ChemInform Abstract: Use of Parallel-Synthesis Combinatorial Libraries for Rapid Identification of Potent FKBP12 Inhibitors.

ChemInform ◽  
2010 ◽  
Vol 33 (38) ◽  
pp. no-no
Author(s):  
Yong-Qian Wu ◽  
et al. et al.
2002 ◽  
Vol 12 (10) ◽  
pp. 1421-1428 ◽  
Author(s):  
Chi Choi ◽  
Jia-He Li ◽  
Mark Vaal ◽  
Christine Thomas ◽  
David Limburg ◽  
...  

2007 ◽  
Vol 9 (6) ◽  
pp. 1084-1093 ◽  
Author(s):  
Qian Li ◽  
Rachel M. Ndonye ◽  
Petr A. Illarionov ◽  
Karl O. A. Yu ◽  
Elliot S. Jerud ◽  
...  

2011 ◽  
Vol 13 (5) ◽  
pp. 466-477 ◽  
Author(s):  
Sarvesh Kumar ◽  
Thomas O. Painter ◽  
Benoy K. Pal ◽  
Benjamin Neuenswander ◽  
Helena C. Malinakova

ChemInform ◽  
2006 ◽  
Vol 37 (49) ◽  
Author(s):  
Andrey S. Trifilenkov ◽  
Vladimir V. Kobak ◽  
Marina A. Salina ◽  
Julya A. Kusovkova ◽  
Alexey P. Ilyin ◽  
...  

1996 ◽  
Vol 313 (1) ◽  
pp. 141-147 ◽  
Author(s):  
Sylvie E. BLONDELLE ◽  
Ema TAKAHASHI ◽  
Richard A. HOUGHTEN ◽  
Enrique PÉREZ-PAYÁ

We have combined the strength of our synthetic combinatorial library approach for the rapid identification of highly active compounds with prior knowledge of the relationship between the antimicrobial activities of individual peptides with specific induced conformations in order to identify new peptides with enhanced activity relative to a starting known antimicrobial sequence. In the current study, conformationally defined combinatorial libraries were generated based on an 18-mer antimicrobial peptide known to be induced into an α-helical conformation in a lipidic environment. Not only were novel sequences readily identified with 10-fold increases in activity, but detailed information about the structure-activity relationships of the peptides studied was also obtained during the deconvolution process. By using circular dichroism spectroscopy it was found that the individual 18-mer peptides could be induced into α-helical conformations on interaction with the cell lipid layer and/or sialic acids, which could result in bacterial cell lysis due to perturbation of the lipid packing of the cell wall.


1996 ◽  
Vol 118 (8) ◽  
pp. 2109-2110 ◽  
Author(s):  
Dale L. Boger ◽  
Christine M. Tarby ◽  
Peter L. Myers ◽  
Lynn Helena Caporale

2019 ◽  
Author(s):  
Meagan Beatty ◽  
Allison Selinger ◽  
YuQi Li ◽  
Fraser Hof

<div><div><div><p>We report here a parallel synthesis-driven approach to create a family of self-assembling dimeric sensors that we call DimerDyes, and its use for the rapid identification of salt-tolerant sensors for illicit drugs. We developed an efficient method that involves parallel synthesis and screening in crude form without the need to purify each potential sensor. Structurally diverse “hit” DimerDyes were re-synthesized, purified and were each shown to assemble into homodimers in water in the programmed way. DimerDyes provided a “turn-on” fluorescence detection of multiple illicit drugs at low micromolar concentrations in water and in saliva. The combination of multiple agents into a sensor array was successfully able to detect and discriminate between closely related drugs and metabolites in multiple important drug families. This report includes extensive NMR data on synthetic characterization, and on binding and assembly processes. It also includes UV-Vis and fluorescence spectroscopy data, and their use for quantitation and identification of drug-related analytes using multivariate statistical analysis. </p></div></div></div>


2001 ◽  
Vol 73 (7) ◽  
pp. 1033-1039 ◽  
Author(s):  
A. Ganesan

The fields of natural product total synthesis and combinatorial chemistry have major differences as well as much in common. Unique to combinatorial chemistry is the need to devise rapid and efficient methods for parallel synthesis and purification, while an area of overlap is the targeting of natural product scaffolds for combinatorial libraries. Both these aspects are illustrated with examples from our research.


2006 ◽  
Vol 8 (4) ◽  
pp. 469-479 ◽  
Author(s):  
Andrey S. Trifilenkov ◽  
Vladimir V. Kobak ◽  
Marina A. Salina ◽  
Julya A. Kusovkova ◽  
Alexey P. Ilyin ◽  
...  

ChemInform ◽  
2010 ◽  
Vol 33 (49) ◽  
pp. no-no
Author(s):  
Maria-Elena Theoclitou ◽  
Nancy G. J. Delaet ◽  
Leslie A. Robinson

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