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Special Issue on Granular Knowledge Discovery

Dominik Ślȩzak, Andrzej Skowron, Yukio Ohsawa, Junzo Watada
2015 International Journal of Intelligent Decision Technologies  
In summary, we hope that this special issue shows a variety of ways of embedding data, information and knowledge granulation into Knowledge Discovery and Decision Support.  ...  Special Issue on Granular Knowledge Discovery Granular Computing becomes increasingly popular in modeling of intelligent systems.  ... 
doi:10.3233/idt-140225 fatcat:wnyffacfmzc45npwaxhydmgf3m

Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor

Chris Dockendorff, Omozuanvbo Aisiku, Lynn VerPlank, James R. Dilks, Daniel A. Smith, Susanna F. Gunnink, Louisa Dowal, Joseph Negri, Michelle Palmer, Lawrence MacPherson, Stuart L. Schreiber, Robert Flaumenhaft
2012 ACS Medicinal Chemistry Letters  
Discovery of 1,3-diaminobenzenes as selective inhibitors of platelet activation at the PAR1 receptor. ACS Medicinal Chemistry Letters 3(3): 232-237. Published Version  ...  Of these, compound 4 was selected as a starting point for SAR studies, as it showed acceptable potency in the primary assay measuring inhibition of dense granule release (IC 50 = 1−10 μM). 17 Importantly  ...  The best results were observed with electron-withdrawing or neutral lipophilic ortho groups, with the bromide substituent of compound 4 proving optimal, giving an IC 50 of 0.26 μM.  ... 
doi:10.1021/ml2002696 pmid:22408714 pmcid:PMC3297361 fatcat:5xxoz62yxbcqjngwlj7q5qkimm

A High-Content Biosensor-Based Screen Identifies Cell-Permeable Activators and Inhibitors of EGFR Function

Christophe Antczak, Jeni P. Mahida, Bhavneet Bhinder, Paul A. Calder, Hakim Djaballah
2012 Journal of Biomolecular Screening  
Taken together, our results validate this novel approach and demonstrate its utility in the discovery of novel kinase modulators with potential use in the clinic.  ...  For this purpose, we have used our recently optimized EGFR biosensor (EGFRB) assay to screen for modulators of EGFR activity.  ...  Alice Goodwin and the Commonwealth Foundation for Cancer Research, the Experimental Therapeutics Center of MSKCC, the William Randolph Hearst Fund in Experimental Therapeutics, the Lillian S.  ... 
doi:10.1177/1087057112446174 pmid:22573732 pmcid:PMC3615554 fatcat:7mgubgt2svgydpytuwrs637o3y

Table of Contents

2013 Acta Pharmaceutica Sinica B  
rate and tableting proper- ties of cefuroxime axetil by melt-granulated dispersion and surface adsorption Dispersion granules were prepared by using gelucire 50/13 and sylysia 350 as carriers of melt  ...  Chencheng Zhu, Ling Jing, Nengjiang Yu, Xuedong Yang and Yimin Zhao A new lignan and active compounds inhibiting NF-kB signaling pathway from Caulis Trachelospermi ................109 In vitro bioassays  ... 
doi:10.1016/s2211-3835(13)00026-9 fatcat:azq5uvekina3hewvodp2i7tdmi

Preface

Dominik Ślęzak, Andrzej Skowron
2014 Natural Computing  
Using the obtained framework for further acceleration of evolutionary-driven optimizations of information granulation models can be one of future steps in this area.  ...  In summary, we hope that this special issue illustrates how to utilize Information Granulation in practical applications related to modeling, classification and discovery, how to combine principles of  ... 
doi:10.1007/s11047-014-9480-3 pmcid:PMC4648981 fatcat:qt42evagmrae5e6xfxejtcqg7e

COMPUTER AIDED DRUG DEVELOPMENT (CADD) PROCESS AND SCREENING: HIGH THROUGHPUT SCREENING (HTS)

Lakhan D. Baheti*, Aditya R. Pachghare
2021 Zenodo  
Computer aided drug development (CADD) comprises of a broad range of theoretical and computational approaches, CADD method have a major role in modern drug discovery, design and development that plays  ...  From the last decade incremental developments in R&D processes, the selection of tools for optimizing the functionality and viability has become the important factor in early drug development and is said  ...  The typical role of CADD in drug discovery is to screen out large compound libraries into smaller clusters of predicted active compounds (Figure 1 ), enabling optimization of lead compounds by improving  ... 
doi:10.5281/zenodo.5636093 fatcat:4szxnq5mb5gibpvsd4q5r5sxey

Approximate Reasoning in MAS: Rough Set Approach

Andrzej Skowron
2006 2006 IEEE/WIC/ACM International Conference on Web Intelligence (WI 2006 Main Conference Proceedings)(WI'06)  
The research has been supported by the grant 3 T11C 002 26 from Ministry of Scientific Research and Information Technology of the Republic of Poland.  ...  Components involved in construction of concept approximation which are tuned in searching for sub-optimal models relative to MLP are called information granules.  ...  This research may also help us to develop strategies for discovery of ontologies relevant for compound concept approximation.  ... 
doi:10.1109/wi.2006.43 fatcat:ey4peluof5aorkc7hvzvwxmovi

Domain-Based Biosensor Assay to Screen for Epidermal Growth Factor Receptor Modulators in Live Cells

