Vol.8 No.2A June 2003
IPK'2003
3rd International Conference Inhibitors of Protein Kinases
June 22-27, 2003
and Workshop
Phosphoryl-Transfer Mechanisms
June 27-28, 2003 Warsaw, Poland
DESIGN * STRUCTURAL BIOLOGY * PHOSPHORYLATION/ DEPHOSPHORYLATION PROCESSES * BIOCHEMISTRY * BIOTECHNOLOGY * SIGNALING PATHWAYS * CLINICAL ASPECTS * CHEMOTHERAPY
| Volume 8 (2003) pp 503 | |
| Title | PREFACE |
| Authors | David Shugar |
|
This special number of Cellular & Molecular Biology Letters presents the Abstracts
of Invited Lectures, and of submitted accepted Posters (some of which have been
selected for oral presentation) to the 3rd International Conference on INHIBITORS
OF PROTEIN KINASES (IPK'2003). Also included are Abstracts of lectures at
an associated Workshop on Phosphoryl-Transfer Mechanisms. Protein phosphorylation is widely recognized as the most important pathway for regulation of protein functions in living cells, by switching cellular activities from one state to another and, in this way, regulating gene expression, cell proliferation and cell differentiation. It is the major mechanism wherewith cells respond to extracellular signals such as hormones and growth factors, and controls all events at various stages of the cell cycle. Reversible protein phosphorylation is catalyzed by protein kinases and protein phosphatases.It has long been known that dysfunctions in activities of protein kinases may lead to severe pathological states. It is consequently not surprising that the biotechnology sector has for some time been devoting major efforts to “targeting” protein kinases for drug development, with considerable success in the past few years. The foregoing led to organization, in September, 1998, in Warsaw, Poland, of the 1st International Conference on INHIBITORS OF PROTEIN KINASES (IPK'98), followed by publication of the texts of invited lectures, and of some posters selected for oral presentation, each in the form of an overview, in the international journal Pharmacology & Therapeutics 82, Nos. 2-3 (1999). Subsequent unabated progress in this field led, in turn, to the 2nd International Conference in Warsaw, September, 2001 (IPK'2001) devoted, as before, to real breakthroughs in identification and specificities of protein kinases, their three-dimensional structures and mechanisms of action, design and development of inhibitors, delineation of signaling pathways, in many instances with the aid of inhibitors, and numerous promising applications of inhibitors as therapeutic agents. Also included was a Workshop on Computer-Aided Drug Design, which attracted broader interest from participants than originally envisaged. The Proceedings subsequently appeared in Pharmacology &Therapeutics 99, Nos. 2-3 (2002). The present 3rd International Conference (IPK'2003) has been extended somewhat in scope to include a special session on the newly developing field of protein kinases of pathogenic agents such as viruses, parasites and fungi, and their potential as therapeutic targets. It also includes a Workshop on Phosphoryl-Transfer Mechanisms, and relevance to protein kinases and protein phosphatases. It should be noted that, apart from being truly international in scope, IPK'2003 includes participation of leading specialists representing a broad range of disciplines from both Academia and the Biotechnology sector, thus ensuring adequate consideration of potential therapeutic applications. |
