Frontiers in Medicinal Chemistry

Volume 3

by

Atta-ur-Rahman , Allen B. Reitz

DOI: 10.2174/97816080520661060301
eISBN: 978-1-60805-206-6, 2006
ISBN: 978-1-60805-674-3
ISSN: 1567-2042

  
  


Indexed in: Scopus

Frontiers in Medicinal Chemistry is a book series devoted to the review of area...[view complete introduction]
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Table of Contents

Editorial , Pp. iv- (1)

Allen B. Reitz, Cheryl P. Kordik, Atta-Ur-Rahman and M. Iqbal Chouhary

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Contributors , Pp. ix-xiv (6)

Atta-ur-Rahman and Allen B. Reitz

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Structure and Function of HIV-1 Integrase: An Update , Pp. 3-22 (20)

Thang K. Chiu and David R. Davies

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Anti-HIV Drugs and Resistance: Inhibitors of HIV-1 Reverse Transcriptase and Protease , Pp. 23-44 (22)

Tomozumi Imamichi

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Gene Therapy for Cardiovascular Diseases , Pp. 59-85 (27)

Marcin Gruchala, Himadri Roy, Shalini Bhardwaj and Seppo Yla-Herttuala

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Drug Development and the Importance of Ethnicity: Lessons from Heart Failure Management and Implications for Hypertension , Pp. 45-58 (14)

Michael D. Sosin, Gurbir S. Bhatia, Gregory Y.H. Lip and Russell C. Davis

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Design and Discovery of Novel Antihypertensive Drugs Through Conformation and Bioactivity Studies , Pp. 87-111 (25)

Thomas M. Mavromoustakos, Maria V. Zervou and Panagiotis G. Zoumpoulakis

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Novel Antiarrhythmic Compounds with Combined Class IB and Class III Mode of Action , Pp. 113-124 (12)

Peter Matyus, Ildiko Varga, Tivadar Rettegi, Antal Simay, Peter Kovacs, Laszlo Karolyhazy, Akos Kocsis, Szilvia Vajda and Andras Va

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A1 Adenosine Receptor Agonists: Medicinal Chemistry and Therapeutic Potential , Pp. 125-151 (27)

Sally A. Hutchinson and Peter J. Scammells

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Are the Extracellular Pathways a Conduit for the Delivery of Therapeutics to the Brain? , Pp. 153-161 (9)

William A. Banks

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A Review of Neuroprotective Agents , Pp. 163-194 (32)

Margaret A. Brimble and Mark S. Levi

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Design of Ligands for the Nicotinic Acetylcholine Receptors: The Quest for Selectivity , Pp. 195-247 (53)

William H. Bunnelle, Michael J. Dart and Michael R. Schrimpf

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New Trends in the Design of Drugs Against Alzheimer's Disease , Pp. 249-284 (36)



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Development of Melanocortin Receptor Selective Ligands , Pp. 285-334 (50)

Boman G. Irani, Jerry R. Holder, Aleksandar Todorovic, Andrzej M. Wilczynski, Christine G. Joseph, Krista R. Wilson and Carrie Hask

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Inhibition of Protein Tyrosine Phosphatase 1B for the Treatment of Diabetes and Obesity , Pp. 335-368 (34)

Zhonghua Pei, Gang Liu, Thomas H. Lubben and Bruce G. Szczepankiewicz

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The Impact of Infection on the Incidence of Autoimmune Disease , Pp. 369-382 (14)

Thomas D.C. Thomas, Paola Zaccone, David W. Dunne and Anne Cooke

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Transcription Factors in Autoimmune Diseases , Pp. 383-397 (15)

Martin Eggert, Andreas Kluter, Uwe K. Zettl and Gunther Neeck

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Small Molecule FLT3 Tyrosine Kinase Inhibitors , Pp. 399-416 (18)

