scholarly journals Strategies for Transporter-targeted Drug Discovery

2021 ◽  
Vol 141 (4) ◽  
pp. 489-490
Author(s):  
Yoshinori Moriyama ◽  
Yasuo Shinohara
Keyword(s):  
Drug Discovery ◽  
Targeted Drug ◽  
Targeted Drug Discovery

scholarly journals Protein Interaction-Targeted Drug Discovery: Evaluating Critical Issues

BioTechniques ◽  
2002 ◽  
Vol 32 (3) ◽  
pp. 636-647 ◽  
Author(s):  
Erica A. Golemis ◽  
Kenneth D. Tew ◽  
Disha Dadke
Keyword(s):  
Drug Discovery ◽  
Protein Interaction ◽  
Critical Issues ◽  
Targeted Drug ◽  
Targeted Drug Discovery

scholarly journals Novel Insights of Structure-Based Modeling for RNA-Targeted Drug Discovery

2012 ◽  
Vol 52 (10) ◽  
pp. 2741-2753 ◽  
Author(s):  
Lu Chen ◽  
George A. Calin ◽  
Shuxing Zhang
Keyword(s):  
Drug Discovery ◽  
Targeted Drug ◽  
Targeted Drug Discovery

scholarly journals Artificial intelligence and big data facilitated targeted drug discovery

2019 ◽  
Vol 4 (4) ◽  
pp. 206-213 ◽  
Author(s):  
Benquan Liu ◽  
Huiqin He ◽  
Hongyi Luo ◽  
Tingting Zhang ◽  
Jingwei Jiang
Keyword(s):  
Artificial Intelligence ◽  
Big Data ◽  
Drug Discovery ◽  
Three Dimensional ◽  
Data Bank ◽  
The Cancer Genome Atlas ◽  
Biological Databases ◽  
Cancer Genome Atlas ◽  
Targeted Drug ◽  
Targeted Drug Discovery

Different kinds of biological databases publicly available nowadays provide us a goldmine of multidiscipline big data. The Cancer Genome Atlas is a cancer database including detailed information of many patients with cancer. DrugBank is a database including detailed information of approved, investigational and withdrawn drugs, as well as other nutraceutical and metabolite structures. PubChem is a chemical compound database including all commercially available compounds as well as other synthesisable compounds. Protein Data Bank is a crystal structure database including X-ray, cryo-EM and nuclear magnetic resonance protein three-dimensional structures as well as their ligands. On the other hand, artificial intelligence (AI) is playing an important role in the drug discovery progress. The integration of such big data and AI is making a great difference in the discovery of novel targeted drug. In this review, we focus on the currently available advanced methods for the discovery of highly effective lead compounds with great absorption, distribution, metabolism, excretion and toxicity properties.

Splice variants in the proteome: a promising and challenging field to targeted drug discovery

2015 ◽  
Vol 20 (3) ◽  
pp. 353-360 ◽  
Author(s):  
Raphael Tavares ◽  
Nicole M. Scherer ◽  
Carlos G. Ferreira ◽  
Fabricio F. Costa ◽  
Fabio Passetti
Keyword(s):  
Drug Discovery ◽  
Splice Variants ◽  
Targeted Drug ◽  
Targeted Drug Discovery

Abstract 1344: HMGA2-targeted drug discovery for breast cancer brain metastasis

2011 ◽  
Author(s):  
Riesa Burnett ◽  
Hitesh Appaiah ◽  
Poornima Bhat-Nakshatri ◽  
Jim Wikel ◽  
Peter Crooks ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Drug Discovery ◽  
Brain Metastasis ◽  
Breast Cancer Brain Metastasis ◽  
Targeted Drug ◽  
Targeted Drug Discovery

scholarly journals Teaching Targeted Drug Discovery and Development to Healthcare Professionals

2017 ◽  
Vol 11 (3) ◽  
pp. 277-282 ◽  
Author(s):  
Renee Fruchter ◽  
Meleha Ahmad ◽  
Michael Pillinger ◽  
Claudia Galeano ◽  
Bruce N. Cronstein ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Healthcare Professionals ◽  
Drug Discovery And Development ◽  
Targeted Drug ◽  
Targeted Drug Discovery

scholarly journals A High-Throughput Screening Platform Targeting PDLIM5 for Pulmonary Hypertension

2016 ◽  
Vol 21 (4) ◽  
pp. 333-341 ◽  
Author(s):  
Han Cheng ◽  
Tianji Chen ◽  
Merve Tor ◽  
Deborah Park ◽  
Qiyuan Zhou ◽  
...  
Keyword(s):  
Pulmonary Hypertension ◽  
Drug Discovery ◽  
Cell Line ◽  
High Throughput ◽  
High Throughput Screening ◽  
Pdz Domain ◽  
Luciferase Reporter ◽  
Targeted Drug ◽  
Screening Platform ◽  
Targeted Drug Discovery

Pulmonary arterial hypertension is a complex disease with multiple etiologic factors. PDLIM5, a member of the Enigma subfamily of PDZ and LIM domain protein family, contains an N-terminal PDZ domain and three LIM domains at its C-terminus. We have previously shown that overexpression of PDLIM5 prevents hypoxia-induced pulmonary hypertension (PH), and deletion of PDLIM5 in smooth muscle cells enhances hypoxia-induced PH in vivo. These results suggest that PDLIM5 may be a novel therapeutic target of PH. In this study, we aim to establish a high-throughput screening platform for PDLIM5-targeted drug discovery. We generated a stable mink lung epithelial cell line (MLEC) containing a transforming growth factor–β/Smad luciferase reporter with lentivirus-mediated suppression of PDLIM5 (MLEC-shPDLIM5) and measured levels of Smad2/3 and pSmad2/3. We found that in MLEC, suppression of PDLIM5 decreased Smad-dependent luciferase activity, Smad3, and pSmad3. We used MLEC-shPDLIM5 and a control cell line (MLEC-shCTL) to screen the Prestwick library (1200 compounds) and identified and validated paclitaxel as a PDLIM5 inhibitor in MLEC. Furthermore, we showed that paclitaxel inhibited Smad2 expression and Smad3 phosphorylation in A549 cells. Our study suggests that this system is robust and suitable for PDLIM5-targeted drug discovery.

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