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1

Gordon, Eric M., Ronald W. Barrett, William J. Dower, Stephen P. A. Fodor, and Mark A. Gallop. "Applications of Combinatorial Technologies to Drug Discovery. 2. Combinatorial Organic Synthesis, Library Screening Strategies, and Future Directions." Journal of Medicinal Chemistry 37, no. 10 (1994): 1385–401. http://dx.doi.org/10.1021/jm00036a001.

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2

GORDON, E. M., R. W. BARRETT, W. J. DOWER, S. P. A. FODOR, and M. A. GALLOP. "ChemInform Abstract: Applications of Combinatorial Technologies to Drug Discovery. Part 2. Combinatorial Organic Synthesis, Library Screening Strategies, and Future Directions." ChemInform 25, no. 39 (2010): no. http://dx.doi.org/10.1002/chin.199439303.

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3

Hamann, Andrew, Alvin K. Thomas, Tyler Kozisek, et al. "Screening a chemically defined extracellular matrix mimetic substrate library to identify substrates that enhance substrate-mediated transfection." Experimental Biology and Medicine 245, no. 7 (2020): 606–19. http://dx.doi.org/10.1177/1535370220913501.

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Nonviral gene delivery, though limited by inefficiency, has extensive utility in cell therapy, tissue engineering, and diagnostics. Substrate-mediated gene delivery (SMD) increases efficiency and allows transfection at a cell-biomaterial interface, by immobilizing and concentrating nucleic acid complexes on a surface. Efficient SMD generally requires substrates to be coated with serum or other protein coatings to mediate nucleic acid complex immobilization, as well as cell adhesion and growth; however, this strategy limits reproducibility and may be difficult to translate for clinical applicat
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4

Appell, Kenneth C., Thomas D. Y. Chung, Michael J. H. Ohlmeyer, Nolan H. Sigal, John J. Baldwin, and Daniel Chelsky. "Biological Screening of a Large Combinatorial Library." Journal of Biomolecular Screening 1, no. 1 (1996): 27–31. http://dx.doi.org/10.1177/108705719600100111.

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Encoding technology has allowed for the creation of libraries of 50,000 or more low-molecular-weight compounds for biological testing. The current challenge is to properly and efficiently screen among these compounds for useful biological activities. In this example, actives against two related G-protein coupled receptors were sought from a combinatorial library of 56,000 members. The library was synthesized on solid phase using the split synthesis method and photochemically released for testing. At a screening concentration of 0.5-1 /LM, 86 unique structures were identified as active against
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5

Pötzelberger, Isabella, Andrei Ionut Mardare, and Achim Walter Hassel. "Copper-nickel combinatorial library screening for electrocatalytic formaldehyde oxidation." physica status solidi (a) 214, no. 9 (2016): 1600552. http://dx.doi.org/10.1002/pssa.201600552.

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6

Chu, Yen-Ho, Xu Zang, and Jian Tu. "Affinity Capillary Electrophoresis: From Binding Measurement to Combinatorial Library Screening." Journal of the Chinese Chemical Society 45, no. 6 (1998): 713–20. http://dx.doi.org/10.1002/jccs.199800108.

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7

Poulsen, Sally-Ann. "Direct screening of a dynamic combinatorial library using mass spectrometry." Journal of the American Society for Mass Spectrometry 17, no. 8 (2006): 1074–80. http://dx.doi.org/10.1016/j.jasms.2006.03.017.

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8

Ramström, Olof, Lei Ye, and Klaus Mosbach. "Screening of a combinatorial steroid library using molecularly imprinted polymers." Analytical Communications 35, no. 1 (1998): 9–11. http://dx.doi.org/10.1039/a707876e.

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9

Doudican, Nicole A., Shireen Vali, Shweta Kapoor, et al. "Ex Vivo Patient-Specific Validation Of Personalized Therapeutic Designed For Multiple Myeloma." Blood 122, no. 21 (2013): 4219. http://dx.doi.org/10.1182/blood.v122.21.4219.4219.

