- Email: [email protected]
Contents 1 continued pages 1-2 2
CONTENTS 1 Continued
REVIEWS (continued) INFORMATICS
1125 Systems mapping of genes controlling chemotherapeutic drug efficiency for cancer stem cells Weimiao Wu, Sisi Feng, Yaqun Wang, Ningtao Wang, Han Hao and Rongling Wu
POST SCREEN
1131 Exploratory toxicology as an integrated part of drug discovery. Part I: Why and how Jorrit J. Hornberg, Morten Laursen, Nina Brenden, Mikael Persson, Annemette V. Thougaard, Dorthe B. Toft and Tomas Mow
1137 Exploratory toxicology as an integrated part of drug discovery. Part II: Screening strategies Jorrit J. Hornberg, Morten Laursen, Nina Brenden, Mikael Persson, Annemette V. Thougaard, Dorthe B. Toft and Tomas Mow
1145 A potential role for GPR55 in the regulation of energy homeostasis Anna C. Simcocks, Lannie O’Keefe, Kayte A. Jenkin, Michael L. Mathai, Deanne H. Hryciw and Andrew J. McAinch
Themed section: Rheumatology/Mechanisms underlying inflammatort bone & joint disease Guest Editor: Costantino Pitzalis 1152 Pathogenesis of rheumatoid arthritis: from systemic autoimmunity to localised joint disease Costantino Pitzalis
1155 Novel immunological targets in rheumatic diseases: clues from current therapies Fulvio D’Acquisto, Lorenza Rattazzi, Giuseppa Piras and Maria Letteria Galuppo
1161 Peripheral and synovial mechanisms of humoral autoimmunity in rheumatoid arthritis Elisa Corsiero, Costantino Pitzalis and Michele Bombardieri
1166 Resolution of inflammation: examples of peptidergic players and pathways Tazeen J. Ahmed, Magdalena K. Kaneva, Costantino Pitzalis, Dianne Cooper and Mauro Perretti
1172 Cellular and molecular mechanisms of cartilage damage and repair Joanna C. Sherwood, Jessica Bertrand, Suzanne E. Eldridge and Francesco Dell’Accio
1178 Cellular and molecular mechanisms of bone damage and repair in inflammatory arthritis Catherine Swales and Afsie Sabokbar
1186 Resolution of inflammation: targeting GPCRs that interact with lipids and peptides Jenna L. Cash, Lucy V. Norling and Mauro Perretti
ScienceDirect
CONTENTS 2 Continued
DRUG DISCOVERY TODAY Editorial Editor: Steve Carney Content Development Managers: Sandra Korver and Jasmin Bakker Journal Manager: Herman Engelen Publisher: Jaap van Harten Editorial Enquiries: Drug Discovery Today Elsevier 32 Jamestown Road, London, NW1 7BY, UK Tel: +44 (0)20 7424 4200 Fax: +44 (0)1865 853067 Email: [email protected]
Themed section: Autoimmunity Guest Editor: Esteban Masuda and Donald G. Payan 1193 Targeting autoimmunity: strategies and tactics Esteban S. Masuda and Donald G. Payan ADVISORY EDITORIAL BOARD Jurgen Bajorath University of Bonn, Germany Walter Blackstock Experimental Therapeutics Centre, Singapore David Brayden University College Dublin, Ireland Paul Caron Integrated Profiling, USA David Cavalla Numedicus Ltd., UK David Clark Argenta Discovery, UK Dalia Cohen ALN Associates, USA Donald Daley Argenta Discovery, UK Sean Ekins ACT LLC and Collaborations in Chemistry, USA Hans-Peter Fischer GeneData, Switzerland Peter Ghazal University of Edinburgh, UK Christopher M. Hill Merck, USA Nick Hird Takeda Chemical Industries, Japan Enoch Huang Pfizer, USA Thomas Joos University of Tuebingen, Germany Vincent H.L. Lee Chinese University of Hong Kong, China David Lewin Yale University, USA Christopher A. Lipinski Melior Discovery, USA Lorenz Mayr AstraZeneca, UK Nick Meanwell Bristol-Myers Squibb, USA BK Muralidhara AstraZeneca, USA Mark Murcko Disruptive Biomedical, LLC, USA Fajun Nan Shanghai Institute of Materia Medica, China Pradeep Nathan Experimental Medicine, GSK and University of Cambridge Gitte Neubauer Cellzome, Germany Eric Neumann Clinical Semantics Group Consulting, USA Tim Peakman UK Biobank, UK Norton Peet Microbiotix, Inc., USA Manuel Peitsch Swiss Institute of Bioinformatics, Switzerland Kurt Rasmussen Eli Lilly and Co. Ltd. USA Janice Reichert Reichert Biotechnology Consulting LLC, MA, USA John Reidhaar-Olson Albert Einstein College of Medicine, New York, USA Mike Romanos Crescendo Biologics, Cambridge, UK Raymond C. Rowe Intelligensys, UK Andreas Russ University of Oxford, UK Esther Schmid EFS Strategy and Business Consulting, UK Jonathan Sheldon Translational Medicine, Oracle, UK Michael Snyder Stanford University, USA Susie Stephens Johnson & Johnson, USA Robert Strausberg Ludwig Institute for Cancer Research, New York, USA Yuichi Sugiyama University of Tokyo, Japan David Szymkowski Xencor, USA Nick Terrett Ensemble Discovery, USA Vladimir Torchilin Northeastern University, Boston, USA Mark Whittaker Evotec OAI, UK Hans Winkler Janssen Pharmaceutica, Belgium Limsoon Wong National University of Singapore X.F. Steven Zheng Robert Wood Johnson Medical School, USA