Mark Levis and Donald Small

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Potentiality and Limitations of a Strategy for the Control of Cell Proliferation: The Block of Ca2+ Entry , Pp. 417-433 (17)

Luca Munaron, Susanna Antoniotti, Alessandra Fiorio Pla and Davide Lovisolo

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An Expanding Appreciation of the Role Chemokine Receptors Play in Cancer Progression , Pp. 435-454 (20)

O. M. Zack Howard and Carole L. Galligan

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Structural Bioinformatics and its Impact to Biomedical Science and Drug Discovery , Pp. 455-502 (48)

Kuo-Chen Chou

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Recent Advances in Chemical Genomics , Pp. 503-550 (48)

Gyorgy Dorman, Peter Krajcsi, Laszlo G. Puskas, Zoltan Kovari, Zsolt Lorincz, Laszlo Urge and Ferenc Darvas

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Predicting Molecular Interactions In Silico: I. An Updated Guide to Pharmacophore Identification and its Applications to Drug Design , Pp. 551-584 (34)

Oranit Dror, Alexandra Shulman-Peleg, Ruth Nussinov and Haim J. Wolfson

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In Silico Methods for Predicting Ligand Binding Determinants of Cytochromes P450 , Pp. 615-652 (38)

Marcel J. de Groot, Stewart B. Kirton and Michael J. Sutcliffe

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Trends in Hit-to-Lead: An Update , Pp. 653-673 (21)

Benoit Deprez and Rebecca Deprez-Poulain

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Recent Development and Application of Virtual Screening in Drug Discovery: An Overview , Pp. 675-703 (29)

Tingjun Hou and Xiaojie Xu

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Biology of Heme in Health and Disease , Pp. 705-714 (10)

Nastiti Wijayanti and Stephan Immenschuh

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Preface

Frontiers in Medicinal Chemistry, Vol. 3 continues the tradition of the two previous volumes in providing a comprehensive selection of manuscripts involving diverse therapeutic areas as well as a section on important enabling technologies. Although the topics covered were selected from the Bentham journals "Current Medicinal Chemistry", "Current Topics in Medicinal Chemistry" and "Current Pharmaceutical Design", each of the authors has had the opportunity to update their original contributions with additional information or commentary, and many have chosen to do so. Therefore, there is a substantial amount of new material in these reviews that has not been published previously.

This volume contains 26 chapters arranged in eight sections. The first section covers the area of Infectious Diseases with manuscripts on HIV-1 integrase and drug resistance mediated by HIV-1 reverse transcriptase and HIV protease inhibitors. The next section is on Cardiovascular Diseases which addresses ethnicity in heart failure management and hypertension, gene therapy, novel antihypertensive agents, combined Class IB and Class III antiarrhythmics, and the adenosine A1 receptor. The section on Central Nervous System Disorders then starts with a review on extracellular transport into the CNS which is a nontraditional approach to the delivery of useful therapeutics across the blood brain barrier. This is followed by articles that review neuroprotective agents, the nicotinic acetylcholine receptor and Alzheimer's disease. The Endocrine and Metabolic Disorders section highlights melanocortin receptors and protein tyrosine phosphatase 1B inhibitors for diabetes and obesity. The Immunology section addresses autoimmune disease and transcription regulators. In the Oncology section are found manuscripts on FLT3 tyrosine kinase inhibitors, Ca2+ channel blockade, and chemokine receptors. The Enabling Technologies section is the longest one with seven manuscripts, reflecting the importance of new approaches to conduct modern drug discovery and medicinal chemistry research. The topics covered include bioinformatics, chemical genomics, trends in hit-to-lead work, virtual screening, and computational approaches to pharmacophore identification, protein-protein and protein-drug interactions, and cytochrome P450s. Finally, the biology of the heme protein in health and disease is reviewed as well.

We thank the authors, who contributed to this volume, and congratulate them for the high quality of their work. We also thank Bentham for sponsoring this book series. We expect that Frontiers in Medicinal Chemistry will continue to be published on an annual basis with timely and helpful reviews in areas of keen interest to practicing medicinal chemists throughout the world.

