secondary assays for evaluating potential small molecule hits

... in human ASM for the discovery of potential small molecule therapeutic agents against airflow obstruction in asthma First, we screened a library of compounds that could act as small molecule modulators ... cyclodextrin as a vehicle for the delivery of small molecules Among the seven scaffolds which showed activity in the FP assay as small molecule analogs of pHSP20, only a small subset of compounds ... Screening small molecule modulators of pHSP20-14-3-3 g protein interactions Testing functional efficacy of small molecule analogs of pHSP20 C yc lo de xt rin inactive phosphorylated form as reported...

Ngày tải lên: 12/08/2014, 13:22

... reverse transcriptase assays (C) Mean values of five (panel A) or four (panel C) independent determinations are shown B and D: assays of viral infectivity HIV-1 and SIV were assayed for infectivity ... specific for SIV CA Panel B: effects of DSB on SIV infectivity Viral supernatants were assayed for infection of P4-CCR5 indicator cells Infectivity was calculated after normalizing for the RT ... relative to wild type HIV-1, possibly owing to the small but detectable reduction in infectivity observed for the mutant virus in single-round infection assays (Fig 2B) In additional studies, we observed...

Ngày tải lên: 13/08/2014, 13:20

... rotatable bonds for ordinary molecules, ligands and ligands with different protein-binding potentials Descriptor* PSA Small molecules† Average values Standard error Number of molecules Molecules 111.81 ... responsible for the differences between ligands and ordinary molecules, which is supported by the different average values of the four kinds of parameters for ligands and ordinary molecules (Table ... responsible for the strong protein-binding potential of the super ligands, which is supported by the different average values of the four kinds of parameters for ligands with different protein-binding potentials...

Ngày tải lên: 14/08/2014, 08:20

... siRNA knockdown studies Selective small molecule inhibitors for these ALDH isoenzymes are not currently available We hypothesized that novel and selective small molecule inhibitors of ALDH3A1 would ... tough times and the long distances Thanks for being there for me v Abstract Bibek Parajuli IDENTIFICATION, KINETIC AND STRUCTURAL CHARACTERIZATION OF SMALL MOLECULE INHIBITORS OF ALDEHYDE DEHYDROGENASE ... phenotypes Table 3A: SAR for CB29 analogs .61 Table 3B: SAR for CB29 analogs 62 Table 4: SAR for CB7 analogs 65 Table 5: Refinement statistics for CB29 bound to ALDH3A1...

Ngày tải lên: 24/08/2014, 09:51

... responsible for ensuring that individual replication forks fire only once during S-phase (11) Cyclin-dependent kinases (CDKs) directly prevent the formation of the pre-RC, and therefore the formation ... patients Therefore, targeting essential regulatory proteins that are required for both normal cell proliferation and the response to chemotherapeutic treatment has the potential for widespread ... sister, Josh and Jodi, for all of their love and support throughout the years iii ABSTRACT Sarah C Shuck Identification of novel small molecule inhibitors of proteins required for genomic maintenance...

Ngày tải lên: 24/08/2014, 11:28

... CHAPTER Introduction 1.1 Small Molecule Activation Small molecules are defined as molecules consisting of two to four atoms, such as CO, N2, H2O, O2, CO2 and H2 Certain small molecules, such as H2 ... metal compounds to coordinate to small molecules and alter their molecular and electronic structures makes them excellent candidates for the activation of small molecules Scheme 1.2 An example ... SPECTROSCOPIC STUDIES OF METAL CARBONYL COMPLEXES FOR SMALL MOLECULE ACTIVATION KEE JUN WEI (B.Sc (HONS), NUS) A THESIS SUBMITTED FOR THE DEGREE OF DOCTOR OF PHILOSOPHY DEPARTMENT OF CHEMISTRY...

