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Pharmacology Research & Perspectives

Articles are published under the terms of the Creative Commons License as stated in the final article.

Cover image for Vol. 5 Issue 1

Editors: Darrell R. Abernethy & Andrew J. Lawrence

Online ISSN: 2052-1707

Associated Title(s): British Journal of Clinical Pharmacology, British Journal of Pharmacology

From Early Discovery to Clinical Evaluation: Pharmacology Research & Perspectives Advances Drug Discovery

Evaluation and publication of rigorous studies that support each stage of drug discovery and development are key to the mission of Pharmacology Research & Perspectives. After careful review, the papers in this virtual issue have been published in PR & P, and each provides useful and important understanding of the likelihood of success of “drugging” a potential drug target. This success is contingent on far more than a good idea, or a promising result from a molecular or cellular assay. In addition to those early discovery findings we publish studies in each step along the path to the realization of a drug that has efficacy for the treatment of human disease.

Darrell R. Abernethy, MD, PhD

Andrew Lawrence, PhD
Deputy Editor-in-Chief

Preclinical and translational evaluation of coagulation factor IXa as a novel therapeutic target
Wendy Ankrom, Harold B. Wood, Jiayi Xu, Wayne Geissler, Tom Bateman, Manash S. Chatterjee, Kung-I Feng, Joseph M. Metzger, Walter R. Strapps, Marija Tadin-Strapps, Dietmar Seiffert and Patrick Andre

Mitochondrial fission – a drug target for cytoprotection or cytodestruction?
Ayeshah A. Rosdah, Jessica K. Holien, Lea M. D. Delbridge, Gregory J. Dusting and Shiang Y. Lim

Pharmacological evaluation of a series of smoothened antagonists in signaling pathways and after topical application in a depilated mouse model
Emilie Lauressergues, Peter Heusler, Fabrice Lestienne, David Troulier, Isabelle Rauly-Lestienne, Amélie Tourette, Marie-Christine Ailhaud, Claudie Cathala, Stéphanie Tardif, Delphine Denais-Laliève, Marie-Thérèse Calmettes, Anne-Dominique Degryse, Antoine Dumoulin, Luc De Vries and Didier Cussac

In silico identified targeted inhibitors of P-glycoprotein overcome multidrug resistance in human cancer cells in culture
Courtney A. Follit, Frances K. Brewer, John G. Wise and Pia D. Vogel

Preclinical pharmacology and pharmacokinetics of CERC-301, a GluN2B-selective N-methyl-D-aspartate receptor antagonist
Rachel Garner, Shobha Gopalakrishnan, John A. McCauley, Rodney A. Bednar, Stanley L. Gaul, Scott D. Mosser, Laszlo Kiss, Joseph J. Lynch, Shil Patel, Christine Fandozzi, Armando Lagrutta, Richard Briscoe, Nigel J. Liverton, Blake M. Paterson, James J. Vornov and Reza Mazhari

Increased efficacy of VX-809 in different cellular systems results from an early stabilization effect of F508del-CFTR
Carlos M. Farinha, Marisa Sousa, Sara Canato, André Schmidt, Inna Uliyakina and Margarida D. Amaral

Saroglitazar, a novel PPARα/γ agonist with predominant PPARα activity, shows lipid-lowering and insulin-sensitizing effects in preclinical models
Mukul R. Jain, Suresh R. Giri, Chitrang Trivedi, Bibhuti Bhoi, Akshyaya Rath, Geeta Vanage, Purvi Vyas, Ramchandra Ranvir and Pankaj R. Patel

Pharmacodynamic assays to facilitate preclinical and clinical development of pre-mRNA splicing modulatory drug candidates
Yihui Shi, Amanda S. Joyner, William Shadrick, Gustavo Palacios, Chandraiah Lagisetti, Philip M. Potter, Lidia C. Sambucetti, Stefan Stamm and Thomas R. Webb

Natural compound methyl protodioscin protects against intestinal inflammation through modulation of intestinal immune responses
Rongli Zhang, Shila Gilbert, Xinsheng Yao, Jefferson Vallance, Kris Steinbrecher, Richard Moriggl, Dongsheng Zhang, Madhu Eluri, Haifeng Chen, Huiqing Cao, Noah Shroyer, Lee Denson and Xiaonan Han

Teleocidin A2 inhibits human proteinase-activated receptor 2 signaling in tumor cells
Sonja Stahn, Lisa Thelen, Ina-Maria Albrecht, Jens Bitzer, Thomas Henkel and Nicole Elisabeth Teusch

Preclinical evaluation of SMM-189, a cannabinoid receptor 2-specific inverse agonist
Chaela Presley, Ammaar Abidi, Satyendra Suryawanshi, Suni Mustafa, Bernd Meibohm and Bob M. Moore II

The discovery of a selective and potent A2a agonist with extended lung retention
Annika B. M. Åstrand, Eva Lamm Bergström, Hui Zhang, Lena Börjesson, Therese Söderdahl, Cecilia Wingren, Anne-Helene Jansson, Amir Smailagic, Camilla Johansson, Håkan Bladh, Igor Shamovsky, Anders Tunek and Tomas Drmota

Pharmacological characterization of a novel potent, selective, and orally active phosphodiesterase 10A inhibitor, PDM-042 [(E)-4-(2-(2-(5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazin-2-yl)vinyl)-6-(pyrrolidin-1-yl)pyrimidin-4-yl)morpholine] in rats: potential for the treatment of schizophrenia
Keita Arakawa, Shunsuke Maehara, Natsuko Yuge, Makoto Ishikawa, Yutaka Miyazaki, Hiroyasu Naba, Yutaka Kato and Kazunari Nakao

Inhibition of Let-7 microRNA attenuates myocardial remodeling and improves cardiac function postinfarction in mice
Anna-Maria Tolonen, Johanna Magga, Zoltán Szabó, Pirkko Viitala, Erhe Gao, Anne-Mari Moilanen, Pauli Ohukainen, Laura Vainio, Walter J. Koch, Risto Kerkelä, Heikki Ruskoaho and Raisa Serpi

Drofenine: a 2-APB analog with improved selectivity for human TRPV3
Cassandra E. Deering-Rice, Virginia K. Mitchell, Erin G. Romero, May H. Abdel Aziz, Daniel A. Ryskamp, David Križaj, Raj Gopal Venkat and Christopher A. Reilly