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Abstract Background The unique signature of a patient’s tumor mandates the need to rationally design personalized therapies employing N=1 segmentation conceptually. Repurposing of existing drug agents with validated clinical safety and pharmacokinetics data provides a rapid translational path to clinic which otherwise would require years of development time and associated new chemical risks. By focusing on rationally designed personalized treatment mechanisms, our strategy targets multiple key pathways to address the clinical problem of emergence of single therapy resistance. In order to overc
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10

Shumate, Chris, Scott Beckey, Peter Coassin, and Harry Stylli. "Ultra-High Throughput Screening." Laboratory Automation News 2, no. 4 (1997): 24–29. http://dx.doi.org/10.1177/221106829700200406.

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Aurora Biosciences Corporation designs and develops proprietary drug discovery systems, services and technologies to accelerate and enhance the discovery of new pharmaceuticals. Aurora is developing an integrated technology platform centered around two technologies; 1) a portfolio of proprietary fluorescent assay technologies and, 2) an ultra-high throughput screening (“UHTS”) system designed to allow assay miniaturization and to overcome many of the limitations associated with the traditional drug discovery process. This approach takes advantage of the opportunities created by recent advances
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11

Sepetov, N. F., V. Krchnak, M. Stankova, S. Wade, K. S. Lam, and M. Lebl. "Library of libraries: approach to synthetic combinatorial library design and screening of "pharmacophore" motifs." Proceedings of the National Academy of Sciences 92, no. 12 (1995): 5426–30. http://dx.doi.org/10.1073/pnas.92.12.5426.

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12

Watanabe, Masaki, Takuji Kita, Tomoteru Fukumura, Akira Ohtomo, Kazunori Ueno, and Masashi Kawasaki. "High-Throughput Screening for Combinatorial Thin-Film Library of Thermoelectric Materials." Journal of Combinatorial Chemistry 10, no. 2 (2008): 175–78. http://dx.doi.org/10.1021/cc700094a.

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13

Wang, Yan, and Tingyu Li. "Screening of a Parallel Combinatorial Library for Selectors for Chiral Chromatography." Analytical Chemistry 71, no. 19 (1999): 4178–82. http://dx.doi.org/10.1021/ac9905017.

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14

Carney, Randy P., Yann Thillier, Zsofia Kiss, et al. "Combinatorial Library Screening with Liposomes for Discovery of Membrane Active Peptides." ACS Combinatorial Science 19, no. 5 (2017): 299–307. http://dx.doi.org/10.1021/acscombsci.6b00182.

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15

MacConnell, Andrew B., Alexander K. Price, and Brian M. Paegel. "An Integrated Microfluidic Processor for DNA-Encoded Combinatorial Library Functional Screening." ACS Combinatorial Science 19, no. 3 (2017): 181–92. http://dx.doi.org/10.1021/acscombsci.6b00192.

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16

Svensen, Nina, Juan José Díaz-Mochón, Kevin Dhaliwal, et al. "Screening of a Combinatorial Homing Peptide Library for Selective Cellular Delivery." Angewandte Chemie 123, no. 27 (2011): 6257–60. http://dx.doi.org/10.1002/ange.201101804.

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17

Svensen, Nina, Juan José Díaz-Mochón, Kevin Dhaliwal, et al. "Screening of a Combinatorial Homing Peptide Library for Selective Cellular Delivery." Angewandte Chemie International Edition 50, no. 27 (2011): 6133–36. http://dx.doi.org/10.1002/anie.201101804.

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18

Poulsen, Sally-Ann, Rohan A. Davis, and Timothy G. Keys. "Screening a natural product-based combinatorial library using FTICR mass spectrometry." Bioorganic & Medicinal Chemistry 14, no. 2 (2006): 510–15. http://dx.doi.org/10.1016/j.bmc.2005.08.030.

