Integration of RNAi and Small Molecule Screens to Identify Targets for Drug Development

2019 ◽  
pp. 33-42
Author(s):  
Konstantinos Drosopoulos ◽  
Spiros Linardopoulos
Keyword(s):  
Drug Development ◽  
Small Molecule

Drug Development of Small-Molecule Inhibitors of AD-Relevant Kinases as Novel Perspective Multitargeted Approach

2016 ◽  
Vol 13 (12) ◽  
pp. 1330-1336 ◽  
Author(s):  
V. Tell ◽  
I. Hilbrich ◽  
M. Holzer ◽  
Frank Totzke ◽  
Christoph Schachtele ◽  
...  
Keyword(s):  
Drug Development ◽  
Small Molecule ◽  
Small Molecule Inhibitors

scholarly journals Towards Academic Drug Development Guidelines

2019 ◽  
Author(s):  
Christopher Southan
Keyword(s):  
Drug Development ◽  
Success Rate ◽  
Case Studies ◽  
Small Molecule ◽  
Research Productivity ◽  
Medicinal Chemistry ◽  
Academic Development ◽  
Commercial Development ◽  
Small Molecule Drug

This report covers academic small-molecule drug development with a view to distilling guidelines. The first section covers research productivity feeding into commercial development before reviewing the literature on statistics of academic development It then considers differences between probes and drugs before discussing the role of author guidelines in medicinal chemistry and pharmacology journals. Resources for comprehensive compound and target cross-checking are then covered followed by comparisons between public and commercial databases including case studies of selected compounds. It concludes with an outline of new scientific developments that could increase the success rate of academic drug development.

scholarly journals Towards Academic Drug Development Guidelines

2019 ◽  
Author(s):  
Christopher Southan
Keyword(s):  
Drug Development ◽  
Success Rate ◽  
Case Studies ◽  
Small Molecule ◽  
Research Productivity ◽  
Medicinal Chemistry ◽  
Academic Development ◽  
Commercial Development ◽  
Small Molecule Drug

This report covers academic small-molecule drug development with a view to distilling guidelines. The first section covers research productivity feeding into commercial development before reviewing the literature on statistics of academic development It then considers differences between probes and drugs before discussing the role of author guidelines in medicinal chemistry and pharmacology journals. Resources for comprehensive compound and target cross-checking are then covered followed by comparisons between public and commercial databases including case studies of selected compounds. It concludes with an outline of new scientific developments that could increase the success rate of academic drug development.

scholarly journals A homogeneous SIRPα-CD47 cell-based, ligand-binding assay: Utility for small molecule drug development in immuno-oncology

PLoS ONE ◽  
2020 ◽  
Vol 15 (4) ◽  
pp. e0226661 ◽  
Author(s):  
Teresa L. Burgess ◽  
Joshua D. Amason ◽  
Jeffrey S. Rubin ◽  
Damien Y. Duveau ◽  
Laurence Lamy ◽  
...  
Keyword(s):  
Drug Development ◽  
Ligand Binding ◽  
Small Molecule ◽  
Binding Assay ◽  
Ligand Binding Assay ◽  
Small Molecule Drug

scholarly journals Xanthohumol Is a Potent Pan-Inhibitor of Coronaviruses Targeting Main Protease

2021 ◽  
Vol 22 (22) ◽  
pp. 12134
Author(s):  
Yuxi Lin ◽  
Ruochen Zang ◽  
Yanlong Ma ◽  
Zhuoya Wang ◽  
Li Li ◽  
...  
Keyword(s):  
Clinical Trials ◽  
Drug Development ◽  
Small Molecule ◽  
Drug Target ◽  
Antiviral Drug ◽  
High Morbidity ◽  
Lead Compound ◽  
Human Beings ◽  
Main Protease ◽  
Ic50 Value

Coronaviruses cause diseases in humans and livestock. The SARS-CoV-2 is infecting millions of human beings, with high morbidity and mortality worldwide. The main protease (Mpro) of coronavirus plays a pivotal role in viral replication and transcription, which, in theory, is an attractive drug target for antiviral drug development. It has been extensively discussed whether Xanthohumol is able to help COVID-19 patients. Here, we report that Xanthohumol, a small molecule in clinical trials from hops (Humulus lupulus), was a potent pan-inhibitor for various coronaviruses by targeting Mpro, for example, betacoronavirus SARS-CoV-2 (IC50 value of 1.53 μM), and alphacoronavirus PEDV (IC50 value of 7.51 μM). Xanthohumol inhibited Mpro activities in the enzymatical assays, while pretreatment with Xanthohumol restricted the SARS-CoV-2 and PEDV replication in Vero-E6 cells. Therefore, Xanthohumol is a potent pan-inhibitor of coronaviruses and an excellent lead compound for further drug development.

scholarly journals On the development of miransertib for rare diseases: an interview with ArQule's Brian Schwartz

2020 ◽  
Vol 2 (1) ◽  
pp. FDD27
Author(s):  
Brian Schwartz
Keyword(s):  
Drug Development ◽  
Precision Medicine ◽  
Small Molecule ◽  
Rare Diseases ◽  
Kinase Inhibitors ◽  
Clinical Stage ◽  
Proteus Syndrome ◽  
Biopharmaceutical Company

Brian Schwartz is CMO of ArQule, a clinical-stage biopharmaceutical company developing small-molecule kinase inhibitors for precision medicine oncology and rare diseases. In this interview he tells us more about the company's current projects, which include drug development for the rare diseases Proteus syndrome and PROS.

Associating Histopathological Findings with Drug-Induced Kidney Injury Rat Biomarkers in Small Molecule Drug Development—A Case Study

2017 ◽  
Vol 88 ◽  
pp. 213
Author(s):  
Andre Nogueira da Costa ◽  
Marcia Santos ◽  
Pierrette De Ron ◽  
Jean-Pierre Valentin ◽  
Renaud Fleurance ◽  
...  
Keyword(s):  
Drug Development ◽  
Small Molecule ◽  
Kidney Injury ◽  
Drug Induced ◽  
Histopathological Findings ◽  
Small Molecule Drug
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