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| Volume 8 (2003) pp 508-548 | |
| Invited Lectures | |
| Abstracts List |
STRUCTURAL INSIGHTS INTO AGC-KINASE INHIBITOR BINDING FROM STUDIES WITH THE WORKHORSE PKA Michael Gaßel, Christine B. Breitenlechner, Satur Herrero De Vega, Richard A.Engh and Dirk Bossemeyer - p508ANTISENSE PROTEIN KINASE A RI∂-INDUCED TUMOR REVERSION: PORTRAIT OF A MICROARRAY Yoon S. Cho-Chung - p510PROTEIN KINASE SIGNALING CASCADE DURING NITRIC OXIDE-INDUCED APOPTOSIS, DEDIFFERENTIATION AND INFLAMMATORY RESPONSES OF ARTICULAR CHONDROCYTES Jang-Soo Chun - p512INHIBITION OF HSP90 AS A SPECIAL WAY TO INHIBIT PROTEIN KINASES Peter Csermely and Csaba Soti - p514THE KINETIC MECHANISM OF THE SERINE/THREONINE SPECIFIC PROTEIN KINASE ERK2 William F. Waas, Mark Rainey, Anna Szafranska and Kevin N. Dalby - p516STRUCTURE/FUNCTION STUDIES OF THE PHOSPHORYL-TRANSFER ENZYME: PHOSPHOENOLPYRUVATE CARBOXYKINASE Louis T. J. Delbaere, Athena M. Sudom, Lata Prasad, Yvonne Leduc and Hughes Goldie - p519BACTERIAL SERINE AND TYROSINE PROTEIN KINASES CONTAINING A WALKER MOTIF Josef Deutscher - p522PROTEIN KINASES AS TARGETS FOR ANTI-PARASITIC CHEMOTHERAPY Christian Doerig - p524PROTEIN KINASE INHIBITORS AS ANTILEUKEMIC AGENTS Doriano Fabbro - p526STRUCTURE, REGULATION AND FUNCTION OF PKB/AKT - A MAJOR THERAPEUTIC TARGET Brian A. Hemmings - p527STRUCTURE-BASED DESIGN OF THE ANTITUMOR 2-HYDROXYARY-LIDENE-4-CYCLOPENTENE-1,3-DIONE TX-1123 AS A PROTEIN TYROSINE KINASE INHIBITOR HAVING LOW MITOCHONDRIAL TOXICITY Hitoshi Hori, Hideko Nagasawa and Yoshihiro Uto - p528BIOSENSORS OF PROTEIN KINASE ACTION: FROM IN VITRO ASSAYS TO LIVING CELLS David S. Lawrence - p531ADVANCES IN THE STRUCTURAL BIOLOGY, DESIGN AND CLINICAL DEVELOPMENT OF VEGF-R KINASE INHIBITORS FOR THE TREATMENT OF ANGIOGENESIS Paul William Manley, Guido Bold, Gabrielle Fendrich, Pascal Furet, Jürgen Mestan, Thomas Meyer, Bernd Meyhack, Wilhelm Stark, Andre Strauss and Jeanette Wood - p532PHARMACOLOGICAL INHIBITORS OF CYCLIN-DEPENDENT KINASES (CDKS) AND GLYCOGEN SYNTHASE KINASE -3 (GSK-3) Laurent Meijer - p534THE UL97 PROTEIN KINASE OF HUMAN CYTOMEGALOVIRUS (HCMV) AND HOMOLOGUES IN OTHER HERPESVIRUSES: RELEVANCE FOR VIRUS AND HOST Detlef Michel and Thomas Mertens - p535VIRAL AND CELLULAR KINASES PLAY A CENTRAL ROLE IN VZV PATHOGENESIS AND ARE TARGETS FOR ANTIVIRAL KINASE INHIBITORS Jennifer F. Moffat, Shannon L. Taylor and Stacey Leisenfelder - p537MOLECULAR DISSECTION OF FERTILISATION SIGNALLING WITH THE AID OF TYROSINE-KINASE-SPECIFIC INHIBITORS Ken-ichi Sato, Tetsushi Iwasaki and Yasuo Fukami - p541EFFECTS OF PHARMACOLOGICAL CYCLIN-DEPENDENT KINASE INHIBITORS ON VIRAL TRANSCRIPTION AND REPLICATION Luis M. Schang - p543cAMP-DEPENDENT PROTEIN KINASE: DYNAMICS OF CATALYSIS AND DOCKING Susan S. Taylor, Pearl Akamine, Jerry Yang, Jian Wu, Ganesh Iyer, Ganesh Anand, Marat Valiev, John h. Weare and Donna D. Johnson - p545THE ROLE OF CYCLIN-DEPENDENT KINASE 5 IN BRAIN DEVELOPMENT AND DEGENERATION Li-Huei Tsai - p546TYROSINE KINASE INHIBITORS AND ASTHMA WS Fred Wong - p548 |
