target validation for biopharmaceutical drug discovery

... drug interactions To add on to the list is the emerging drug resistance that further complicates the disease management The urgent need for new antiTB drugs drives the search for novel drug targets ... tuberculosis ClpC1: A POTENTIAL TARGET FOR TUBERCULOSIS DRUG DISCOVERY MELIANA RIWANTO (B.Sc.(Pharm) (Hons.), National University of Singapore) A THESIS SUBMITTED FOR THE DEGREE OF MASTER OF SCIENCE ... caused by TB and the lack of new drugs in the market makes it imperative to have new anti-TB drugs with novel biological target However, no new anti-TB drugs with novel target have been discovered...

Ngày tải lên: 26/11/2015, 22:38

... is for a gene to code for multiple proteins What if someone applies for a patent for a gene that expresses a particular protein and someone else applies for a patent for the same gene coding for ... and informed him that his friend was insane: he had been employing men for nearly a month in battering stones to bits, and if he had any friendship for the gentleman, he ought certainly to inform ... worker for trying to form a union generally has the upper hand That also applies to jobs covered by labor laws Ac20 cording to Human Rights Watch, the financial penalty for firing a worker for orgaPRIVATE-SECTOR...

Ngày tải lên: 12/05/2014, 16:09

... equatorial conformers for the dierent force elds All force elds correctly predict the equatorial Molecular Mechanics and Comparison of Force Fields Figure Calculated equatorialaxial conformational ... different force elds to reproduce conformational energies The relative performance of the ability to reproduce geometries is not included as this is done reasonably well by most force elds The force ... 90% Data for most force elds were taken from the literature [30,35] Updated and newly determined results can be found in Appendix A The mean absolute errors (MAEs) for each force eld and for three...

Ngày tải lên: 12/05/2014, 17:28

... Novel drugs and Circumventing drug infections annually resistance Safe, orally bioavailable drugs, especially for the visceral form of the disease Safe, orally bioavailable drugs, especially for ... and describes the in silico drug discovery activities against potential malarial targets Drugs against all diseases Drugs against neglected diseases Figure 1: Number of drugs developed against neglected ... confer reduced sensitivity to a given drug or class of drugs For some drugs, only a single point mutation is required to confer resistance, while for other drugs, multiple mutations appear to be...

Ngày tải lên: 02/07/2014, 13:13

... Here, we investigated whether CD134 can be used as a target for specific drug delivery to activated auto-aggressive CD4+ T cells in arthritis For this purpose, the rat adjuvant arthritis (AA) model ... studied drug delivery to CD134+ T cells both in vitro and in vivo using liposomes coated with a CD134-directed monoclonal antibody (mAb) as a drug targeting system To investigate the possibility for ... for investigating in vitro binding and internalization contained 0.1 mol% Texas red-phosphatidylethanolamine (Molecular Probes Europe) Liposomes used for studying drug delivery in vitro and for...

Ngày tải lên: 09/08/2014, 06:22

... limitations of the current one -drug- one -target paradigm in drug discovery [79,86] Therefore, more and more efforts are devoted to finding new therapeutics aimed at multiple targets [86], which is becoming ... these old 'safe' drugs, which supports an increasingly shared notion in drug development that the most fruitful basis for the discovery of a new drug is to start with an old drug [83-85] Another ... that the US Food and Drug Administration (FDA) has approved approximately 2,000 drugs (chemical entities) and there exist only 2,000-3,000 druggable genes and 600-1,500 drug targets [81,82], it...

Ngày tải lên: 14/08/2014, 08:20

Ngày tải lên: 14/11/2014, 06:18

... COMPUTATIONAL METHODS IN DRUG DISCOVERY INTRODUCTION Figure 1.1 Stages of drug discovery and development Before work is started to discover any potential new medicine for a specific disease, scientists ... a particular therapeutic target in the search for a treatment for Dengue The Dengue RNA-dependent RNA polymerase (RdRp) was chosen as the target since it is critical for the replication of the ... be applied for the selection and prioritization of compounds in drug discovery The research work has been allocated into four parts, each catering to a different stage of the drug discovery process...

Ngày tải lên: 08/09/2015, 22:12

... 42 1.3.1 Metabolomics for quality control of medicinal plants 44 1.3.2 Metabolomics and analysis of pharmacological effects 45 1.3.3 Using metabolomics for drug discovery from medicinal ... HPLC 60 3.1.3.8 Sample preparation for amyrin quantification 61 3.1.3.9 GC-MS assay for amyrin quantification 61 3.1.3.10 Method validation for GC-MS assay 62 3.1.4 Results and ... responsible for the anticoagulant activity in extracts of A elliptica As the conventional process of repeated fractionation is a tedious process for the discovery of bioactive components, a platform...

Ngày tải lên: 10/09/2015, 08:25

... 1.2 Bioinformatics and cheminformatics in drug discovery 1.3 Introduction of bioinformatics and cheminformatics database development 11 1.4 Overview of virtual screening in drug discovery ... targets and drugs Owing to the effort of target discovery, hundreds of success targets and more than 1000 research targets have been identified [58-61] There are several well known target and drug databases ... successful drug from initial design to market Although a log of efforts have been made for drug discovery, the successful drugs did not increase significantly over the past few decades Bioinformatics...