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19

Loch, Jennifer A., and Robert H. Crabtree. "Rapid screening and combinatorial methods in homogeneous organometallic catalysis." Pure and Applied Chemistry 73, no. 1 (2001): 119–28. http://dx.doi.org/10.1351/pac200173010119.

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Methods are discussed for rapid screening of soluble and polymer-bound homo-geneous catalysts for activity. A polymer-bound phosphine library is synthesized, and a modular tridentate pincer CNC bis-carbene Pd complex is described. The possibility of C-bound His in metalloenzymes is raised.
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20

MacConnell, Andrew B., and Brian M. Paegel. "Poisson Statistics of Combinatorial Library Sampling Predict False Discovery Rates of Screening." ACS Combinatorial Science 19, no. 8 (2017): 524–32. http://dx.doi.org/10.1021/acscombsci.7b00061.

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21

Pirrung, Michael C., and Jrlung Chen. "Preparation and Screening against Acetylcholinesterase of a Non-Peptide "Indexed" Combinatorial Library." Journal of the American Chemical Society 117, no. 4 (1995): 1240–45. http://dx.doi.org/10.1021/ja00109a007.

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22

Krauson, Aram J., Jing He, Andrew W. Wimley, Andrew R. Hoffmann, and William C. Wimley. "Synthetic Molecular Evolution of Pore-Forming Peptides by Iterative Combinatorial Library Screening." ACS Chemical Biology 8, no. 4 (2013): 823–31. http://dx.doi.org/10.1021/cb300598k.

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23

Appell, Kenneth C., Thomas D. Y. Chung, Kelli J. Solly, and Daniel Chelsky. "Biological Characterization of Neurokinin Antagonists Discovered Through Screening of a Combinatorial Library." Journal of Biomolecular Screening 3, no. 1 (1998): 19–27. http://dx.doi.org/10.1177/108705719800300103.

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Recent advances in combinatorial chemistry have resulted in the rapid screening of libraries against biological targets. Another advance in biological screening is the ability to design and utilize novel, automated, nonradioactive assays for targets of pharmaceutical interest. Using encoding technology and europium time-resolved fluorescence, we have designed primary receptor binding assays to define active compounds against the neurokinin-1 and neurokinin-2 receptor subtypes. In addition, a secondary, cell-based, functional assay measuring intracellular calcium flux with calcium sensitive flu
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24

Larsson, Rikard, Zhichao Pei, and Olof Ramström. "Catalytic Self-Screening of Cholinesterase Substrates from a Dynamic Combinatorial Thioester Library." Angewandte Chemie International Edition 43, no. 28 (2004): 3716–18. http://dx.doi.org/10.1002/anie.200454165.

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25

Camperi, Silvia A., Silvana L. Giudicessi, María C. Martínez‐Ceron, et al. "Combinatorial Library Screening Coupled to Mass Spectrometry to Identify Valuable Cyclic Peptides." Current Protocols in Chemical Biology 8, no. 2 (2016): 109–30. http://dx.doi.org/10.1002/cpch.2.

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26

Larsson, Rikard, Zhichao Pei, and Olof Ramström. "Catalytic Self-Screening of Cholinesterase Substrates from a Dynamic Combinatorial Thioester Library." Angewandte Chemie 116, no. 28 (2004): 3802–4. http://dx.doi.org/10.1002/ange.200454165.

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27

Reddy, M. Muralidhar, Rosemary Wilson, Johnnie Wilson, et al. "Identification of Candidate IgG Biomarkers for Alzheimer's Disease via Combinatorial Library Screening." Cell 144, no. 1 (2011): 132–42. http://dx.doi.org/10.1016/j.cell.2010.11.054.

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28

Gillies, Robert J., John M. Hoffman, Kit S. Lam, et al. "Meeting Report: High-Throughput Technologies for In Vivo Imaging Agents." Molecular Imaging 4, no. 2 (2005): 153535002005051. http://dx.doi.org/10.1162/15353500200505115.