| abstracts of posters selected for oral presentations | |
| Abstracts List |
DEVELOPMENT AND USE OF A PEPTIDE INHIBITOR OF THE C-JUN N-TERMINAL KINASE (JNK) SUBFAMILY OF MITOGEN-ACTIVATED PROTEIN KINASES Marie A. Bogoyevitch, Renae K. Barr, Richard M. Hopkins, Paul M. Watt, Ingrid Boehm, Angela Chan and Peter G. Arthur - p550INHIBITORS OF Civ1 KINASE BELONGING TO 6-AMINOAROMATIC-2-CYCLOHEXYLDIAMINO PURINE SERIES AS POTENT ANTI-FUNGAL COMPOUNDS Jean-Luc Haesslein, Paul Ferrari, Nathalie Jullian, Jacques Biton, Marie-Therese Bocquel, Christian Ciot, Anne-Marie Girard and Florence Bordon-Pallier - p552A STATISTICAL PROCEDURE (CHAIN) TO STUDY PROTEIN KINASE STRUCTURAL MECHANISMS Natarajan Kannan and Neuwald Af - p554INSIGHTS INTO SELECTIVITY OF STI571 (Gleevec™) FROM X-RAY CRYSTALLOGRAPHY Jacek Nowakowski, Vandana Sridhar, Devon A. Thompson, Ciarán N. Cronin, Daniel E. Vaughn, Anthony R. Gangloff, Bi-Ching Sang, Hua Zoa, Mark W. Knuth, Ronald V. Swanson, Gyorgy Snell, Clifford D. Mol, Keith P. Wilson and Duncan E. McRee - p556NEURONAL CYCLIN-DEPENDENT KINASE 5(CDK5) AND ITS SPECIFIC INHIBITOR (CIP): ITS PHYSIOLOGICAL AND PATHOLOGICAL ROLE IN THE NERVOUS SYSTEM Yali Zheng, Sashi Kesavapany and Harish C. Pant - p558VALIDATION OF NOVEL PROTEIN KINASE TARGETS AND DEVELOPMENT OF NEXT GENERATION PROTEIN KINASE INHIBITORS USING ProQinase's INTEGRATED TECHNOLOGY PLATFORM PROTEIN KINASES Christoph Sachsenmaier - p561STRUCTURE-BASED OPTIMIZATION OF CDK2 INHIBITORS Martina Schäfer, Hans Briem, Thomas Brumby, Uwe Eberspächer, Michael Grimm, Martin Haberey, Holger Hess-Stumpp, Rolf Jautelat. Martin Krüger, Ulrich Lücking, Olaf Prien, Andreas Reichel, Gerhard Siemeister and Andreas Steinmeyer - p562BIFUNCTIONAL INHIBITORS OF PROTEIN KINASES FOR INTRACELLULAR APPLICATIONS Asko Uri, Kaido Viht and Margus Pooga - p564COMBINING MEDICINAL CHEMISTRY WITH CHEMOGENOMIC AND COMPUTER-AIDED STRUCTURE-BASED DESIGN IN DEVELOPMENT OF NOVEL KINASE INHIBITORS Michal Vieth, Harold B. Brooks, Chafiq Hamdouchi, William McMillen, Jason S. Sawyer, Jonathan M. Yingling and Faming Zhang - p566 |
| Posters | |
| Abstracts List |
INHIBITION OF HYPOXIA-INDUCED TOLERANCE TO SUBSEQUENT HYPEROXIC INJURY IN LUNG CELLS BY PHOSPHATIDYL INOSITOL 3-KINASE INHIBITORS: LY294002 AND WORTMANNIN Shama Ahmad, Aftab Ahmad, Evgenia Gerasmivoskaya, Kurt R. Stenmark and Carl W. White - p570AN INVESTIGATION OF CRK PROTEIN KINASES OF LEISHMANIA AND THE ASSESSMENT OF THEIR POTENTIAL AS DRUG TARGETS Nahla Om Ali, Muntaser E. Ibrahim, Imadeldin E. Aradaib, Karen M. Grant and Jeremy C. Mottram - p571EVOLVING THE DESIRED COMPOUND PROFILE WITHIN AN LCK PROJECT Ian R. Baldwin - p573CYCLIN-DEPENDENT PROTEIN KINASE-2 REGULATION BY PHOSPHORYLATION, A MOLECULAR DYNAMICS