Ngày tải lên: 08/09/2015, 19:33

... trastuzumab-functionalized NP formulation can be 1.215-, 1.215- and 1.073-fold more effective for MCF-7 cells, and 1.697-, 1.886and 1.126-fold more effective for SK-BR-3 cells than the NP formulation without ... trastuzumab on NP surface for targeted drug delivery Experiments were carried out to investigate the feasibility of the obtained NPs for targeted delivery of small molecule drugs The trastuzumab ... Figure 4-5 SDS-PAGE analysis of HER2 antibody: lane is for the molecular weight markers; lane 2-3 are for the native HER2 antibody; lane 4-7 are for the NP20-HER .100 Figure 4-6 In vitro drug release...

Ngày tải lên: 14/09/2015, 08:48

... Phosphorylation 1.4 Small Molecule Chemical Biology Tools for Studying Cellular Phosphorylation Events In vivo 1.4.1 Small- Molecule Mimetics of Phosphorylated Amino Acids 1.4.2 Activity Based Probes for Protein ... 1.4.5 Small- Molecule Environment-Sensitive Biosensors 26 1.4.6 Genetically Encoded Protein Biosensors for measurement of 30 In vivo Phosphorylation Event 1.4.7 Small- Molecule Microarray for High-Throughput ... signal transduction pathways in eukaryotes 1.4 Small Molecule Chemical Biology Tools for Studying Cellular Phosphorylation Events in vivo 1.4.1 Small- Molecule Mimetics of Phosphorylated Amino Acids...

Ngày tải lên: 04/10/2015, 15:45

... NANOPARTICLES OF BIODEGRADABLE POLYMERS FOR CONTROLLED AND TARGETED DELIVERY OF PROTEIN DRUGS SMALL AND MOLECULE DRUGS BY LEE SIE HUEY (B.Sc (Hons.), NUS) A THESIS SUBMITTED FOR THE DEGREE OF MASTER NANOENGINEERING ... of DOX in free form or formulated in the 0%, 20%, 33% and 50% TPGS-FOL nanoparticles (n=6) 78 Figure 5-8 (a) MCF-7 and (b) C6 cell uptake efficiency of DOX in free form or formulated in the ... demonstrated that PLA-TPGS nanoparticles for paclitaxel formulation have shown great advantages over Taxol and the PVAemulsifier PLGA nanoparticles formulation for oral delivery (Zhang and Feng, 2006b;...

Ngày tải lên: 26/11/2015, 22:41

... Conclusion By being aware of the aforementioned issues, ESL teachers can more effectively assess their students' writing Holistic evaluation is a useful tool that informs teachers and allows them ... a descriptive task, such as a student describing his or her country, may elicit a different performance than a student explaining the role of pets in America, which is more an expository writing ... Your Students' Backgrounds Writing clearly and adeptly is a learned skill that can be challenging for both native and nonnative English speakers ESL educators are aware that their students often...

Ngày tải lên: 06/09/2013, 05:10

... ports in one card reserved for local/ remote configuration, network, and timing management The remaining ports 64 A TESTBED FOR EVALUATING VoIP SERVICE can be used for BRI and/or T1 (CAS or PRI) ... A TESTBED FOR EVALUATING VoIP SERVICE Figure 5-1 Block diagram of a VoIP testbed The softswitch contains various VoIP CC functions, such as, H.323 GK, MGCP/H.248 MGC, and SIP servers for registration, ... worst match) technique Other 66 A TESTBED FOR EVALUATING VoIP SERVICE Figure 5-2 Sequence of interactions during a typical telephone conversation techniques for objective speech quality measurement...

Ngày tải lên: 30/09/2013, 07:20

... CDR data in a prespecified format for remote storage using standard protocols in the billing system or server for settlement of prices for regulatory 58 CRITERIA FOR EVALUATING VoIP SERVICE purposes ... 50 CRITERIA FOR EVALUATING VoIP SERVICE SERVICE REQUIREMENTS BEFORE CALL SETUP ATTEMPTS Two of the most important parameters of interest for VoIP even before a call setup attempt ... no more than sec for local calls, sec for toll calls, and sec for international calls, with 95% values of 6, 8, and 11 sec, respectively To deliver PSTN-grade call processing performance, the edge...