Ngày tải lên: 10/09/2015, 09:04

... 1.2.1 Discovery of anti-mycobacterial drugs 1.2.2 Ideal drug candidates 1.2.3 Drug development pipeline 1.2.4 Combination therapy 1.2.5 Challenges in TB drug discovery ... of drug discovery and development of treatment regimens for TB Reprinted from Ma et al (2010), with permission from Elsevier Figure Global tuberculosis drug pipeline With permission of Oxford ... and night sweats Treatment for active, drug- sensitive TB consists of medicines known as first-line drugs and is administered for a period of months [a combination of drugs (rifampicin, isoniazid,...

Ngày tải lên: 22/09/2015, 15:17

... of additional substance such as drugs (Shappell, 2003) Therefore, metabolic-based cell viability assay may not be suitable for the drug discovery tool since the drug tested may cause alteration ... as a building block of a discovery tool for anti-fibrotic drugs Graduate Program in Bioengineering vi List of Tables List of Tables Table 3.1 The filter configurations for Olympus IX-71 fluorescence ... fibroblasts Therefore, the assessment of anti-fibrotic drugs usually employs fibroblast culture to determine the effect of the drug on the cell proliferation and collagen deposition Unfortunately,...

Ngày tải lên: 09/10/2015, 11:07

... their function In sum, either as a model for drug discovery or implant testing, hESCs are able to perform as well or even better than the cell lines used for majority of the studies ix List of ... treatment for 5mins before manual scrapping to smaller cell aggregate clumps using serological pipettes Clumps of cells were collected and centrifuged at 200g for 5mins before seeding for further ... far early from practice This study aims to open the horizon for the use of hESCs as a cellular model for implant testing and drug discovery along its differentiation process toward osteogenic...

Ngày tải lên: 16/10/2015, 15:38

... learning for LBVS will be covered Hence, the following chapter will introduce some basic concepts of in silico modeling for drug discovery Concepts Machine learning models for drug discovery ... development process, which form the task of drug discovery In this context, one also often speaks of chemoinformatics Disease pathways are modeled and analyzed in order to identify targets Furthermore, ... models for drug discovery, and introduces chemically intuitive interpretations Thereby, we hope to contribute to further enhanced communication in interdisciplinary drug development teams The drug...

Ngày tải lên: 26/11/2015, 09:59

... the thesis É Kalmár, K Ueno, P Forgó, G Szakonyi, G Dombi Novel sample preparation method for surfactant containing suppositories; effect of micelle formation on drug recovery Journal of Pharmaceutical ... effect is desired, the API, for example an analgesic drug can be applied in oral powder dosage form (Flector®) 2.1.2 Suppositories Suppositories are currently very popular formulations especially ... solution before and after micelle formation differ, the rate of turbidity increase changes when the surfactant concentration is increased This method therefore appeared appropriate for CMC determination...

Ngày tải lên: 10/12/2016, 13:40

... cause the conformational alteration (reviewed in [27,28]) The low-affinity conformation of drug binding sites in ABC multidrug efflux pumps is assumed to correspond to the outward-facing conformation ... ideal for the mediation of drug binding site reorientation, although the binding data cannot unequivocally inform on the orientation of the sites, only their affinity for interaction with drugs ... crystal structures Investigations with multidrug transporters, involved in conferring drug resistance in cancer cells, have provided the most information For two of the proteins, ABCB1 and ABCC1,...

Ngày tải lên: 18/02/2014, 18:20

... this information For additional information please contact Storey Books, Schoolhouse Road, Pownal, Vermont 05261 Storey Books are available for special premium and promotional uses and for customized ... exchange information Bacteria, in fact, possess a kind of biological Internet, and these information exchanges occur with great frequency Unfortunately for us, one of the types of information ... against bacteria (Information on how to make herbal preparations from these herbs can be found in chapter 4, Making and Using Herbal Medicines For instance, the tincture formula for echinacea says...

Ngày tải lên: 15/03/2014, 09:20

... were used for a tuning set for minimum error rate training, and another 1,500 for development set for analysis experiment We report testing results on the remaining 2,000 sentence pairs for the ... the reordering of Korean for Korean-English translation degraded the performance They presumed that the performance decrease might come from low parsing performance for conversational domain ... preprocessing method for both training and decoding in EnglishKorean SMT In particular, we transform a source language sentence by inserting pseudo words and syntactically reordering it to form a target sentence...

Ngày tải lên: 17/03/2014, 02:20

... isolation, identification and validation and hit the drug cell interaction I would like to thank all contributors for their excellent effort regarding the drug discovery issues and I believe ... attention must be paid to food -drug interactions (Figure 2) Figure Bioassay models for studying drug- phytochemical interaction Drug Discovery There are four types of accepted drug- food interactions based ... addition, 17 18 Drug Discovery polyphenols have been shown to interact with ABC drug transporters involved in drug re‐ sistance and drug absorption, distribution and excretion [32] Drug- food interaction...

Ngày tải lên: 29/03/2014, 21:20

... can generate for an event We propose an event description format that uses coarse-grained event, time, and location descriptions to achieve this goal We perform threshold-based validation on ... certainty for a MH-relevant event, vehicles rely on a threshold number of vehicles to report that event before alerting the driver The core challenge in thresholdbased event validation for VANETs ... priori what values are appropriate for a given scenario Time and location information Time and location information is required in each event description E The information can be provided by the...

Ngày tải lên: 30/03/2014, 16:20