ALLEN B. REITZ
Johnson & Johnson
USA

CHERYL P. KORDIK
Johnson & Johnson
USA

ATTA-UR-RAHMAN
Higher Education Commission
International Center for Chemical Sciences
Pakistan

M. IQBAL CHOUDHARY
International Center for Chemical Sciences
Pakistan

List of Contributors

Co-Editor(s):
Atta-ur-Rahman
H.E.J. Research Institute of Chemistry
University of Karachi
Karachi, 75270
Pakistan


Allen B. Reitz
Johnson & Johnson Pharmaceutical Research and Development, Spring House
Pennsylvania , 19477
USA




Associate Editor(s):
M. Iqbal Choudhary
H.E.J. Research Institute of Chemistry
University of Karachi
Karachi, 75270
Pakistan


Cheryl P. Kordik
Johnson & Johnson Pharmaceutical Research and Development, Spring House
Pennsylvania , 19477
USA




Editorial Advisory Board:
P.R. Bernstein
University of Delaware
Newark
DE
USA


C. Bor-Luen
National Taiwan University, Taipei
Taiwan
R.O.C.


R. Efremov
M.M. Shemyakin & Yu.A. Ovchinnikov Institute of Bioorganic Chemistry
Moscow
Russia


C. Garcia-Echeverria
Sanofi-Aventis
Paris
France


D. Hadjipavlou-Litina
Arristotle Universith of Thessaloniki
Thessaloniki
Greece


D. Heymann
University of Nantes
Nantes
France


D.A. Jans
Nuclear Signaling Laboratory, Monash University
Australia


G.B. Mahady
University of Illinois at Chicago
Chicago
IL
USA


B. Malawska
Jagiellonian University Collegium Medicum
Kraków
Poland


C. Philippe
Sciences and Technologies University of Lille
Lille
France




Contributor(s):
Thang K. Chiu
NIH, NIDDK, Laboratory of Molecular Biology
Building 5, Room 338
Bethesda
MD , 20892-0560
USA


David R. Davies
NIH, NIDDK, Laboratory of Molecular Biology
Building 5, Room 338
Bethesda
MD , 20892-0560
USA


Tomozumi Imamichi
Laboratory of Human Retrovirology, Applied and Development Research Program
Science Applications International Corporation-Frederick, Inc., National Institute of Allergy and Infectious Diseases at Frederick
P.O. Box B, Building 550, Room 126
Frederick
MD, 21702
USA


Michael D. Sosin
University Department of Medicine
Sandwell & West Birmingham Hospitals NHS Trust, City Hospital
Birmingham , B18 7QH
UK


Gurbir S. Bhatia
University Department of Medicine
Sandwell & West Birmingham Hospitals NHS Trust, City Hospital
Birmingham , B18 7QH
UK


Gregory Y.H. Lip
University Department of Medicine
Sandwell & West Birmingham Hospitals NHS Trust, City Hospital
Birmingham , B18 7QH
UK


Russell C. Davis
University Department of Medicine
Sandwell & West Birmingham Hospitals NHS Trust, City Hospital
Birmingham , B18 7QH
UK


Marcin Gruchala
Department of Biotechnology and Molecular Medicine, First Department of Cardiology
A.I. Virtanen Institute for Molecular Sciences, University of Kuopio
Medical University of Gdansk
Finland
Poland


Himadri Roy
Department of Biotechnology and Molecular Medicine
A.I. Virtanen Institute for Molecular Sciences
University of Kuopio
Finland


Shalini Bhardwaj
Department of Biotechnology and Molecular Medicine
A.I. Virtanen Institute for Molecular Sciences
University of Kuopio
Finland