STUDY Iveta Bártová, Michal Otyepka, Zdeněk Kříž and Jaroslav Koča - p574THE INHIBITION OF PROTEIN KINASE C BY HEPATITIS C VIRUS NON-STRUCTURAL PROTEIN 3 DEPENDS ON ITS CONFORMATIONAL STATUS Peter Borowski and Philip Hartjen - p576EFFICIENT CHARACTERIZATION OF KINASE INHIBITORS USING LeadCodeTM TECHNOLOGY Carsten Degenhart - p578THE PI3K KINASE INHIBITOR, LY294002, DECREASES RANTES-INDUCED PERITONEAL RECRUITMENT OF NEUTROPHILS IN MICE Chiara Ferrandi, Hong Ji, Christian Rommel and Rocco Cirillo - p579CRYSTAL STRUCTURE OF AN ALTERED CATALYTIC SUBUNIT OF cAMP-DEPENDENT PROTEIN KINASE IN COMPLEX WITH THE PKC-KINASE INHIBITOR BISINDOLYL-MALEIMIDE 2 IN TWO DIFFERENT CONFORMATIONS-IMPLICATIONS FOR SELECTIVITY Michael Gassel, Christine B. Breitenlechner, Richard A. Engh and Dirk Bossemeyer - p582INHIBITION OF C-JUN/JNK AND MLK PATHWAY ACTIVATION BLOCKS DNA DAMAGE-INDUCED DEATH IN EMBRYONIC CORTICAL NEURONS Mohammad H. Ghahremani, Elizabeth Keramaris, Chantal Bazenet, Jonathan Ham, Ruth S. Slack and David S. Park - p583STUDY OF CASEIN KINASE II INHIBITORY ACTIVITY OF 4-AMINOQUINOLINE AND 4-AMINOQUINAZOLINE DERIVATIVES BY COMBINED DOCKING - MOLECULAR DYNAMICS APPROACH Andriy G. Golub, Alexander O. Y. Yakovenko, Volodymyr G. Bdzhola and Sergiy M. Yarmoluk - p584HIGH-THROUGHPUT INTERACTION SCREENING FOR THE ELUCIDATION OF PROTEIN KINASE NETWORKS AND THE IDENTIFICATION OF PROTEIN KINASE INHIBITORS Claudia Kruse, Sergey Vasiliev, Sabine Hanke and Hanjo Hennemann - p585EFFECT OF VARIOUS PROTEIN KINASE INHIBITORS ON OSMOTIC STRESS-ACTIVATED PROTEIN KINASE (OSAK) ACTIVITY Anna Kelner, Izabela Pękala and Grażyna Dobrowolska - p586NOVEL SMALL-MOLECULE INHIBITORS OF C-TERMINAL Src KINASE (Csk) Anna Kilimnik, Maria N. Kostjukova, Ilya H. Pyatkin, Andrey M.Pronin, Svetlana R. Strelnikova, Yuri A. Fedotov and Alexander V. Kolesnikov - p588TYROSINE PHOSPHATASE SHP-1 REGULATES LPS-INDUCED CYTOKINE NETWORKS INVOLVED IN INFLAMMATION Chinonso Okenwa, Dorothy Rego, Natalie J. Pang and Maya Kozlowski - p590THEORETICAL STUDIES ON SUGAR AND PROTEIN KINASES: STRUCTURAL AND MUTATIONAL VARIABILITY Jacek Kuśka and Jacek Leluk - p592COMPARATIVE STUDIES OF SUGAR AND PROTEIN KINASES: GENETIC RELATIONSHIPS AND CONSENSUS SEQUENCES Anna Zdyb and Jacek Leluk - p593IMPROVING THE EFFICIENCY OF HALOGENATED BENZIMIDAZOLE INHIBITORS OF PROTEIN KINASE CK2 Flavio Meggio, Mario A. Pagano, Mariola Andrzejewska, Luca Cesaro, Zygmunt Kazimierczuk and Lorenzo A. Pinna - p594TETRASUBSTITUTED PURINES AS INHIBITORS OF CDK1 Jiří Moravec, Libor Havlicek, Daniela Moravcova, Jan Hanus, Květoslava Fuksova, Michal Otyepka, Vladimír Krystof and Miroslav Strnad - p596RATIONAL DESIGN OF NEW COMPETITIVE INHIBITORS OF HUMAN CK2 ACTIVITY Stefano Moro, Diego Dal Ben, Giuseppe Zagotto, Flavio Meggio, Stefania Sarno and Lorenzo A. Pinna - p598DEVELOPING KINASE TOOLS FOR DRUG DISCOVERY Steve Davies, Andrew Paterson, Joachim Morr, Barry Ewen, Chris Armstrong and Sue Dale - p599STRUCTURAL GENOMICS OF THE HUMAN PROTEIN KINASE FAMILY Anna Aparicio, Alexei Brooun, Ellen Chien, Ellen Chi, Bernard Collins, Ciarán