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Combinatorial chemistry and high-throughput screening have become standard tools for discovering new drug candidates with suitable pharmacological properties. Now, those same technologies are starting to be applied to the problem of discovering novel in vivo imaging agents. Important differences in the biological and pharmacological properties needed for imaging agents, compared to those for a therapeutic agent, require new screening methods that emphasize those characteristics, such as optimized residence time and tissue specificity, that make for a good imaging agent candidate.
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29

Sun, Ted X., and G. E. Jabbour. "Combinatorial Screening and Optimization of Luminescent Materials and Organic Light-Emitting Devices." MRS Bulletin 27, no. 4 (2002): 309–15. http://dx.doi.org/10.1557/mrs2002.98.

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AbstractThe rapid development of modern photonic technologies—for example, mercury-free lamps, flat-panel displays, and solid-state lamps—demands the timely discovery of advanced phosphors. A combinatorial process has been developed to dramatically accelerate the experimental search for such phosphors. High-density phosphor “libraries” containing from 100 to over 1000 discrete chemical compositions on a 1 in. × 1 in. substrate have been made in thin-film or powder form using selective vapor deposition and liquid-dispensing techniques, respectively. In this article, the existing methods of comb
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30

Wu, Xianghong, Punit Upadhyaya, Miguel A. Villalona-Calero, Roger Briesewitz, and Dehua Pei. "Inhibition of Ras–effector interactions by cyclic peptides." MedChemComm 4, no. 2 (2013): 378–82. http://dx.doi.org/10.1039/c2md20329d.

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31

Prasher, Parteek, and Mousmee Sharma. "Tailored therapeutics based on 1,2,3-1H-triazoles: a mini review." MedChemComm 10, no. 8 (2019): 1302–28. http://dx.doi.org/10.1039/c9md00218a.

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32

Fujimori, Taketoshi, Peter Wirsching, and Kim D. Janda. "Preparation of a Kröhnke Pyridine Combinatorial Library Suitable for Solution-Phase Biological Screening." Journal of Combinatorial Chemistry 5, no. 5 (2003): 625–31. http://dx.doi.org/10.1021/cc0300208.

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33

Maclean, D., J. R. Schullek, M. M. Murphy, Z. J. Ni, E. M. Gordon, and M. A. Gallop. "Encoded combinatorial chemistry: Synthesis and screening of a library of highly functionalized pyrrolidines." Proceedings of the National Academy of Sciences 94, no. 7 (1997): 2805–10. http://dx.doi.org/10.1073/pnas.94.7.2805.

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34

Stern, Baruch, Galina Denisova, Dianna Buyaner, Daphna Raviv, and Jonathan M. Gershoni. "Helical epitopes determined by low‐stringency antibody screening of a combinatorial peptide library." FASEB Journal 11, no. 2 (1997): 147–53. http://dx.doi.org/10.1096/fasebj.11.2.9039957.

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35

Garaud, Mathieu, and Dehua Pei. "Substrate Profiling of Protein Tyrosine Phosphatase PTP1B by Screening a Combinatorial Peptide Library." Journal of the American Chemical Society 129, no. 17 (2007): 5366–67. http://dx.doi.org/10.1021/ja071275i.

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36

Vongvilai, Pornrapee, Marcus Angelin, Rikard Larsson, and Olof Ramström. "Dynamic Combinatorial Resolution: Direct Asymmetric Lipase-Mediated Screening of a Dynamic Nitroaldol Library." Angewandte Chemie International Edition 46, no. 6 (2007): 948–50. http://dx.doi.org/10.1002/anie.200603740.

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37

Vongvilai, Pornrapee, Marcus Angelin, Rikard Larsson, and Olof Ramström. "Dynamic Combinatorial Resolution: Direct Asymmetric Lipase-Mediated Screening of a Dynamic Nitroaldol Library." Angewandte Chemie 119, no. 6 (2007): 966–68. http://dx.doi.org/10.1002/ange.200603740.

