Rapid Parallel Screening for Strain Optimization

2013 ◽  
Author(s):  
Chuck Merryman ◽  
Tony Yee
Keyword(s):  
Strain Optimization ◽  
Parallel Screening

scholarly journals Discovery and Optimization of Selective Inhibitors of Meprin α (Part I)

2021 ◽  
Vol 14 (3) ◽  
pp. 203 ◽  
Author(s):  
Shurong Hou ◽  
Juan Diez ◽  
Chao Wang ◽  
Christoph Becker-Pauly ◽  
Gregg B. Fields ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
De Novo ◽  
Selective Inhibitors ◽  
Preclinical Development ◽  
Starting Point ◽  
Good Starting Point ◽  
Parallel Screening ◽  
Low Cytotoxicity

Meprin α and β are zinc-dependent proteinases implicated in multiple diseases including cancers, fibrosis, and Alzheimer’s. However, until recently, only a few inhibitors of either meprin were reported and no inhibitors are in preclinical development. Moreover, inhibitors of other metzincins developed in previous years are not effective in inhibiting meprins suggesting the need for de novo discovery effort. To address the paucity of tractable meprin inhibitors we developed ultrahigh-throughput assays and conducted parallel screening of >650,000 compounds against each meprin. As a result of this effort, we identified five selective meprin α hits belonging to three different chemotypes (triazole-hydroxyacetamides, sulfonamide-hydroxypropanamides, and phenoxy-hydroxyacetamides). These hits demonstrated a nanomolar to micromolar inhibitory activity against meprin α with low cytotoxicity and >30-fold selectivity against meprin β and other related metzincincs. These selective inhibitors of meprin α provide a good starting point for further optimization.

Parallel screening for ALK, MET and ROS1 alterations in non-small cell lung cancer with implications for daily routine testing

Lung Cancer ◽  
2015 ◽  
Vol 87 (2) ◽  
pp. 122-129 ◽  
Author(s):  
Philipp Jurmeister ◽  
Dido Lenze ◽  
Erika Berg ◽  
Stefanie Mende ◽  
Frank Schäper ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Small Cell Lung Cancer ◽  
Cell Lung Cancer ◽  
Small Cell ◽  
Daily Routine ◽  
Small Cell Lung ◽  
Routine Testing ◽  
Parallel Screening

scholarly journals Probabilistic strain optimization under constraint uncertainty

2013 ◽  
Vol 7 (1) ◽  
pp. 29 ◽  
Author(s):  
Mona Yousofshahi ◽  
Michael Orshansky ◽  
Kyongbum Lee ◽  
Soha Hassoun
Keyword(s):  
Strain Optimization
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