Christophe Antczak, Alun Bermingham, Paul Calder, Dmitry Malkov, Keming Song, John Fetter, Hakim Djaballah
2012 Assay and drug development technologies  
Upon activation of the receptor, EGFR function in live cells is measured by the number of green granules that form.  ...  Traditional drug discovery efforts have resulted in the approval of a handful of receptor tyrosine kinase (RTK) inhibitors; however, their discovery relied solely on screening recombinant kinases, often  ...  ACKNOWLEDGMENTS DISCLOSURE STATEMENT Dmitry Malkov, Keming Song, and John Fetter are employees of Sigma-Aldrich, the company selling the A549 EGFR biosensor cells.  ... 
doi:10.1089/adt.2011.423 pmid:22280060 pmcid:PMC3277729 fatcat:a7pnaslgo5fdhghylo3kf26rii

Approximate Reasoning in MAS: Rough Set Approach

Andrzej Skowron
2006 2006 IEEE/WIC/ACM International Conference on Intelligent Agent Technology  
The research has been supported by the grant 3 T11C 002 26 from Ministry of Scientific Research and Information Technology of the Republic of Poland.  ...  Components involved in construction of concept approximation which are tuned in searching for sub-optimal models relative to MLP are called information granules.  ...  This research may also help us to develop strategies for discovery of ontologies relevant for compound concept approximation.  ... 
doi:10.1109/iat.2006.38 dblp:conf/iat/Skowron06 fatcat:hceu4eympjem7cltvv4ipc73oa

New Perspectives on Chinese Herbal Medicine (Zhong-Yao) Research and Development

Si-Yuan Pan, Si-Bao Chen, Hong-Guang Dong, Zhi-Ling Yu, Ji-Cui Dong, Zhi-Xian Long, Wang-Fun Fong, Yi-Fan Han, Kam-Ming Ko
2011 Evidence-Based Complementary and Alternative Medicine  
Since the research and development of new chemical drugs remain time-consuming, capital-intensive and risky, much effort has been put in the search for alternative routes for drug discovery in China.  ...  Synthetic chemical drugs, while being efficacious in the clinical management of many diseases, are often associated with undesirable side effects in patients.  ...  formulae Matching of CHM Ingredients and molecular targets of disease Optimization of CHM-derived lead compound CHM-derived new chemical compound CHM-derived new chemical composition  ... 
doi:10.1093/ecam/neq056 pmid:21785622 pmcid:PMC3135515 fatcat:qf6fqjafqreylcrhivgtct34te

Novel Class of Potential Therapeutics that Target Ricin Retrograde Translocation

Veronika Redmann, Thomas Gardner, Zerlina Lau, Keita Morohashi, Dan Felsenfeld, Domenico Tortorella
2013 Toxins  
Quantitative analysis of the fluorescent granules provided the basis to discover compounds from a small chemical library (2080 compounds) with known bioactive properties.  ...  Stabilizing RTA E177Q egfp through the inclusion of proteasome inhibitor produced fluorescent peri-nuclear granules.  ...  Veronika Redmann and Thomas Gardner were supported in part by an USPHS Institutional Research Training Award AI07647.  ... 
doi:10.3390/toxins6010033 pmid:24366208 pmcid:PMC3920248 fatcat:brmihr7ehjboxjeuorybdmvkfi

Wisdom Technology: A Rough-Granular Approach [chapter]

Andrzej Jankowski, Andrzej Skowron
2009 Lecture Notes in Computer Science  
The system carries out a fine-grained, parallel search of possibilities. 4. The system exhibits a continual interplay of bottom-up and top-down processes. Primary literature  ...  Global information is encoded as statistics and dynamics of patterns over the system's components. 2. Randomness and probabilities are essential. 3.  ...  In searching for (sub)optimal solutions it is necessary to construct many compound granules using some specific operations such as generalization, specification or fusion.  ... 
doi:10.1007/978-3-642-04735-0_1 fatcat:nubs2htmkncsvnurxrezyiql5i

Interactive granular computing

Andrzej Skowron, Andrzej Jankowski, Soma Dutta
2016 Granular Computing  
In the paper, we emphasize the role of the rough set-based methods in IGrC.  ...  In Granular Computing (GrC), all such constructed and/or induced objects are called granules.  ...  , and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made.  ... 
doi:10.1007/s41066-015-0002-1 fatcat:qe77wrv72bgprofjlexot4cgx4

Interactive Granular Computing [chapter]

Andrzej Skowron, Andrzej Jankowski
2015 Lecture Notes in Computer Science  
In the paper, we emphasize the role of the rough set-based methods in IGrC.  ...  In Granular Computing (GrC), all such constructed and/or induced objects are called granules.  ...  , and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made.  ... 
doi:10.1007/978-3-319-25754-9_5 fatcat:5o3p7ezblvb4tgnymcf3shckoi

Development of a Cell-Based Fluorescence Polarization Biosensor Using Preproinsulin to Identify Compounds That Alter Insulin Granule Dynamics

Na Young Yi, Qingping He, Thomas B. Caligan, Ginger R. Smith, Lawrence J. Forsberg, Jay E. Brenman, Jonathan Z. Sexton
2015 Assay and drug development technologies  
We observed that bafilomycin, a vacuolar H + ATPase inhibitor and inhibitor of insulin granule formation, significantly increased mCherry FP in INS-1 cells with PPI-mCherry.  ...  FP substantially decreases when insulin is tightly packaged in the granules, and the homo-FRET decreases when insulin granule packaging is inhibited, resulting in increased FP.  ...  In conclusion, this insulin reporter system and HTS platform delivers a viable approach for phenotypic drug discovery for the identification of compounds that alter insulin granule packaging and insulin  ... 
doi:10.1089/adt.2015.665 pmid:26505612 pmcid:PMC4955689 fatcat:ymewvx2l6zdkha25gqo6wdcit4
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