Ngày tải lên: 30/09/2013, 07:20

... encapsulation is used primarily for VPN connectivity for mobile users, teleworkers, small branch offices with two or less local subnets, or for overlaying IPSec for IP unicast data encryption ... be used for conferencing but only for G.711 calls Therefore, if G.729 is going to be used for calls over the WAN, then hardware-based digital signal processing (DSP) farms must be used for conferencing ... monitored • Before Release 12.3.8T, ACLs on the Internet perimeter were checked before and after encryption Release 12.3.8T removed this requirement See the following URL for more complete information...

Ngày tải lên: 21/12/2013, 06:16

... Transient Performance As noted, the transient performance characterization was performed with an input file containing an early steam generator tube bundle configuration, and therefore the following ... would provide a path for cooling the primary system Such an effective heat transfer mechanism may obviate the need for a sump makeup valve Therefore, a calculation was performed to evaluate the ... required for inventory for the situation where minimum inventory makeup capability is available Main Steam Line Break A Main Steam Line Break calculation was performed to investigate the potential...

Ngày tải lên: 16/01/2014, 22:20

... substrates for a variety of other NAD+-dependent enzymes Therefore, other methods, such as forward chemical genetics, have recently been used to screen for novel small molecule Sir2 regulators Forward ... important to point out that the in vitro assays were performed on whole cell extracts of an hst2 deletion yeast strain rather than purified ySir2 Therefore, 4611 Small molecule regulation of Sir2 protein ... extension has motivated the hunt for small molecule sirtuin activators that increase lifespan in yeast, with the potential promise of identifying such compounds for human use Utilizing a commercially...

Ngày tải lên: 20/02/2014, 01:20

... of nugget importance Exploring this thread of argument, we can formulate additional approaches for tackling these issues We could, for example, solicit more granular individual judgments on each ... at most once per run—i.e., a system is not rewarded for retrieving a nugget multiple times If the system’s output contains more than one match for a nugget, the best match is selected and the rest ... possible for assessors to consistently enumerate the total set of nuggets contained in an answer, which corresponds to the denominator in a precision calculation (Voorhees, 2003) Thus, a penalty for...

Ngày tải lên: 20/02/2014, 12:20

... domain, resulting in conformational activation of the substrate binding site and oxyanion hole required for proteolytic activity) [5–8] Our laboratory has been searching for small- molecule natural products ... identification and functional characterization of such small- molecule modulators of zymogen activation in the fibrinolytic and coagulation systems Table Small- molecule zymogen modulators identified in this ... alone cannot substitute for plasma, and the presence of a cofactor for the plactin action is suggested On cultured U937 cells, most of the u-PA molecules exist in the zymogen form, scuPA Upon treatment...

Ngày tải lên: 06/03/2014, 22:21

... performance on random data suggests using the nearest neighbor approach for experiments Nearest neighbor avoids evaluating on ‘easy’ datasets, and our baseline (at 79.5%) still provides room for ... training size when trained on either NYT or APW (the APW portion is smaller in total size, and the smaller BNC is provided for comparison) The first point on each line (the highest points) contains ... similar to each other Given two potential arguments for a verb, the correct one should correlate higher with the arguments observed with the verb during training Formally, given a verb v and a...

Ngày tải lên: 07/03/2014, 22:20

... accuracy for the whole predicate-argument structure the corpus to form a meta-evaluation corpus To maintain Note that wpred , wj and wpartial are the weights for the a controlled environment for experiments ... ARGM-TMP/temporal) only partially translated Assuming for now that the metric aggregates ten types of semantic roles with uniform weight for each role (optimization of weights will be discussed ... error analysis, and (b) potentially directly usable for automatic credit/blame assignment in tuning tree-structured SMT systems We also believe that to provide a foundation for better design of...

Ngày tải lên: 07/03/2014, 22:20