Evaluation of Dipeptide-derivatives of 5-aminolevulinic Acid as Precursors for Photosensitizers in Photodynamic Therapy PDF Download
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Languages : en
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N-terminal-blocked and N-terminal-free pseudotripeptide Gly-Gly and Gly-Pro derivatives of 5-aminolevulinic acid (ALA) esters were synthesized as potential specific substrates for cellular peptidases and precursors for the production of the photosensitizer protoporphyrin IX (PpIX). These precursors were evaluated using human cell lines of either carcinoma or endothelial origin. N-blocked or N-free dipeptides-ALA-ethyl esters, but not tripeptides-ALA-ethyl esters (or dipeptides-ALA-ethyleneglycols,) were substrates for cellular peptidases and were metabolized to ALA. The precursors were hydrolyzed intracellularly involving serine-proteases and metalloproteases. Cell selectivity for human endothelial or carcinoma cells was observed for some of these dipeptides-ALA. Thus drugs coupled to Gly-Gly-/Gly-Pro-derivatives may selectively target defined cells in human cancer, depending on specific cellular activating pathways expressed by the cells.
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Languages : en
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Book Description
N-terminal-blocked and N-terminal-free pseudotripeptide Gly-Gly and Gly-Pro derivatives of 5-aminolevulinic acid (ALA) esters were synthesized as potential specific substrates for cellular peptidases and precursors for the production of the photosensitizer protoporphyrin IX (PpIX). These precursors were evaluated using human cell lines of either carcinoma or endothelial origin. N-blocked or N-free dipeptides-ALA-ethyl esters, but not tripeptides-ALA-ethyl esters (or dipeptides-ALA-ethyleneglycols,) were substrates for cellular peptidases and were metabolized to ALA. The precursors were hydrolyzed intracellularly involving serine-proteases and metalloproteases. Cell selectivity for human endothelial or carcinoma cells was observed for some of these dipeptides-ALA. Thus drugs coupled to Gly-Gly-/Gly-Pro-derivatives may selectively target defined cells in human cancer, depending on specific cellular activating pathways expressed by the cells.
Author: Louis Mark-Antony Rogers
Publisher:
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Category :
Languages : en
Pages : 221
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Author: Tebello Nyokong
Publisher: Springer Science & Business Media
ISBN: 9048138728
Category : Science
Languages : en
Pages : 672
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Book Description
This book addresses the synthesis of photosensitizers, the main emphasis being on the new methods of synthesis such as microwave, sonochemistry and the use of ionic liquids. It also addresses the photochemistry and photophysics of the photosensitizers alone and in combination with nanoparticles, the use of the photosensitizers in environmental control, safety and medicine. It discusses the common structures of the photosensitizers which are beneficial to these applications.
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Category : Medicine
Languages : en
Pages : 1666
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Book Description
Vols. for 1963- include as pt. 2 of the Jan. issue: Medical subject headings.
Author: R. Rigler
Publisher: Springer Science & Business Media
ISBN: 3642565441
Category : Science
Languages : en
Pages : 375
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Book Description
The topics range from single molecule experiments in quantum optics and solid-state physics to analogous investigations in physical chemistry and biophysics.
Author: Valentino Stella
Publisher: Springer Science & Business Media
ISBN: 038749782X
Category : Medical
Languages : en
Pages : 1447
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Book Description
These volumes represent a comprehensive guide to prodrugs. They guide the reader through the current status of the prodrug concept and its many applications and highlight its many successes in overcoming formulation and delivery of problematic drugs. Replete with examples of approved and marketed prodrugs, these volumes introduce the topic to the novice as well as professional in the design of prodrugs.
Author: Raja K Sivamani
Publisher: CRC Press
ISBN: 1482214172
Category : Medical
Languages : en
Pages : 460
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Book Description
Cosmeceuticals and Active Cosmetics discusses the science of nearly two dozen cosmeceuticals used today. This third edition provides ample evidence on specific cosmeceutical substances, their classes of use, skin conditions for which they are used, and points of interest arising from other considerations, such as toxicology and manufacturing. The book discusses both cosmetic and therapeutic uses of cosmeceuticals for various conditions including rosacea, dry skin, alopecia, eczema, seborrheic dermatitis, purpura, and vitiligo. Active ingredients in the following products are discussed: caffeine, curcumin, green tea, Rhodiola rosea, milk thistle, and more. Also covered are topical peptides and proteins, amino acids and derivatives, antioxidants, vitamins E and C, niacinamide, botanical extracts, and biomarine actives. Providing ample scientific references, this book is an excellent guide to understanding the science behind the use of cosmeceuticals to treat a variety of dermatological conditions.
Author: Xiaodong Liu
Publisher: Springer Nature
ISBN: 9811376476
Category : Medical
Languages : en
Pages : 580
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Book Description
This book provides with a comprehensive overview of the role of drug transporters in drug disposition and efficacy/toxicity, as well as drug-drug interactions and recent advances in the field. Transporters are known determinants of drug disposition and efficacy/toxicity. In general, they are divided into solute carrier (SLC) and ATP binding cassette (ABC) families, and are located along cell membranes, where they mediate drug uptake into cells and export out of cells. Drug transporters are essential in maintaining cell homeostasis, and their gene mutations may cause or contribute to severe human genetic disorders, such as cystic fibrosis, neurological disease, retinal degeneration, anemia, and cholesterol and bile transport defects. Conversely, some diseases may also alter transporter functions and expressions, in turn aggravating disease process. Further, since over-expression of some ABC transporters is a potential contributor to multidrug-resistance (MDR), the book presents a number of strategies to overcome MDR, including ABC transporter inhibitors and applying epigenetic methods to modulate transporter expressions and functions. This book is useful for graduate students and professionals who are looking to refresh or expand their knowledge of this exciting field.
Author: Jaime Castillo
Publisher: CRC Press
ISBN: 9814364479
Category : Medical
Languages : en
Pages : 318
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Book Description
The self-organization of bionanostructures into well-defined functional machineries found in nature has been a priceless source of ideas for researchers. The molecules of life, proteins, DNA, RNA, etc., as well as the structures and forms that these molecules assume serve as rich sources of ideas for scientists or engineers who are interested in de
Author: Ülo Langel
Publisher: Springer
ISBN: 9811387478
Category : Science
Languages : en
Pages : 470
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Book Description
In this book, a summary and update of the most important areas of CPP research are presented, whilst raising relevant questions for further development. The CPP sequences are presented and discussed throughout the book. The methods for testing CPP mechanisms are discussed in detail. Various approaches for the testing of endocytotic pathways of CPP uptake are also described. Different CPP uptake experiments are compared since it is becoming clear that it is often best to apply several methods in a complementary manner in order to most comprehensively evaluate CPP uptake mechanisms due to the complexity of these processes. A brief summary of functionality issues of CPPs, both in vitro and in vivo are discussed. Therapeutic potential of CPPs and commercial developments are discussed. The monograph is written for researchers and students in the field.