N. Cronin, Anthony Davies, Douglas Dougan, Erin Heien, Mark Hilgers, David Hosfield, Marie Hu, Daniel Kassel, Stella Kim, Mark W. Knuth, Michelle Kraus, Irena Levin, Kheng Lim, Melinda Manuel, Duncan E. Mcree, Clifford D. Mol, Jacek Nowakowski, Joe Rogers, Bettina Roth, Bi-Ching Sang, Daniel Scheibe, Robert Skene, Vandana Sridhar, Ronald V. Swanson, Devon A. Thompson, Darbi Witmer, Robert Wynands, Gyorgy Snell, Keith P. Wilson, Garret Textor, Daniel Vaughn, Sheng Ye and Hua Zoa - p600WP744, A NOVEL HIGHLY APOPTOTIC AND ANTI-PROLIFERATIVE AGENT AGAINST STI-571-RESISTANT LEUKEMIC CELLS Waldemar Priebe, Gilad Evrony, Izabela Fokt, Sangyou Lee, Moshe Talpaz and Nicholas J. Donato - p601SCC DFT-TB ENERGY CALCULATIONS OF THE PHOSPHORYL TRANSFER REACTION IN THE PKA ACTIVE SITE Franciszek Rakowski, Pawel Grochowski and Bogdan Lesyng - p603PEPTIDE MICRO-ARRAYS FOR KINASE PROFILING Mike Schutkowski, Ulf Reimer, Sören Panse, Liying Dong and Jens Schneider-Mergener - p605STUDIES ON CK2 INHIBITION CAPACITY OF 4-AMINOQUINOLINES AND 4-AMINOQUINAZOLINES Natalia M. Ryabchenko, Olexandr G. Kukharenko, Vadim M. Sapelkin, Galina G. Dubinina, Svetlana Y. Dmitrieva and Sergiy M. Yarmoluk - p606INHIBITION OF A Ca2+-DEPENDENT PROTEIN KINASE FROM IRANIAN RICE LEAVES BY pH AND TEMPERATURE Reyhaneh Sariri and Amir Arasteh - p607EFFECTS OF PROTEIN KINASE A INHIBITOR (H-89) ON SPATIAL MEMORY AND EXPRESSION OF CHOLINE ACETYLTRANSFERASE (ChAT) AND VESICULAR ACETYLCHOLINE TRANSPORTER (VAChT) PROTEINS Mohammad Sharifzadeh, Kurdastan Sharifzadeh and Mohammad H. Ghahremani - p609TOPBUILDER-MOLECULAR TOPOLOGY BUILDING AND CHEMICAL DATABASE PROCESSING SOFTWARE Alexander O.Y. Yakovenko, Andryi G. Golub, Volodymyr G. Bdzhola and Sergiy M. Yarmoluk - p610YEAST Cu,Zn-SUPEROXIDE DISMUTASE (SOD) AS AN INHIBITORY SUBUNIT OF PROTEIN KINASE CK2ďˇ Rafał Zieliński, Olga Abramczyk, Piotr Zień, Marek Pilecki, Konrad Kubiński, Ulf Hellman and Ryszard Szyszka - p611SELECTIVITY OF 4,5,6,7-TETRABROMOBENZIMIDAZOLE (TBBZ) AS AN ATP-COMPETITIVE POTENT INHIBITOR OF PROTEIN KINASE CK2 FROM VARIOUS SOURCES Piotr Zień, Maria Bretner, Katarzyna Zastąpiło, Ryszard Szyszka and David Shugar - p613 |
| Workshop on phosphoryl-transfer mechanisms | |
| Abstracts List |
PATHWAYS AND PROTONATION STATES IN THE MECHANISM OF PROTEIN TYROSINE PHOSPHATASE: A STUDY USING COMBINED MACROSCOPIC AND QUANTUM-MECHANICAL MODELS Dilipkumar Asthagiri, Valerie Dillet, Tiqing Liu, Louis Noodleman, Robert L Van Etten and Donald Bashford - p616QUANTUM AND QUANTUM-CLASSICAL STUDIES OF PHOSPHORYL-TRANSFER MECHANIMS IN MODEL SYSTEMS Paweł Grochowski - p617SIMULATIONS OF STRUCTURE AND DYNAMICS OF PHOSPHOLAMBAN: INFLUENCE OF ENVIRONMENT AND OF PHOSPHORYLATION Krzysztof Kuczera and Yao Houndonougbo - p619A COMPARATIVE STUDY OF THE PRIMARY STRUCTURES OF PROTEIN AND SUGAR KINASES Jacek Leluk and Bogdan Lesyng - p620COMPUTATIONAL STUDIES ON ENZYMATIC PHOSPHATE HYDROLYSIS Jordi Villa - p622THE MECHANISM OF ADP PHOSPHORYLATION BY ATP SYNTHASE Joachim Weber - p623MODELS FOR BIOLOGICAL PHOSPHORYL TRANSFER Nicholas H. Williams - p624 |