Seppo Ylä-Herttuala
Department of Biotechnology and Molecular Medicine, Department of Medicine, University of Kuopio
A.I. Virtanen Institute for Molecular Sciences, University of Kuopio, University of Kuopio
Kuopio University Hospital
Finland


Thomas M. Mavromoustakos
National Hellenic Research Foundation
Institute of Organic and Pharmaceutical Chemistry
Vas. Constantinou 48
Athens , 11635
Greece


Maria V. Zervou
National Hellenic Research Foundation
Institute of Organic and Pharmaceutical Chemistry
Vas. Constantinou 48
Athens , 11635
Greece


Panagiotis G. Zoumpoulakis
National Hellenic Research Foundation
Institute of Organic and Pharmaceutical Chemistry
Vas. Constantinou 48
Athens , 11635
Greece


Péter Mátyus
Department of Organic Chemistry
Semmelweis University
Budapest
Hungary


Ildikó Varga
Ivax Drug Research Institute
Budapest
Hungary


Tivadar Rettegi
Ivax Drug Research Institute
Budapest
Hungary


Antal Simay
Ivax Drug Research Institute
Budapest
Hungary


Péter Kovács
Department of Organic Chemistry
Semmelweis University
Budapest
Hungary


László Károlyházy
Department of Organic Chemistry
Semmelweis University
Budapest
Hungary


Ákos Kocsis
Department of Organic Chemistry
Semmelweis University
Budapest
Hungary


Szilvia Vajda
Department of Pharmacology and Pharmacotherapy
University of Szeged
Szeged
Hungary


András Varró
Department of Pharmacology and Pharmacotherapy
University of Szeged
Szeged
Hungary


István Pénzes
Department of Anesthesiology and Intensive Therapy
Budapest
Hungary


Julius Gy. Papp
Department of Pharmacology and Pharmacotherapy, Division of Cardiovascular Pharmacology
University of Szeged, Hungarian Academy of Sciences
Szeged
Hungary


Sally A. Hutchinson
CSIRO Textile and Fibre Technology
Henry St, Belmont VIC
Oregon, 3216
Australia


Peter J. Scammells
Department of Medicinal Chemistry
Victorian College of Pharmacy, Monash University
381 Royal Parade, Parkville VIC
London, 3052
Australia


William A. Banks
Department of Internal Medicine
GRECC, Veterans Affairs Medical Center-St. Louis and Saint Louis University School of Medicine
Division of Geriatrics, 915 N. Grand Blvd., St. Louis
London
MO , 63106
USA


Margaret A. Brimble
Department of Chemistry
University of Auckland
23 Symonds St.
Auckland
New Zealand


Mark S. Levi
Department of Pharmacology & Toxicology
University of Arkansas for Medical Sciences
4301 W. Markham St.
Little Rock
AR , 72205
USA


William H. Bunnelle
Abbott Laboratories Global Pharmaceutical Research and Development
Department R47W, AP9A-1, Abbott Park
Illinois , 60064
USA


Michael J. Dart
Abbott Laboratories Global Pharmaceutical Research and Development
Department R47W, AP9A-1, Abbott Park
Illinois , 60064
USA


Michael R. Schrimpf
Abbott Laboratories Global Pharmaceutical Research and Development
Department R47W, AP9A-1, Abbott Park
Illinois , 60064
USA


Pierre Francotte
Natural and Synthetic Drugs Research Center, Dept of Medicinal Chemistry
University of Liège
Av. de l'Hôpital, 1, B36
Liège, 4000
Belgium


Pascal de Tullio
Natural and Synthetic Drugs Research Center, Dept of Medicinal Chemistry
University of Liège
Av. de l'Hôpital, 1, B36
Liège, 4000
Belgium


Pierre Fraikin
Natural and Synthetic Drugs Research Center, Dept of Medicinal Chemistry
University of Liège
Av. de l'Hôpital, 1, B36
Liège, 4000
Belgium


