Download or read book Molecular Modes of Action of 1 alpha 25 dihydroxyvitamin D3 and Analogs written by Guy Eelen and published by Leuven University Press. This book was released on 2005 with total page 206 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Influences of 1 alpha 25 dihydroxyvitamin D3 Analogs on Coactivator Recruitment to the Vitamin D Receptor Transcriptional Complex written by Marie Kristan Schwinn and published by . This book was released on 2006 with total page 170 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Sunlight Vitamin D and Skin Cancer written by Jörg Reichrath and published by Springer Nature. This book was released on 2020-09-11 with total page 428 pages. Available in PDF, EPUB and Kindle. Book excerpt: The third edition is a comprehensive and updated overview of positive and negative effects of UV-exposure, with a focus on Vitamin D and skin cancer. Researchers, oncologists,and students will be provided with the most significant and timely information related to topics such as the epidemiology of skin cancer, the immune system and skin cancer, ultraviolet damage, DNA repair and Vitamin D in Nonmelanoma skin cancer and malignant melanoma. There have been a number of new, scientific findings in this fast moving field that necessitated a thoroughly updated and revised edition including new Vitamin D metabolites and skin cancer, new findings on the beneficial effects of UV and solar UV and skin cancer, adverse effects of sun protection and sunscreens, sun exposure and mortality, and more. The book will summarize essential, up-to-date information for every clinician or scientist interested in how to balance the positive and negative effects of UV‐exposure to minimize the risks of developing vitamin D deficiency and skin cancer.
Download or read book Synthesis of 20S hydroxyvitamin D3 Analogs and Their 1 alpha hydroxyl Derivatives as Potent Anti inflammatory Agents written by Zongtao Lin and published by . This book was released on 2017 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: Rheumatoid arthritis (RA) is one of the autoimmune diseases, and is affecting 2.5 million Americans in total. Among the treatment options of RA, 1[alpha],25-dihydroxyvitamin D3 [1,25(OH)2D3] is the only steroidal drug used clinically for anti-inflammatory and immune diseases. However, long-term use of 1,25(OH)2D3 (625 [mu]g/day) in human would result in hypercalcemia (toxicity), and 1,25(OH)2D3 has substantial hypercalcemic effects (toxicity) in mice at a dose as low as only 2 [mu]g/kg. Fortunately, during the investigation of novel metabolic pathway of vitamin D3 by cytochrome P450 enzymes, we found 20S-hydroxyvitamin D3 [20S(OH)D3] as a good lead compound. 20S(OH)D3 suppressed disease symptoms at 2 [mu]g/kg in collagen-induced arthritis model, and high doses of 20S(OH)D3 (up to 30 [mu]g/kg) do not cause hypercalcemia in rats or mice. Thus 20S(OH)D3 has the potential to be structurally optimized for providing anti-inflammatory agents without toxicity. In this study, four series of 20S(OH)D3 analogs have been synthesized and studied, they are C20 Gemini analogs, C24-hydroxlated analogs, C23-hydroxlated analogs and C24 modified analogs together with their 1[alpha]-hydroxylated derivatives. Since D3 analogs with two symmetric side chains (Gemini analogs) result in potent activation of the vitamin D receptor (VDR), we hypothesized that the chain length and composition of these types of analogs also containing a 20-hydroxyl group would affect their biological activities. In this study, we designed and synthesized a series of Gemini 20S(OH)D3 analogs. Biological tests showed that some of these analogs are partial VDR activators and can significantly stimulate the expression of mRNA for VDR and VDR-regulated genes including CYP24A1 and transient receptor potential cation channel V6 (TRPV6). These analogs inhibited the proliferation of melanoma cells with potency comparable to that of 1[alpha],25-dihydroxyvitamin D3. Moreover, these analogs reduced the level of interferon [gamma] and up-regulated the expression of leukocyte associated immunoglobulin-like receptor 1 in splenocytes, indicating that they have potent anti-inflammatory activities. There are no clear correlations between the Gemini chain length and their VDR activation or biological