ScienceDirect
1195 PI3K inhibitors as potential therapeutics for autoimmune disease Jennifer Ball, Sophie Archer and Stephen Ward
1200 Bruton’s tyrosine kinase inhibitors for the treatment of rheumatoid arthritis Jennifer A. Whang and Betty Y. Chang
1205 Inhibiting ROR␥t/Th17 axis for autoimmune disorders Fujio Isono, Saori Fujita-Sato and Shuichiro Ito
1212 Targeting IL-34 in chronic inflammation Emma L. Masteller and Brian R. Wong
1217 Protein kinase C inhibitors for immune disorders Amnon Altman and Kok-Fai Kong
1222 Histamine H4 receptor antagonists for the treatment of inflammatory disorders Wai L. Liu
Themed section: Pulmonary Disease Guest Editor: R James White 1226 Drug discovery in pulmonary arterial hypertension: attacking the enigmatic root of a deadly weed R. James White, Katie L. Lannan and Richard P. Phipps
1230 Thrombosis, platelets, microparticles and PAH: more than a clot Katie L. Lannan, Richard P. Phipps and R. James White
1236 Endpoints in PAH clinical trials in the era of combination therapy: How do we decide whether something is working without going bankrupt? Neil McGlinchey and Andrew J. Peacock
1241 Rescuing the BMPR2 signaling axis in pulmonary arterial hypertension James West, Eric Austin, Joshua P. Fessel, James Loyd and Rizwan Hamid
1246 Assessment of right ventricular responses to therapy in pulmonary hypertension Onno A. Spruijt, Harm-Jan Bogaard and Anton Vonk-Noordegraaf
1251 Inflammation in pulmonary hypertension: what we know and what we could logically and safely target first Sylvia Cohen-Kaminsky, Aurélie Hautefort, Laura Price, Marc Humbert and Frédéric Perros
1257 How do we measure pathology in PAH (lung and RV) and what does it tell us about the disease Rubin M. Tuder
REVIEWS (continued) INFORMATICS
1125 Systems mapping of genes controlling chemotherapeutic drug efficiency for cancer stem cells Weimiao Wu, Sisi Feng, Yaqun Wang, Ningtao Wang, Han Hao and Rongling Wu
POST SCREEN
1131 Exploratory toxicology as an integrated part of drug discovery. Part I: Why and how Jorrit J. Hornberg, Morten Laursen, Nina Brenden, Mikael Persson, Annemette V. Thougaard, Dorthe B. Toft and Tomas Mow
1137 Exploratory toxicology as an integrated part of drug discovery. Part II: Screening strategies Jorrit J. Hornberg, Morten Laursen, Nina Brenden, Mikael Persson, Annemette V. Thougaard, Dorthe B. Toft and Tomas Mow
1145 A potential role for GPR55 in the regulation of energy homeostasis Anna C. Simcocks, Lannie O’Keefe, Kayte A. Jenkin, Michael L. Mathai, Deanne H. Hryciw and Andrew J. McAinch
Themed section: Rheumatology/Mechanisms underlying inflammatort bone & joint disease Guest Editor: Costantino Pitzalis 1152 Pathogenesis of rheumatoid arthritis: from systemic autoimmunity to localised joint disease Costantino Pitzalis
1155 Novel immunological targets in rheumatic diseases: clues from current therapies Fulvio D’Acquisto, Lorenza Rattazzi, Giuseppa Piras and Maria Letteria Galuppo
1161 Peripheral and synovial mechanisms of humoral autoimmunity in rheumatoid arthritis Elisa Corsiero, Costantino Pitzalis and Michele Bombardieri
1166 Resolution of inflammation: examples of peptidergic players and pathways Tazeen J. Ahmed, Magdalena K. Kaneva, Costantino Pitzalis, Dianne Cooper and Mauro Perretti
1172 Cellular and molecular mechanisms of cartilage damage and repair Joanna C. Sherwood, Jessica Bertrand, Suzanne E. Eldridge and Francesco Dell’Accio
1178 Cellular and molecular mechanisms of bone damage and repair in inflammatory arthritis Catherine Swales and Afsie Sabokbar
1186 Resolution of inflammation: targeting GPCRs that interact with lipids and peptides Jenna L. Cash, Lucy V. Norling and Mauro Perretti
ScienceDirect
CONTENTS 2 Continued