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38

Choi, Hye-Ji, Ye-Jin Kim, Dong-Ki Choi, and Yong-Sung Kim. "Engineering of Immunoglobulin Fc Heterodimers Using Yeast Surface-Displayed Combinatorial Fc Library Screening." PLOS ONE 10, no. 12 (2015): e0145349. http://dx.doi.org/10.1371/journal.pone.0145349.

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39

Dikant, F., F. Gáplovský, and V. Garaj. "Virtual screening of combinatorial library of novel benzenesulfonamides on mycobacterial carbonic anhydrase II." European Pharmaceutical Journal 63, no. 2 (2016): 1–6. http://dx.doi.org/10.1515/afpuc-2016-0020.

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AbstractCombinatorial library of novel benzenesulfonamides was docked (Schrodinger Glide) into mycobacterial carbonic anhydrase (mtCA II) and human (hCA II) isoforms with an aim to find drug candidates with selective activity on mtCA II. The predicted selectivity was calculated based on optimized MM-GBSA free energies for ligand enzyme interactions. Selectivity, LogP (o/w) and interaction energy were used to calculate the selection index which determined the subset of best scoring molecules selected for further evaluation. Structure-activity relationship was found for fragment subsets, showing
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40

Shinoda, Satoshi, Keiko Yano, and Hiroshi Tsukube. "Combinatorial screening of a lanthanide complex library for luminescence sensing of amino acids." Chemical Communications 46, no. 18 (2010): 3110. http://dx.doi.org/10.1039/c000542h.

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41

Sankaranarayanan, Nehru Viji, Balaji Nagarajan та Umesh R. Desai. "Combinatorial Virtual Library Screening Study of Transforming Growth Factor-β2–Chondroitin Sulfate System". International Journal of Molecular Sciences 22, № 14 (2021): 7542. http://dx.doi.org/10.3390/ijms22147542.

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Transforming growth factor-beta (TGF-β), a member of the TGF-β cytokine superfamily, is known to bind to sulfated glycosaminoglycans (GAGs), but the nature of this interaction remains unclear. In a recent study, we found that preterm human milk TGF-β2 is sequestered by chondroitin sulfate (CS) in its proteoglycan form. To understand the molecular basis of the TGF-β2–CS interaction, we utilized the computational combinatorial virtual library screening (CVLS) approach in tandem with molecular dynamics (MD) simulations. All possible CS oligosaccharides were generated in a combinatorial manner to
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42

Chow, Mun Juinn, Mohammad Alfiean, Giorgia Pastorin, Christian Gaiddon, and Wee Han Ang. "Apoptosis-independent organoruthenium anticancer complexes that overcome multidrug resistance: self-assembly and phenotypic screening strategies." Chemical Science 8, no. 5 (2017): 3641–49. http://dx.doi.org/10.1039/c7sc00497d.

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43

Lavoie, R. Ashton, Alice di Fazio, Ruben G. Carbonell, and Stefano Menegatti. "Multiplexed Competitive Screening of One-Bead-One-Component Combinatorial Libraries Using a ClonePix 2 Colony Sorter." International Journal of Molecular Sciences 20, no. 20 (2019): 5119. http://dx.doi.org/10.3390/ijms20205119.

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Screening solid-phase combinatorial libraries of bioactive compounds against fluorescently labeled target biomolecules is an established technology in ligand and drug discovery. Rarely, however, do screening methods include comprehensive strategies—beyond mere library blocking and competitive screening—to ensure binding selectivity of selected leads. This work presents a method for multiplexed solid-phase peptide library screening using a ClonePix 2 Colony Picker that integrates (i) orthogonal fluorescent labeling for positive selection against a target protein and negative selection against c
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44

Li, Jinyang, Helge S. Stein, Kirill Sliozberg, et al. "Combinatorial screening of Pd-based quaternary electrocatalysts for oxygen reduction reaction in alkaline media." Journal of Materials Chemistry A 5, no. 1 (2017): 67–72. http://dx.doi.org/10.1039/c6ta08088j.

