Proteinase 2013


Speakers: 15 April 2013

Joerg Eder
Protease Platform, Novartis Institutes for BioMedical Research
Protease-directed drug discovery

Benedikt Kessler
University of Oxford
Novel tools for DUB inhibitor specificity profiling in cancer cells

Brian O'Neill
Pfizer Inc
ß-secretase inhibitors for the treatment of Alzheimer’s disease

Thomas Lübbers
F Hoffmann-La Roche
Optimization of β-secretase modulators through variation of scaffolds

Warren J Porter
Eli Lilly and Company
Discovery of a novel notch inhibitor

Douglas S Johnson
Pfizer Worldwide Research and Development
Application of chemical biology in the discovery of fatty acid amide hydrolase (FAAH) inhibitors and β-secretase modulators (GSMs)

Francois Bischoff
Janssen Research and Development

β-secretase modulators with reduced lipophilicity and reduced liver toxicity

Dieter Broemme
University of British Columbia
Complex formation and exosite inhibitors as specific collagenase and elastase blockers of Cathepsin K

Chris Hutchison
Queen's University Belfast
Oxazolidinones: beyond antibacterials- novel serine protease inhibitors

Jurgen Joossens
University of Antwerp
Novel and highly selective inhibitors of fibroblast activation protein (FAP)

Lorraine Martin
Queen's University Belfast
Targeting trypsin-like proteases: a mechanism to restore mucociliary function in cystic fibrosis airways

Darragh McCafferty
Queen's University Belfast
Overexpression of MMPs in prostate cells by propionibacterium acnes

Dmitriy Minond
Torrey Pines Institute
Discovery of novel non-zinc-binding exosite inhibitors of ADAM17 (TACE)

Pascal Rigollier
Novartis Institutes for BioMedical Research
Arylsulfonamide-based inhibitors of matrix metalloproteinase 13

Sven Ruf
Sanofi Aventis Deutschland GmbH
Inhibition of Cathepsin A: a novel strategy for the treatment of cardiovascular diseases

Michael Shokhen
Bar Ilan University
EMBM – Enzyme Mechanism Based Method for rational design of chemical sites of covalent inhibitors

Charlene Stewart
Queen's University Belfast
The inhibition of matrix metalloproteinases associated with inflammatory disease

Pavol Zlatoidsky
Astra Zeneca AB
Hydantoins-a new warhead for metalloproteinase inhibitors: the discovery of AZD6067

Kelly Aubart
GlaxoSmithKline
Discovery of peptide deformylase inhibitor GSK1322322, a novel mechanism of action antibiotic

Speakers: 16 April 2013

Shawn Stachel
Merck and Co Inc
Discovery and development of Odanacatib: a selective cathepsin K Inhibitor for the treatment of osteoporosis

Prabhakar K Jadhav
Discovery Chemistry Research and Technologies, LRL, Eli Lilly and Company
Discovery of potent, orally-bioavailable nonpeptide Cathepsin S inhibitor lacking interactions with catalytic cysteine

Peter Sjö
AstraZeneca R&D
N-arylpyridones: discovery and development of non-electrophilic inhibitors of human neutrophil elastase

Deqiang Niu
Celgene Avilomics Research
Silencing HCV with a potent and selective irreversible protease inhibitor

David Norton
Astex Pharmaceuticals
Novel allosteric inhibitors of HCV protease-helicase

Helena Danielson
Beactica AB and Uppsala University
From transition state analogues to fragments - drug discovery using SPR biosensor technology

Gerhard Klebe
Philipps-University Marburg
Molecular recognition in protein-ligand binding: what drives the binding?


Downloadable Files

Novel tools for DUB inhibitor specificity profiling in cancer cells
Benedikt Kessler
PDF iconPDF (1371k)  

Optimization of β-secretase modulators through variation of scaffolds
Thomas Lübbers
PDF iconPDF (1045k)  

Discovery of a novel notch inhibitor
Warren J Porter
PDF iconPDF (442k)  

Application of chemical biology in the discovery of fatty acid amide hydrolase (FAAH) inhibitors and β-secretase modulators (GSMs)
Douglas S Johnson
PDF iconPDF (1633k)  

β-secretase modulators with reduced lipophilicity and reduced liver toxicity
Francois Bischoff
PDF iconPDF (157k)  

Complex formation and exosite inhibitors as specific collagenase and elastase blockers of Cathepsin K
Dieter Broemme
PDF iconPDF (45k)  

Oxazolidinones: beyond antibacterials- novel serine protease inhibitors
Chris Hutchison
PDF iconPDF (84k)  

Novel and highly selective inhibitors of fibroblast activation protein (FAP)
Jurgen Joossens
PDF iconPDF (83k)  

Targeting trypsin-like proteases: a mechanism to restore mucociliary function in cystic fibrosis airways
Lorraine Martin
PDF iconPDF (212k)  

Overexpression of MMPs in prostate cells by propionibacterium acnes
Darragh McCafferty
PDF iconPDF (174k)  

Discovery of novel non-zinc-binding exosite inhibitors of ADAM17 (TACE)
Dmitriy Minond
PDF iconPDF (87k)  

Arylsulfonamide-based inhibitors of matrix metalloproteinase 13
Pascal Rigollier
PDF iconPDF (43k)  

Inhibition of Cathepsin A: a novel strategy for the treatment of cardiovascular diseases
Sven Ruf
PDF iconPDF (31k)  

EMBM – Enzyme Mechanism Based Method for rational design of chemical sites of covalent inhibitors
Michael Shokhen
PDF iconPDF (96k)  

The inhibition of matrix metalloproteinases associated with inflammatory disease
Charlene Stewart
PDF iconPDF (114k)  

Hydantoins-a new warhead for metalloproteinase inhibitors: the discovery of AZD6067
Pavol Zlatoidsky
PDF iconPDF (23k)  

Discovery and development of Odanacatib: a selective cathepsin K Inhibitor for the treatment of osteoporosis
Shawn Stachel
PDF iconPDF (1083k)  

From transition state analogues to fragments - drug discovery using SPR biosensor technology
Helena Danielson
PDF iconPDF (2964k)  


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