of the British Society for Parasitology Parasitology |
| spellingShingle | Molecular basis of drug design and resistance British Society for Parasitology: Symposia of the British Society for Parasitology Antiparasitic agents Congresses Antiparasitic agents Design Congresses Drug resistance Congresses Parasitic diseases Chemotherapy Congresses |
| subject_GND | (DE-588)1071861417 |
| title | Molecular basis of drug design and resistance |
| title_auth | Molecular basis of drug design and resistance |
| title_exact_search | Molecular basis of drug design and resistance |
| title_full | Molecular basis of drug design and resistance ed. by G. H. Coombs ... |
| title_fullStr | Molecular basis of drug design and resistance ed. by G. H. Coombs ... |
| title_full_unstemmed | Molecular basis of drug design and resistance ed. by G. H. Coombs ... |
| title_short | Molecular basis of drug design and resistance |
| title_sort | molecular basis of drug design and resistance |
| topic | Antiparasitic agents Congresses Antiparasitic agents Design Congresses Drug resistance Congresses Parasitic diseases Chemotherapy Congresses |
| topic_facet | Antiparasitic agents Congresses Antiparasitic agents Design Congresses Drug resistance Congresses Parasitic diseases Chemotherapy Congresses Konferenzschrift |
| url | http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=008237653&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
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