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There has been remarkable progress in the understanding of kinases and the role that they play in various pathological states. The pharmaceutical and biotech industries have been studying these enzymes intensively in recent years in order to discover viable targets as a basis for drug development.

With our increasing knowledge of the underlying genetics of kinases and of their role in signal transmission, more and more work is being done to harness the potential of kinase inhibitors for treatment of diseases such as cancer, inflammation and cardiovascular disease. Second only to proteases, kinases represent the most favoured group of enzymes on which to model new drugs.

SMi’s conference will provide you with the very latest developments in kinase drug discovery and development, including specific case studies of kinase-based drugs in clinical trials and beyond. The conference aims to provide a forum where developments in this field, in terms of target identification and validation, drug design, assaying, molecular modelling and clinical trials can be discussed and evaluated.

A unique opportunity to learn from leading industry experts including:
· Dr Doriano Fabbro, Unit Head, In Vitro Lead Profiling, Oncology Research, Novartis
· Dr Yajun Xu, Associate Director, Immunopharmacology, Millenium Pharmaceuticals
· Dr John Siekierka, Senior Research Fellow & Head, Drug/Device Pharmacology Research, Johnson & Johnson
· Dr Christian Rommel, Senior Scientist, Head, Signal Transduction, Serono
· Dr Neil Moss, Associate Director, Medicinal Chemistry, Boehringer Ingelheim
· Dr Alan Lewis, President, Celgene
· Dr Haile Tecle, Assistant Director, Pfizer
· Dr Jonathan Terrett, Director, Molecular Biology, Oxford GlycoSciences
· Dr Jean-Pierre Gotteland, Head, Enzyme Medicinal Chemistry, Serono
· Dr John Pollard, Group Leader, Vertex Pharmaceuticals

Key benefits of attending:
KINASE INHIBITORS: gain an insight into cutting edge research
ANTI-CANCER TARGETS: review the current strategies
HIGH-THROUGHPUT SCREENING: learn about improved assay technologies
ANTI INFLAMMATORY TARGETS: understand the importance of NFkB signalling
ANTI-ANGIOGENIC ACTIVITY: focus on small molecule kinase inhibitor
NETWORKING: exchange ideas with experts in the field

“ I am always impressed by the quality of the organization and of the information presented at SMi’s Conferences”
Dr Nigel Phillips, Chief Scientific Officer, Bioniche Life Sciences

Conference programme

8:30 Registration and Coffee

9:00 Chairman's Opening Remarks

Dr Alan Lewis

Dr Alan Lewis, President, Celgene

9:10 NOVEL CHEMICAL GENETIC APPROACHES TO KINASE DRUG DISCOVERY

Dr Dapeng Qian

Dr Dapeng Qian, Senior Director, Kinase Program, Cellular Genomics

  • ASKA: CGI’s proprietary chemical genetics platform
  • ASKA-based kinase substrate identification: a powerful tool for pathway mapping and discovery of novel drug targets
  • ASKA mice: pharmacologically relevant kinase target validation and therapeutic index determination
  • ASKA-based drug screens
  • Examples of how CGI uses the ASKA technology for target identification, validation and kinase drug discovery
  • 9:40 KINASE LEAD FINDING

    Dr Aimo Kannt

    Dr Aimo Kannt, Research Scientist, Aventis

  • Preferred assay technologies
  • High-density chip format
  • Automated assay optimisation using the design of experiment principle
  • Enzymological considerations
  • 10:20 STRUCTURE BASED LEAD DISCOVERY

    Dr Paul Wyatt

    Dr Paul Wyatt, Senior Medical Chemist, Astex Technology

  • High-throughput protein: ligand x-ray crystallography
  • Identification of novel scaffolds by fragment based lead discovery
  • Exploiting novel scaffolds within target families
  • Generation of robust drug candidates from fragment hits
  • 11:00 Morning Coffee

