Literature DB >> 25630223

Target engagement in lead generation.

Timothy B Durham1, Maria-Jesus Blanco1.   

Abstract

The pharmaceutical industry is currently facing multiple challenges, in particular the low number of new drug approvals in spite of the high level of R&D investment. In order to improve target selection and assess properly the clinical hypothesis, it is important to start building an integrated drug discovery approach during Lead Generation. This should include special emphasis on evaluating target engagement in the target tissue and linking preclinical to clinical readouts. In this review, we would like to illustrate several strategies and technologies for assessing target engagement and the value of its application to medicinal chemistry efforts.
Copyright © 2015. Published by Elsevier Ltd.

Entities:  

Keywords:  Bioluminescent imaging (BLI); Biomarker; Cellular thermal shift assay (CETSA); Lead Generation; Positron emission tomography (PET); Receptor occupancy (RO); Target engagement

Mesh：

Substances：

Year:  2015        PMID： 25630223     DOI： 10.1016/j.bmcl.2014.12.076

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  32 in total

1.  Mouse Models of Lung Fibrosis.

Authors:  Olivia Mekhael; Safaa Naiel; Megan Vierhout; Aaron I Hayat; Spencer D Revill; Soumeya Abed; Mark D Inman; Martin R J Kolb; Kjetil Ask
Journal:  Methods Mol Biol       Date:  2021

2.  Development of inverse electron demand Diels-Alder ligation and TR-FRET assays for the determination of ligand-protein target occupancy in live cells.

Authors:  Jasmina Marjanovic; Aleksandra Baranczak; Violeta Marin; Henning Stockmann; Paul L Richardson; Anil Vasudevan
Journal:  Medchemcomm       Date:  2017-02-21       Impact factor: 3.597

3.  New Chemical Modalities and Strategic Thinking in Early Drug Discovery.

Authors:  Maria-Jesus Blanco; Kevin M Gardinier
Journal:  ACS Med Chem Lett       Date:  2020-01-14       Impact factor: 4.345

4.  Quantifying the relationship between inhibition of VEGF receptor 2, drug-induced blood pressure elevation and hypertension.

Authors:  Teresa Collins; Kelly Gray; Michal Bista; Matt Skinner; Christopher Hardy; Haiyun Wang; Jerome T Mettetal; Alexander R Harmer
Journal:  Br J Pharmacol       Date:  2018-01-18       Impact factor: 8.739

5.  Photoaffinity Probe Reveals the Potential Target of Harringtonolide for Cancer Cell Migration Inhibition.

Authors:  Tian-Yu Zhu; Xiu-Tao Wu; Chen Chen; Xiao-Qin Liu; Li Zhu; Jian-Guang Luo; Ling-Yi Kong
Journal:  ACS Med Chem Lett       Date:  2022-02-02       Impact factor: 4.345

6.  Designing a Small Fluorescent Inhibitor to Investigate Soluble Epoxide Hydrolase Engagement in Living Cells.

Authors:  Steffen Brunst; Julia Schönfeld; Peter Breunig; Luisa D Burgers; Murphy DeMeglio; Johanna H M Ehrler; Felix F Lillich; Lilia Weizel; Jasmin K Hefendehl; Robert Fürst; Ewgenij Proschak; Kerstin Hiesinger
Journal:  ACS Med Chem Lett       Date:  2022-06-14       Impact factor: 4.632

7.  Quantitative imaging of receptor-ligand engagement in intact live animals.

Authors:  Alena Rudkouskaya; Nattawut Sinsuebphon; Jamie Ward; Kate Tubbesing; Xavier Intes; Margarida Barroso
Journal:  J Control Release       Date:  2018-07-20       Impact factor: 9.776

8.  Increased platelet mitochondrial respiration after cardiac arrest and resuscitation as a potential peripheral biosignature of cerebral bioenergetic dysfunction.

Authors:  Michael A Ferguson; Robert M Sutton; Michael Karlsson; Fredrik Sjövall; Lance B Becker; Robert A Berg; Susan S Margulies; Todd J Kilbaugh
Journal:  J Bioenerg Biomembr       Date:  2016-03-28       Impact factor: 2.945

9.  The Alzheimer's disease drug candidate J147 decreases blood plasma fatty acid levels via modulation of AMPK/ACC1 signaling in the liver.

Authors:  Devin Kepchia; Ling Huang; Antonio Currais; Zhibin Liang; Wolfgang Fischer; Pamela Maher
Journal:  Biomed Pharmacother       Date:  2022-01-17       Impact factor: 6.529

Review 10.  Miniproteins as a Powerful Modality in Drug Development.

Authors:  Zachary R Crook; Natalie W Nairn; James M Olson
Journal:  Trends Biochem Sci       Date:  2020-01-31       Impact factor: 14.264
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