contents page 1

REVIEWS FOUNDATION 8 Tailoring chronic pain treatments for the elderly: are we prepared for the challenge? Stephen P. Arneric, Jennifer M.A. Laird, Amy S. Chappell and Jeffrey D. Kennedy 18 Thymoquinone: fifty years of success in the battle against cancer models Regine Schneider-Stock, Isabelle H. Fakhoury, Angela M. Zaki, Chirine O. El-Baba and Hala U. Gali-Muhtasib KEYNOTE 31 Toward the practical implementation of eye-related bioavailability prediction models Ivan Pepić, Jasmina Lovrić, Biserka Cetina-C ˇ ižmek, Stephan Reichl and Jelena Filipović-Grc ˇić INFORMATICS 45 Fragment-based error estimation in biomolecular modeling John C. Faver and Kenneth M. Merz Jr. POST SCREEN 51 Current strategies for inhibiting FGFR activities in clinical applications: opportunities, challenges and toxicological considerations Han Kiat Ho, Angie Hui Ling Yeo, Tse Siang Kang and Boon Tin Chua 63 Human pregnane X receptor: a novel target for anticancer drug development Vijay Rathod, Sumit Jain, Prajwal Nandekar and Abhay T. Sangamwar 71 Strategies and validation for siRNA-based therapeutics for the reversal of multi-drug resistance in cancer Tahereh Fatemian, Iekhsan Othman and Ezharul Hoque Chowdhury 79 Chemistry-enabled drug delivery (prodrugs): recent progress and challenges Sophie-Dorothee Clas, Rosa I. Sanchez and Rebecca Nofsinger 88 Biofunctionalisation of electrically conducting polymers Catalina Vallejo-Giraldo, Adriona Kelly and Manus J.P. Biggs 95 Hydrogen/deuterium exchange mass spectrometry for probing higher order structure of protein therapeutics: methodology and applications Hui Wei, Jingjie Mo, Li Tao, Reb J. Russell, Adrienne A. Tymiak, Guodong Chen, Roxana E. Iacob and John R. Engen CONTENTS 1 January 2014 Volume 19 Number 1 pp. 1–104 Cover Story The leading story of this issue of Drug Discovery Today by Stephen P. Arneric, Jennifer M.A. Laird, Amy S. Chappell and Jeffrey D. Kennedy entitled “Tailoring Chronic Pain Treatments for the Elderly: Are We Prepared for the Challenge?” details how Chronic pain is increasingly recognized as a disease and accounts for substantial suffering and disability world-wide. It questions whether a shift in the drug discovery paradigm will be necessary to improve efficacy, side-effects or positively impact quality of life (QoL) in the elderly with chronic pain? This short review further highlights a number of potential pitfalls, that should be considered when delivering valued pain relief medicines tailored for the elderly. ScienceDirect

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REVIEWS

FOUNDATION

8 Tailoring chronic pain treatments for the elderly: are we prepared for the challenge?Stephen P. Arneric, Jennifer M.A. Laird, Amy S. Chappell and Jeffrey D. Kennedy

18 Thymoquinone: fi fty years of success in the battle against cancer modelsRegine Schneider-Stock, Isabelle H. Fakhoury, Angela M. Zaki, Chirine O. El-Baba and Hala U. Gali-Muhtasib

KEYNOTE

31 Toward the practical implementation of eye-related bioavailability prediction modelsIvan Pepic, Jasmina Lovric, Biserka Cetina-Cižmek, Stephan Reichl and Jelena Filipovic-Grcic

INFORMATICS

45 Fragment-based error estimation in biomolecular modelingJohn C. Faver and Kenneth M. Merz Jr.

POST SCREEN

51 Current strategies for inhibiting FGFR activities in clinical applications: opportunities, challenges and toxicological considerationsHan Kiat Ho, Angie Hui Ling Yeo, Tse Siang Kang and Boon Tin Chua

63 Human pregnane X receptor: a novel target for anticancer drug developmentVijay Rathod, Sumit Jain, Prajwal Nandekar and Abhay T. Sangamwar

71 Strategies and validation for siRNA-based therapeutics for the reversal of multi-drug resistance in cancerTahereh Fatemian, Iekhsan Othman and Ezharul Hoque Chowdhury

79 Chemistry-enabled drug delivery (prodrugs): recent progress and challengesSophie-Dorothee Clas, Rosa I. Sanchez and Rebecca Nofsinger

88 Biofunctionalisation of electrically conducting polymersCatalina Vallejo-Giraldo, Adriona Kelly and Manus J.P. Biggs

95 Hydrogen/deuterium exchange mass spectrometry for probing higher order structure of protein therapeutics: methodology and applicationsHui Wei, Jingjie Mo, Li Tao, Reb J. Russell, Adrienne A. Tymiak, Guodong Chen, Roxana E. Iacob

and John R. Engen

CONTENTS 1

January 2014 Volume 19 Number 1 pp. 1 – 104

Cover StoryThe leading story of this issue of Drug Discovery Today by Stephen P. Arneric, Jennifer M.A. Laird, Amy S. Chappell and Jeffrey D. Kennedy entitled “Tailoring Chronic Pain Treatments for the Elderly: Are We Prepared for the Challenge?” details how Chronic pain is increasingly recognized as a disease and accounts for substantial suffering and disability world-wide. It questions whether a shift in the drug discovery paradigm will be necessary to improve effi cacy, side-effects or positively impact quality of life (QoL) in the elderly with chronic pain? This short review further highlights a number of potential pitfalls, that should be considered when delivering valued pain relief medicines tailored for the elderly.

ScienceDirect

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