activities, consistent with the high flexibility of the ligand-binding pocket of the VDR. Bioactive vitamin D3 metabolites 20S,24S-dihydroxyvitamin D3 [20S,24S(OH)2D3] and 20S,24R-dihydroxyvitamin D3 [20S,24R(OH)2D3] were chemically synthesized and confirmed to be identical to their enzymatically generated counterparts. The absolute configurations at C24 and its influence on the kinetics of 1[alpha]-hydroxylation by CYP27B1 were determined. Their corresponding 1[alpha]-hydroxyl derivatives were subsequently produced. Biological comparisons of these products showed different properties with respect to vitamin D3 receptor activation, anti-inflammatory activity, and anti-proliferative activity, with 1[alpha],20S,24R(OH)2D3 being the most potent compound. The vitamin D3 metabolite, 20S,23S-dihydroxyvitamin D3, was chemically synthesized for the first time, and identified to be the same as the enzymatically produced metabolite. The C23 absolute configurations of both 20S,23S/R-dihydroxyvitamin D3 epimers were unambiguously assigned by NMR and Mosher ester analysis. Their kinetics of CYP27B1 metabolism were investigated during the production of their 1[alpha]-hydroxylated derivatives. Bioactivities of these products were compared in terms of vitamin D3 receptor activation, anti-inflammatory and anti-proliferative activities. Four C24 modified analogs of 20S(OH)D3 were chemically synthesized and comprehensively tested against different activities together with their 1[alpha]-hydroxyl derivatives. Metabolism of 20S(OH)D3 analogs against cytochrome P450 27B1 (CYP27B1, activation enzyme) and CYP24A1 (catabolism enzyme) suggested that they are better substrates of both enzymes than 20S(OH)D3, and can be activated (1[alpha]-hydroxylated) by CYP27B1 except 23-amide which is not a substrate but an inhibitor of CYP27B1. Their 1[alpha]-OH derivatives were potent vitamin D receptor (VDR) agonists comparable with 1,25(OH)2D3 although they themselves showed weak or none VDR stimulation activity in three cell lines. To understand the molecular interactions between these analog and VDR, two analogs together with 20S(OH)D3 and 1,25(OH)2D3 were co-crystalized with human VDR. These analogs and 1[alpha]-OH derivatives significantly upregulated the mRNA expression of VDR target genes, suggesting their actions via VDR, at least partially. In addition, their anti-inflammatory activities have been investigated in aspect of IFN[gamma] inhibition in splenocytes. This study demonstrates the mechanisms of action of 20S(OH)D3 anlogs, is of great importance for future drug development of anti-inflammatory agents. From the above-mentioned studies, we learned that the introduction of 1[alpha]-hydroxy could potentiate the anti-inflammatory activities of 20S(OH)D3 and its anlogs. Thus it would be beneficial to further investigate the 1[alpha],20S-Dihydroxyvitamin D3 [1,20S(OH)2D3] analogs. 1,20S(OH)2D3 was chemically synthesized for the first time. A semi-reduced intermediate of the Birch reduction for 1[alpha]-OH formation was obtained for the first time, and thus was used to propose the reaction mechanism. X-ray crystallography analysis of the key intermediate confirmed the formation of 1[alpha]-OH. 1,20S(OH)2D3 binds efficiently in vitamin D receptor (VDR), being similar with its native ligand 1[alpha],25-dihydroxyvitamin D3 [1,25(OH)2D3]. However, their co-crystal structures revealed differential molecular interactions of 20S-OH and 25-OH in VDR, which may help understand their biological activities. In addition, 1,20S(OH)2D3 functions as a VDR agonist with stronger/comparable activities than/with 1,25(OH)2D3 in aspects of VDR stimulation and regulating VDR downstream genes, and inhibition of inflammatory markers. This study offers a convenient synthetic route using a novel intermediate 1[alpha],3[beta]-diacetoxypregn-5-en-20-one, and provides molecular basis of design for drug development of 1,20S(OH)2D3 and its analogs. Overall, we have synthesized and biologically evaluated four series of 20S(OH)D3 analogs for their potential applications in anti-inflammatory diseases such as RA. The synthetic scheme of 1,20S(OH)2D3 could pioneer future development of its analogs. These findings will provide important guidance for the development of next generation anti-RA agents using 20S(OH)2D3 scaffold.