Bernard Pirotte
Natural and Synthetic Drugs Research Center, Dept of Medicinal Chemistry
University of Liège
Av. de l'Hôpital, 1, B36
Liège, 4000
Belgium


Boman G. Irani
Department of Medicinal Chemistry
University of Florida
PO Box 100485
Gainesville
FL, 32610-0485
USA


Jerry R. Holder
Department of Medicinal Chemistry
University of Florida
PO Box 100485
Gainesville
FL, 32610-0485
USA


Aleksandar Todorovic
University of Florida, Department of Medicinal Chemistry
PO Box 100485
Gainesville
FL, 32610-0485
USA


Andrzej M. Wilczynski
Department of Medicinal Chemistry
University of Florida
PO Box 100485
Gainesville
FL, 32610-0485
USA


Christine G. Joseph
Department of Medicinal Chemistry
University of Florida
PO Box 100485
Gainesville
FL, 32610-0485
USA


Krista R. Wilson
Department of Medicinal Chemistry
University of Florida
PO Box 100485
Gainesville
FL, 32610-0485
USA


Carrie Haskell-Luevano
Department of Medicinal Chemistry
University of Florida
PO Box 100485
Gainesville
FL, 32610-0485
USA


Zhonghua Pei
Metabolic Disease Research
Global Pharmaceutical Research and Development
Abbott Laboratories
Abbott Park
IL , 60064
USA


Gang Liu
Metabolic Disease Research
Global Pharmaceutical Research and Development
Abbott Laboratories
Abbott Park
IL , 60064
USA


Thomas H. Lubben
Metabolic Disease Research
Global Pharmaceutical Research and Development
Abbott Laboratories
Abbott Park
IL , 60064
USA


Bruce G. Szczepankiewicz
Metabolic Disease Research
Global Pharmaceutical Research and Development
Abbott Laboratories
Abbott Park
IL , 60064
USA


Thomas D.C. Thomas
Department of Pathology
University of Cambridge
UK


Paola Zaccone
Department of Pathology
University of Cambridge
UK


David W. Dunne
Department of Pathology
University of Cambridge
UK


Anne Cooke
Department of Pathology
University of Cambridge
UK


Martin Eggert
Department of Internal Medicine and Center of Rheumatology
Rostock Clinic South, Südring 81
Rostock, D-18059
Germany


Andreas Klüter
Department of Internal Medicine and Center of Rheumatology
Rostock Clinic South, Südring 81
Rostock, D-18059
Germany


Uwe K. Zettl
Department of Neurology
University of Rostock
Gehlsheimer Str. 20
Rostock, D- 18147
Germany


Gunther Neeck
Department of Internal Medicine and Center of Rheumatology
Rostock Clinic South, Südring 81
Rostock, D-18059
Germany


Mark Levis
Johns Hopkins University School of Medicine, Department of Oncology
Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, Bunting-Blaustein Cancer Research Building
Room 251, 1650 Orleans Street, Baltimore
Maryland , 21231-1000
USA


Donald Small
Johns Hopkins University School of Medicine, Departments of Oncology and Pediatrics
Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, Bunting-Blaustein Cancer Research Building
Room 251, 1650 Orleans Street, Baltimore
Maryland , 21231-1000
USA


Luca Munaron
Department of Animal and Human Biology
University of Torino,, Nanostructured Interfaces and Surfaces Centre of Excellence (NIS)
Via Accademia Albertina 13
Torino, I-10123
Italy


Susanna Antoniotti
Department of Animal and Human Biology
University of Torino
Via Accademia Albertina 13
Torino, I-10123
Italy


Alessandra Fiorio Pla
Department of Animal and Human Biology
University of Torino
Via Accademia Albertina 13
Torino, I-10123
Italy


Davide Lovisolo
Department of Animal and Human Biology
University of Torino,, Nanostructured Interfaces and Surfaces Centre of Excellence (NIS)
Via Accademia Albertina 13
Torino, I-10123
Italy