DRUG DISCOVERY TODAY Editorial Editor: Steve Carney Content Development Managers: Sandra Korver and Jasmin Bakker Journal Manager: Herman Engelen Publisher: Jaap van Harten Editorial Enquiries: Drug Discovery Today Elsevier 32 Jamestown Road, London, NW1 7BY, UK Tel: +44 (0)20 7424 4200 Fax: +44 (0)1865 853067 Email: [email protected]
Themed section: Autoimmunity Guest Editor: Esteban Masuda and Donald G. Payan 1193 Targeting autoimmunity: strategies and tactics Esteban S. Masuda and Donald G. Payan ADVISORY EDITORIAL BOARD Jurgen Bajorath University of Bonn, Germany Walter Blackstock Experimental Therapeutics Centre, Singapore David Brayden University College Dublin, Ireland Paul Caron Integrated Profiling, USA David Cavalla Numedicus Ltd., UK David Clark Argenta Discovery, UK Dalia Cohen ALN Associates, USA Donald Daley Argenta Discovery, UK Sean Ekins ACT LLC and Collaborations in Chemistry, USA Hans-Peter Fischer GeneData, Switzerland Peter Ghazal University of Edinburgh, UK Christopher M. Hill Merck, USA Nick Hird Takeda Chemical Industries, Japan Enoch Huang Pfizer, USA Thomas Joos University of Tuebingen, Germany Vincent H.L. Lee Chinese University of Hong Kong, China David Lewin Yale University, USA Christopher A. Lipinski Melior Discovery, USA Lorenz Mayr AstraZeneca, UK Nick Meanwell Bristol-Myers Squibb, USA BK Muralidhara AstraZeneca, USA Mark Murcko Disruptive Biomedical, LLC, USA Fajun Nan Shanghai Institute of Materia Medica, China Pradeep Nathan Experimental Medicine, GSK and University of Cambridge Gitte Neubauer Cellzome, Germany Eric Neumann Clinical Semantics Group Consulting, USA Tim Peakman UK Biobank, UK Norton Peet Microbiotix, Inc., USA Manuel Peitsch Swiss Institute of Bioinformatics, Switzerland Kurt Rasmussen Eli Lilly and Co. Ltd. USA Janice Reichert Reichert Biotechnology Consulting LLC, MA, USA John Reidhaar-Olson Albert Einstein College of Medicine, New York, USA Mike Romanos Crescendo Biologics, Cambridge, UK Raymond C. Rowe Intelligensys, UK Andreas Russ University of Oxford, UK Esther Schmid EFS Strategy and Business Consulting, UK Jonathan Sheldon Translational Medicine, Oracle, UK Michael Snyder Stanford University, USA Susie Stephens Johnson & Johnson, USA Robert Strausberg Ludwig Institute for Cancer Research, New York, USA Yuichi Sugiyama University of Tokyo, Japan David Szymkowski Xencor, USA Nick Terrett Ensemble Discovery, USA Vladimir Torchilin Northeastern University, Boston, USA Mark Whittaker Evotec OAI, UK Hans Winkler Janssen Pharmaceutica, Belgium Limsoon Wong National University of Singapore X.F. Steven Zheng Robert Wood Johnson Medical School, USA
ScienceDirect
1195 PI3K inhibitors as potential therapeutics for autoimmune disease Jennifer Ball, Sophie Archer and Stephen Ward
1200 Bruton’s tyrosine kinase inhibitors for the treatment of rheumatoid arthritis Jennifer A. Whang and Betty Y. Chang
1205 Inhibiting ROR␥t/Th17 axis for autoimmune disorders Fujio Isono, Saori Fujita-Sato and Shuichiro Ito
1212 Targeting IL-34 in chronic inflammation Emma L. Masteller and Brian R. Wong
1217 Protein kinase C inhibitors for immune disorders Amnon Altman and Kok-Fai Kong
1222 Histamine H4 receptor antagonists for the treatment of inflammatory disorders Wai L. Liu
Themed section: Pulmonary Disease Guest Editor: R James White 1226 Drug discovery in pulmonary arterial hypertension: attacking the enigmatic root of a deadly weed R. James White, Katie L. Lannan and Richard P. Phipps
1230 Thrombosis, platelets, microparticles and PAH: more than a clot Katie L. Lannan, Richard P. Phipps and R. James White
1236 Endpoints in PAH clinical trials in the era of combination therapy: How do we decide whether something is working without going bankrupt? Neil McGlinchey and Andrew J. Peacock
1241 Rescuing the BMPR2 signaling axis in pulmonary arterial hypertension James West, Eric Austin, Joshua P. Fessel, James Loyd and Rizwan Hamid
1246 Assessment of right ventricular responses to therapy in pulmonary hypertension Onno A. Spruijt, Harm-Jan Bogaard and Anton Vonk-Noordegraaf
1251 Inflammation in pulmonary hypertension: what we know and what we could logically and safely target first Sylvia Cohen-Kaminsky, Aurélie Hautefort, Laura Price, Marc Humbert and Frédéric Perros
1257 How do we measure pathology in PAH (lung and RV) and what does it tell us about the disease Rubin M. Tuder