The Design, Synthesis and Evaluation of Peptide Based Protease Inhibitors PDF Download
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Author: Stewart A. Thompson
Publisher:
ISBN:
Category :
Languages : en
Pages : 220
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Book Description
Author: Stewart A. Thompson
Publisher:
ISBN:
Category :
Languages : en
Pages : 220
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Author: Jonathan Charles Crisp
Publisher:
ISBN:
Category :
Languages : en
Pages : 0
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Author:
Publisher:
ISBN:
Category :
Languages : en
Pages : 170
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Author: Ellen Kay Kick
Publisher:
ISBN:
Category :
Languages : en
Pages : 402
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Author: Karen Amanda Ellis James
Publisher:
ISBN:
Category : Crysteine proteinase
Languages : en
Pages : 324
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Author: Iuliana L. Gheura
Publisher:
ISBN:
Category : Protease inhibitors
Languages : en
Pages : 338
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Author: Sylvia Shadinger Bridges
Publisher:
ISBN:
Category : Cysteine proteinases
Languages : en
Pages :
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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
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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:
Publisher:
ISBN:
Category :
Languages : en
Pages :
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Author: David B. Weiner
Publisher: CRC Press
ISBN: 9780877629351
Category : Medical
Languages : en
Pages : 382
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Book Description
Investigation into basic and advanced peptide design, synthesis, evaluation and utilization. New therapeutic approaches from experimental systems.