O.M. Zack Howard
Center for Cancer Research (CCR), Laboratory of Molecular Immunoregulation (LMI)
Carole L. Galligan National Cancer Institute (NCI)
NCI-Frederick, P.O. Box B
Frederick
MD , 21702
USA


Kuo-Chen Chou
Gordon Life Science Laboratory
Shanghai Jiaotong University
13784 Torrey Del Mar,
California , 92130
USA


György Dormán
ComGenex
H-1031 Budapest, Záhony u 7.
Hungary


Péter Krajcsi
Cooperative Research Center
Solvo Biotechnology, Gyar u. 2, Semmelweis University
P.O. Box 131, Budapest H-1367
Budaörs, H-2040
Hungary


László G. Puskás
Laboratory of Functional Genomics, Biological Research Center
Hungarian Academy of Sciences
P.O. Box 521
Szeged, H-6701
Hungary


Zoltán Kovári
Gedeon Richter, Ltd., Department of Computer Assisted Drug Discovery
P.O. Box 27
Budapest, H- 1475
Hungary


Zsolt Lo"rincz
RecomGenex, Hungarian Academy of Sciences
Institute of Enzymology, Biological Research Center
Záhony u 7
Budapest, H-1031
Hungary


László Ürge
ComGenex
Záhony u 7.
Budapest, H-1031
Hungary


Ferenc Darvas
ComGenex
Záhony u 7.
Budapest, H-1031
Hungary


Oranit Dror
School of Computer Science, Tel Aviv University
Tel Aviv, 69978
Israel


Alexandra Shulman-Peleg
School of Computer Science, Tel Aviv University
Tel Aviv, 69978
Israel


Ruth Nussinov
Department of Human Genetics and Molecular Medicine
Sackler Faculty of Medicine, Tel Aviv University
NCI - Frederick, Bldg 469, Rm 151
Tel Aviv
MD , 69978
Israel


Haim J. Wolfson
School of Computer Science, Tel Aviv University
Tel Aviv, 69978
Israel


Dina Schneidman-Duhovny
School of Computer Science, Tel Aviv University
Tel Aviv, 69978
Israel


Ruth Nussinov
Department of Human Genetics and Molecular Medicine
Sackler Faculty of Medicine, Tel Aviv University
Tel Aviv
MD , 69978
Israel


Haim J. Wolfson
School of Computer Science, Tel Aviv University
Tel Aviv, 69978
Israel


Marcel J. de Groot
Department of Discovery Chemistry
, Pfizer Global Research & Development, Sandwich Laboratories
Kent CT13 9NJ
United Kingdom


Stewart B. Kirton
Department of Chemistry
University of Leicester
Leicester, LE1 7RH
UK


Michael J. Sutcliffe
Department of Chemistry, Department of Biochemistry
University of Leicester
Leicester, LE1 7RH
UK


Benoit Deprez
Faculté des Sciences Pharmaceutiques et Biologiques
Institut Pasteur de Lille, Université de Lille 2
3 rue du Pr Calmette
Lille Cedex, F-59006
France


Rebecca Deprez-Poulain
Faculté des Sciences Pharmaceutiques et Biologiques
Institut Pasteur de Lille, Université de Lille 2
3 rue du Pr Calmette
Lille Cedex, F-59006
France


Tingjun Hou
College of Chemistry and Molecular Engineering, Peking University
3 rue du Pr Calmette
Beijing , 100871
China


Xiaojie Xu
College of Chemistry and Molecular Engineering, Peking University
3 rue du Pr Calmette
Beijing , 100871
China


Nastiti Wijayanti
Institut für Klinische Immunologie und Transfusionsmedizin der Justus- Liebig Universität Giessen, Langhansstr. 7
Giessen, 35392
Germany


Stephan Immenschuh
Institut für Klinische Immunologie und Transfusionsmedizin der Justus- Liebig Universität Giessen, Langhansstr. 7
Giessen, 35392
Germany




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