    11:20 REDISTRIBUTION: A NEW APPROACH FOR INDENTIFYING KINASE INHIBITORS

    Dr Len Pagliaro

    Dr Len Pagliaro, Vice President, Discovery Projects, BioImage

  • Cell-based assays for primary and secondary screening
  • Green fluorescent protein fusions with target molecules as the sensor
  • Pharmacological responses detected by analysis of kinase translocation in living cells
  • Modulation of translocation as a route to improved selectivity
  • Examples and a case study
  • 12:00 KINASE INHIBITOR LEAD DISCOVERY AT SERONO

    Dr Matthias Schwarz

    Dr Matthias Schwarz, Head, Combinatorial & GPCR Chemistry, Serono

  • Successful lead discovery hinges on three major pillars: target validation, assay technology and a high-value compound collection
  • This presentation will show, through case examples, which solutions Serono has adopted to cover each of these three areas, with a view to building an integrated kinase lead discovery platform, relying on both strategic external alliances and on proprietary tools developed internally over the past four years
  • 12:40 Networking Lunch

    13:40 CELL BASED ASSAYS FOR RECEPTOR TYROSINE KINASES (RTKs)

    Dr Kirsten Mundt

    Dr Kirsten Mundt, Business Development, ESBATech

  • Screening in the physiologically relevant environment
  • Elimination of unstable and toxic compounds or compounds with poor membrane permeability
  • Rapid identification of drug candidates with better pharmacological properties
  • Specific implementation of reliable assays with low interference from redundant processes
  • Assays of RTKs in a membrane associated context
  • 14:20 KINASE INHIBITORS AS ANTI-APOPTOTIC AGENTS

    Dr Jean-Pierre Gotteland

    Dr Jean-Pierre Gotteland, Head, Enzyme Medicinal Chemistry, Serono

  • Kinase platform from target validation to in vivo pharmacology
  • Key role JNK in apoptosis
  • In vitro kinase selectivity
  • Preclinical models of acute stroke
  • Preclinical models of myocardial infarction
  • 15:00 DEVELOPMENT OF IKK2 INHIBITOR AS ANTI-INFLAMMATORY

    Dr Yajun Xu

    Dr Yajun Xu, Associate Director, Immunopharmacology, Millennium Pharmaceuticals

  • NFkB signaling plays vital role in pro-inflammatory responses, IKK2 mediate activation of NFkB
  • Small molecule inhibitor blocks several cykine chemokine production in vitro in reponse to a variety inflammatory stimuli
  • Inflammatory responses in both acute and chronicle inflammatory disease model
  • IKK2 inhibitor provide new exciting opportunity for anti-inflammatory therapy
  • 15:40 Affernoon Tea

    16:00 DESIGN AND SYNTHESIS OF SELECTIVE MEK INHIBITORS

    Dr Haile Tecle

    Dr Haile Tecle, Assistant Director, Pfizer

  • Synthesis
  • SAR
  • In-vitro, ex-vivo, in-vivo pharmacology
  • Clinical phase I results
  • 16:40 INHIBITORS EFFECTIVE IN CANCER PRECLINICAL TRIALS

    Dr Alan Lewis

    Dr Alan Lewis, President, Celgene

  • JNK a universal drug target
  • Anti-tumor, anti-inflammatory and anti-diabetic effects in in vivo models
  • Results of the preclinical studies
  • Selectivity blocking the cellular activity of the pathways
  • Controlling gene expression to prevent onset and progression of diseases
  • Overcoming challenges
  • 17:20 Chairman’s Closing Remarks and Close of Day One

    8:30 Re-registration and Coffee

    9:00 Chairman's Opening Remarks

    Dr Neil Moss

    Dr Neil Moss, Associate Director, Medicinal Chemistry, Boehringer Ingelheim

    9:10 CHEMOGENOMICS

    Dr John Pollard

    Dr John Pollard, Group Leader, Vertex Pharmaceuticals

  • Avantages in targeting entire gene families
  • Mapping biological and chemical space
  • Application of structural information to the design of selective inhibitors
  • Chemogenomic progress and case studies
  • 9:40 FROM LEAD COMPOUND TO CLINICAL CANDIDATE

