Design, Synthesis, and Evaluation of Novel Cysteine Protease Inhibitors PDF Download
Are you looking for read ebook online? Search for your book and save it on your Kindle device, PC, phones or tablets. Download Design, Synthesis, and Evaluation of Novel Cysteine Protease Inhibitors PDF full book. Access full book title Design, Synthesis, and Evaluation of Novel Cysteine Protease Inhibitors by Karen Amanda Ellis James. Download full books in PDF and EPUB format.
Author: Karen Amanda Ellis James
Publisher:
ISBN:
Category : Crysteine proteinase
Languages : en
Pages : 324
Get Book Here
Book Description
Author: Karen Amanda Ellis James
Publisher:
ISBN:
Category : Crysteine proteinase
Languages : en
Pages : 324
Get Book Here
Book Description
Author: Joel Anderson Krauser
Publisher:
ISBN:
Category : Protease inhibitors
Languages : en
Pages : 312
Get Book Here
Book Description
Author: Anthony Kwabla Dotse
Publisher:
ISBN:
Category : Proteolytic enzymes
Languages : en
Pages : 396
Get Book Here
Book Description
Author: Sylvia Shadinger Bridges
Publisher:
ISBN:
Category : Cysteine proteinases
Languages : en
Pages :
Get Book Here
Book Description
Proteases are enzymes that cleave protein amide bonds. Proteases are involved in a myriad of biological processes and are considered good targets for drug design. The proteases described herein are cysteine proteases, which utilize a cysteine residue thiol to attack the amide carbonyl, leading to amide bond cleavage. Irreversible inhibitors of cysteine proteases react with the active site cysteine, forming a covalent bond and rendering the enzyme inactive. The first project involved the design and synthesis of aza-peptide epoxide inhibitors for calpain, a clan CA, ubiquitous, calcium-activated human enzyme involved in neurodegeneration. These inhibitors proved to be poor inactivators of calpain, demonstrating that the aza-peptide epoxide is a warhead specific to clan CD cysteine proteases (caspases, gingipains). Subsequently, a known epoxide inhibitor of calpain was optimized to create a more potent inhibitor. Several of these inhibitors were more potent than the parent, and all were demonstrated to inhibit calpain in a breast cancer cell line which was treated with paclitaxel to spike calpain activity.
Author: Amy J. Campbell
Publisher:
ISBN: 9781109870527
Category :
Languages : en
Pages : 162
Get Book Here
Book Description
This research involved the design, synthesis, and evaluation of irreversible cysteine protease inhibitors. Specifically, irreversible inhibitors of clan CA and clan CD cysteine proteases were studied. This research offers new and valuable insights into recently developed classes of inhibitors.
Author: Iuliana L. Gheura
Publisher:
ISBN:
Category : Protease inhibitors
Languages : en
Pages : 338
Get Book Here
Book Description
Author: Stewart A. Thompson
Publisher:
ISBN:
Category :
Languages : en
Pages : 220
Get Book Here
Book Description
Author: Asli Ovat
Publisher:
ISBN:
Category : Biosynthesis
Languages : en
Pages :
Get Book Here
Book Description
Cysteine proteases are important drug targets due to their involvement in many biological processes such as protein turnover, digestion, blood coagulation, apoptosis, cell differentiation, cell signaling, and the immune response. In this thesis, we have reported the design, synthesis and evaluation of clan CA and clan CD cysteine protease inhibitors. Aza-peptidyl Michael acceptor and epoxide inhibitors for asparaginyl endopeptidases (legumains) from the bloodfluke, Schistosoma mansoni (SmAE) and the hard tick, Ixodes ricinus (IrAE) were designed and synthesized. SARs were similar, but with some notable exceptions. Both enzymes prefer disubstituted amides to monosubstituted amides in the P1' position and potency increased as we increased the hydrophobicity of the inhibitor in this position. Extending the inhibitor to P5 resulted in increased inhibitory potency, especially against IrAE, and both enzymes prefer small over large hydrophobic residues in the P2 position. Aza-peptide Michael acceptor inhibitors are more potent than aza-peptide epoxide inhibitors and, for some of these compounds, second order inhibition rate constants are the fastest yet discovered.
Author: Koen Steert
Publisher:
ISBN:
Category :
Languages : en
Pages : 228
Get Book Here
Book Description
Author: John F. Lynas
Publisher:
ISBN:
Category :
Languages : en
Pages :
Get Book Here
Book Description