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45

Bawazer, Lukmaan A., Ciara S. McNally, Christopher J. Empson, et al. "Combinatorial microfluidic droplet engineering for biomimetic material synthesis." Science Advances 2, no. 10 (2016): e1600567. http://dx.doi.org/10.1126/sciadv.1600567.

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Although droplet-based systems are used in a wide range of technologies, opportunities for systematically customizing their interface chemistries remain relatively unexplored. This article describes a new microfluidic strategy for rapidly tailoring emulsion droplet compositions and properties. The approach uses a simple platform for screening arrays of droplet-based microfluidic devices and couples this with combinatorial selection of the droplet compositions. Through the application of genetic algorithms over multiple screening rounds, droplets with target properties can be rapidly generated.
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46

Silen, Joy L., Amy T. Lu, Dennis W. Solas, et al. "Screening for Novel Antimicrobials from Encoded Combinatorial Libraries by Using a Two-Dimensional Agar Format." Antimicrobial Agents and Chemotherapy 42, no. 6 (1998): 1447–53. http://dx.doi.org/10.1128/aac.42.6.1447.

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ABSTRACT A sensitive lawn-based format has been developed to screen bead-tethered combinatorial chemical libraries for antimicrobial activity. This method has been validated with beads linked to penicillin V via a photocleavable chemical linker in several analyses including a spike-and-recover experiment. The lawn-based screen sensitivity was modified to detect antibacterial compounds of modest potency, and a demonstration experiment with a naive combinatorial library of over 46,000 individual triazines was evaluated for antibacterial activity. Numerous hits were identified, and both active an
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47

Tu, Jian, Zhiguang Yu, and Yen-Ho Chu. "Combinatorial search for diagnostic agents: Lyme antibody H9724 as an example." Clinical Chemistry 44, no. 2 (1998): 232–38. http://dx.doi.org/10.1093/clinchem/44.2.232.

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Abstract Two peptide libraries, Ac-MXXXXXBBRM and Ac-VXXXXXBBRM, were constructed on TentaGel solid support to search for ligands that bind tightly with the H9724 Lyme antibody. By using an on-bead ELISA, approximately 120 ligands were selected as candidates for further study. Matrix-assisted laser desorption ionization mass spectrometry analysis of the candidate ligands indicated a high rate of occurrence of certain amino acids at the randomized positions. On the basis of the initial screening results, a small library was designed and iteratively synthesized. Subsequent library screenings led
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48

Oldenburg, Kevin R., Kham T. Vo, Beatrice Ruhland, Peter J. Schatz, and Zhengyu Yuan. "A Dual Culture Assay for Detection of Antimicrobial Activity." Journal of Biomolecular Screening 1, no. 3 (1996): 123–30. http://dx.doi.org/10.1177/108705719600100305.

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Combinatorial chemistry has opened a new realm of chemical diversity in the search for useful therapeutics as well as the ability to generate chemical libraries of hundreds of thousands to millions of discrete compounds. For the biologist, the goal is to screen these large libraries quickly and to obtain as much information in the primary screen as possible. Ideally, a primary screen would not only identify potential lead compounds but also yield information about the specificity, toxicity, and potency of that compound. Toward this end, a primary screen has been developed in which two organism
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Xiong, Xiahui, Yabin Lu, Lishu Zhang, et al. "Discovery of Novel Cell Proliferation-Enhancing Gene by Random siRNA Library Based Combinatorial Screening." Combinatorial Chemistry & High Throughput Screening 13, no. 9 (2010): 798–806. http://dx.doi.org/10.2174/138620710792927420.

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50

Gordeev, Mikhail F., Dinesh V. Patel, Bruce P. England, Supriya Jonnalagadda, Jesse D. Combs, and Eric M. Gordon. "Combinatorial synthesis and screening of a chemical library of 1,4-dihydropyridine calcium channel blockers." Bioorganic & Medicinal Chemistry 6, no. 7 (1998): 883–89. http://dx.doi.org/10.1016/s0968-0896(98)00048-0.

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