    Dr Neil Moss

    Dr Neil Moss, Associate Director, Medicinal Chemistry, Boehringer Ingelheim

  • P38 as a therapeutic target
  • Identification and optimization of a new class of kinase inhibitors
  • Novel binding mode and binding kinetics
  • In vitro / in vivo characterization
  • Status of clinical trials
  • 10:20 INHIBITORS OF CYCLIN-DEPENDENT KINASES WITH HIGHLY SELECTIVE ANTI-CANCER ACTIVITY

    Dr Robert Jackson

    Dr Robert Jackson, Executive Director, Research & Development, Cyclacel

  • CYC202 (R-roscovitine), an orally available CDK2 inhibitor, is in phase II clinical trials in oncology
  • CYC202 also shows activity in preclinical models of glomerulonephritis
  • CDK inhibitors has shown activity in vitro againts HIV
  • CYC202 strongly potentiates cell cycle-specific cytotoxic agents
  • Inhibitors of CDK2 act at two distinct sites in the cell cycle, depending upon checkpoint function
  • A potent novel series of CDK2 inhibitors selectively triggers mitotic catastrophe in transformed cells
  • 11:00 Morning Coffee

    11:20 CHARACTERIZATION OF A POTENT TYROSINE KINASE INHIBITOR WITH ANTI-ANGIOGENIC AND ANTI-TUMOR ACTIVITY

    Dr Marion Wiesmann

    Dr Marion Wiesmann, Scientist II, Chiron

  • Selectivity profile
  • In vitro and in vivo anti-angiogenic activity
  • In vitro and in vivo anti-tumor activity
  • Pharmacokinetic characteristics
  • Summary and outlook
  • 12:00 PROTEOMICS AND THE SELECTION OF ONCOLOGY KINASE TARGETS

    Alasdair Stamps

    Alasdair Stamps, Head of Target Informatics, Oncology Division, Oxford GlycoSciences

  • Proteomics processes for the identification of kinases
  • Sensitivity and specificty
  • Application to oncology target discovery
  • Target classes, receptors and non receptors for small molecule and Mab drug development
  • Target validation through expression analysis, ligand binding and gain/loss of function
  • 12:40 Networking Lunch

    14:00 MYCOBACTERIAL CELL WALL COMPLEX (MCC) ANTI-CANCER ACTIVITY

    Dr Nigel Phillips

    Dr Nigel Phillips, Senior Vice President, Scientific Affairs & Chief Scientific Officer, Bioniche Life Sciences

  • MCC anti-cancer activity and status
  • Inhibition of proliferation
  • Cell cycle arrest
  • Induction of apoptosis
  • Protein kinase modulation
  • Optimal anti-cancer activity requires inhibition of multiple pathways?
  • 14:40 DEVELOPMENT OF ANTI-CANCER MONOCLONAL ANTIBODIES THAT BLOCK TYROSINE KINASE RECEPTOR SIGNALING

    Dr Peter Bohlen

    Dr Peter Bohlen, Senior Vice President, Research, ImClone Systems

  • Rapid identification by phage display technology of fully human high affinity antibodies capable of blocking ligand binding to growth factor receptors and ligand-activated receptor signaling
  • Specificity of antibodies allows precise determination of roles of receptor in disease, as well as definition of function-associated toxicities
  • Diffiretial functions of VEGF receptors –1 and –2 in angiogenesis and leukemia
  • VEGF receptor-1 antibody as a potential treatment for breast cancer
  • LGF1 receptor antibody as a pro-apoptotic anti-cancer therapy
  • 15:20 SIGNAL TRANSDUCTION FIREWALLS

    Dr Bert Klebl

    Dr Bert Klebl, Vice President, Research, Axxima Pharmaceuticals

  • Making use of the kinome
  • The role of protein phosphorylation in infectious disease
  • The latest methods for target identification, target validation
  • Small molecule inhibitors
  • Early integration of kinase biology and kinase chemistry
  • 16:00 Chairman's Closing Remarks followed by Afternoon Tea. Close of Conference

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    WHAT IS CPD?

    CPD stands for Continuing Professional Development’. It is essentially a philosophy, which maintains that in order to be effective, learning should be organised and structured. The most common definition is:

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    Undertaken over a period of time, CPD ensures that educational qualifications do not become obsolete, and allows for best practice and professional standards to be upheld.

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