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Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 54 for “"Cysteine Proteases"”.
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Development of Specific and Potent α-Helical Inhibitors and Probes of Cysteine Proteases
Cysteine proteases are of great scientific and pharmaceutical interest due to their diverse roles in cellular processes and diseases. However, it has been difficult to design inhibitors for use in determining their individual roles due to the conserved active site. Interestingly, each protease has …
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Synthesis And Biological Evaluation Of Nitrile-Based Inhibitors Of Cysteine Proteases Caged With Ruthenium Complexes
… photocages for caging nitrile-based cysteine protease inhibitors. Four research areas pertaining to this dissertation, i) metals in medicine, ii) photocages in biological applications, iii) photodynamic therapy and iv) cysteine cathepsin proteases were briefly surveyed in the …
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Investigation of the ubiquitin-specific protease UBP41 and of the lysosomal cysteine proteases cathepsin-L and cathepsin-B as potential mediators of proapoptotic signalling
… a possible involvement of the lysosomal cysteine proteases cathepsin-L and cathepsin-B in apoptosis pathways induced by distinct death stimuli, in particular by the tumor necrosis factor a (TNF-a). Therefore, both projects examine a possible regulation of apoptosis induction by proteases …
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Giardia Cathepsins and Their Role in Intestinal Disease
… Giardia genome contains genes for cathepsin-like cysteine proteases; however, their roles are unknown. Using an in vitro model for studying host-parasite interactions, we illustrated that G. duodenalis trophozoites contain and release cathepsin B/L-like cysteine proteases. While cathepsin-like …
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Use of Structure-And Ligand-Based Drug Design Tools for the Discovery of Small Molecule Inhibitors of Cysteine Proteases for the Treatment of Malaria and Sars Infection
… to design and develop inhibitors against cysteine protease of P. Falciparum Malaria and Severe Acute Respiratory Syndrome (SARS). A number of potent inhibitors were developed against cysteine protease and hemoglobinase of P. falciparum , referred as Falcipains (FPs), by the structure-based …
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Calpain inhibitor design inspired by the natural inhibitor calpastatin
Calpains are cysteine proteases that depend on Ca2+ for activation. They have many roles in the cell; hence modifications of calpains or changes in their levels of activity can lead to altered physiological states. Thus, it is of great interest and medical relevance to design inhibitors that can …
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Small molecule inhibitors of parasitic enzymes
… development of potential novel inhibitors of cysteine proteases from the causative agents of Malaria, African sleeping sickness and Chagas disease, (ii) development of potential new and novel anti-trypanosomal inhibitors of trypanosome alternative oxidase, and (ii) synthetic and methodological …
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The recombinant expression and localization of TvCP2 of trichomonas vaginalis
… combat resistant strains. T vagina/is expresses cysteine proteases that have been implicated in vaginal epithelial apoptosis as well as immune system evasion. In the past the various cysteine proteases have been studied as a group, and the following work examines, one specific protease, TvCP2, in …
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Utilization of the Baylis-Hillman and related reactions in antiparasitic drug discovery
… as potential inhibitors of two parasitic cysteine proteases (cruzain and Falcipain-2) and as antiparasitic agents. The utilization of polymer-supported bases in the Baylis-Hillman reaction is described. The use of ultrasound in combination with Lewis acids is also described in an attempt …
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Antimalarial and cysteine protease inhibitor pharmacophores as scaffolds for new antimalarial agents
… mechanism-based inhibiotrs of parasitic cysteine proteases. (iii) Multicomponenet reactions offer the advantage of introducing chemical diversity in fewer steps than conventional multi step organic synthesis. New chloroquine-type compounds were designed and synthesized using the Ugi 4 …
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Antiprotozoal quinolines containing electrophilic moieties
… Extensive research has identified the cysteine proteases in malaria and other parasitic diseases as potential targets for new chemotherapy due to their critical roles in the life cycles of the causative agents. Due to their role in the antimalarial activity of clinically available …
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Structural and Biochemical Characterization of N-Terminal Protease of Classical Swine Fever Virus
… individual proteins by host- and virus-encoded proteases. N-terminal protease Npro is the first translated protein of the pestivirus genome. Npro is a cysteine auto-protease that cleaves between its own C-terminus (Cys168) and the N-terminus of the core protein (Ser169). Npro is essential for …
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Investigating the Structure of the Papain-Inhibitor Complex using SPR and NMR
Cysteine proteases (CPs) are enzymes with a nucleophilic thiol in their active sites. Inhibitors of cysteine proteases (ICPs) occur naturally in bacterial pathogens and some protozoa. In parasites, ICPs are often virulence factors, contributing to the formation and survival of amastigotes within …
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Analysis of a trichomonas vaginalis cysteine protease
… USA. There is increasing focus on the role of cysteine proteases in Trichomonas vaginalis because of their role in virulence of other parasitic protozoa. Determining their location and function will provide insight about their role in the pathogenicity of T. vaginalis and their feasibility as a …
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Tissue and Cell-Type Localization and Partial Characterization of a Xylem Papain-Type Cysteine Protease From Arabidopsis
Cysteine proteases are associated with xylem tracheary element differentiation. XCP1 was recently identified as a xylem-specific cysteine protease in Arabidopsis (Zhao, et al., 2000). For this study a recombinant polyhistidine-tagged XCP1 (XCP1H6) was expressed and purified from an E. coli …
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N-terminomics/proteomics investigation of Calpain-2 substrates
Calpains are a family of intracellular cysteine proteases that require calcium for activation. Calpain-1 and -2, first described as the classical calpains due to their ubiquitous expression, are part of this larger 15-member family in humans and share similar patterns of expression and structural …
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The characterisation of calpain-like proteins in Trypanosoma brucei
… are a ubiquitous family of calcium-dependent cysteine proteases involved in a wide range of cell regulatory and differentiation processes. In many protozoan organisms, atypical calpains have been discovered that lack the characteristic calcium-binding penta-EF-hand motif of typical vertebrate …
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Biochemical investigation of the ubiquitin carboxyl-terminal hydrolase family
… thought not to exist within the active sites of cysteine proteases. Lastly, I will show that a conserved tryptophan in UCH37 has an effect on its catalytic viability.</p>
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Investigation of apoptosis by conditional gene expression
… -2. The effector molecules belong to a class of cysteine proteases, known the ICE -like proteases (e.g. Nedd2). Whilst the known components can have identifiable activity in apoptosis id (or) cell cycle control, it has been suggested that they interact to control apoptosis. Further, it is not …
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New aminoquinoline antimalarial cysteine protease inhibitors based on the isatin natural product scaffold
… moiety previously demonstrated to inhibit cysteine proteases from mUltiple protozoan parasites. Synthesized compounds were tested against the enzyme falcipain-2 (Rec-FP-2) as well as the parasite source of this protease, Plasmodium Jalciparum (P.f. W2). The results of structure activity …
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