Download or read book Studies on the Mechanism of Action of the Steroid Hormone 1 alpha 25 dihydroxyvitamin D subscript 3 written by Wayne Robert Wecksler and published by . This book was released on 1978 with total page 474 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Vitamin D written by Michael F. Holick and published by Springer Science & Business Media. This book was released on 2013-03-09 with total page 456 pages. Available in PDF, EPUB and Kindle. Book excerpt: The Nutrition and Health series of books has as an overriding mission to provide health professionals with texts that are considered essential because each includes: a synthesis of the state of the science; timely, in-depth reviews by the leading researchers in their respective fields; extensive, up-to-date fully annotated reference lists; a detailed index; relevant tables and figures; identification of paradigm shifts and the consequences; of information between chapters, but targeted, inter-chapter refer virtually no overlap rals, suggestions of areas for future research; and balanced, data-driven answers to patient questions that are based on the totality of evidence rather than the findings of any single study. The series volumes are not the outcome of a symposium. Rather, each editor has the potential to examine a chosen area with a broad perspective, both in subject matter as well as in the choice of chapter authors. The international perspective, especially with regard to public health initiatives, is emphasized where appropriate. The editors, whose training is both research and practice oriented, have the opportunity to develop a primary objective for their book, define the scope and focus, and then invite the leading authori ties from around the world to be part of their initiative. The authors are encouraged to provide an overview of the field, discuss their own research, and relate the research de findings to potential human health consequences.
Download or read book Nuclear Mechanism of Action of 1 alpha 25 dihydroxyvitamin written by Joseph Edward Zerwekh and published by . This book was released on 1976 with total page 296 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Vitamin D in Clinical Medicine written by A. Giustina and published by Karger Medical and Scientific Publishers. This book was released on 2018-03-29 with total page 216 pages. Available in PDF, EPUB and Kindle. Book excerpt: Vitamin D deficiency is prevalent today not only among the elderly but pervasively throughout all ages of life.This is due, in part, to systemic diseases that affect vitamin D metabolism, to changes in lifestyle, such as insufficient exposure to sunlight, and to increased use of sunscreen. Apart from the obvious effects of vitamin D deficiency on skeletal metabolism, the problem is assuming even greater significance because observational and interventional studies have linked vitamin D deficiency to cardiovascular disease, cancer, and diabetes. This book addresses a variety of important issues that have emerged from this fast-moving area of clinical medicine. The topics include assays of vitamin D and its binding protein, effects on aging and associated complications, primary and secondary states of altered parathyroid hormone secretion, vitamin D in the growing years of children and adolescents, nutritional requirements, and vitamin D as it relates to systemic disorders such as diabetes mellitus. Vitamin D in Clinical Medicine aims to offer new insights, in an evidence-based way, on important issues related to vitamin D. It is written for general practitioners and internists, as well as for endocrinologists, nutritionists, pulmonologists, cardiologists, and oncologists.
Download or read book Vitamin D written by H.F. DeLuca and published by Springer. This book was released on 2011-12-13 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Because diseases of the bone are often less acute and less lifethreatening than dis eases of the circulatory system, gastrointestinal tract, kidney, liver, and the nervous system, they have received a disproportionately smaller amount of attention in the medical world. With the average increasing life span of man as a result of improve ments in modern medicine, espe~ially in the pediatric field, the seriousness of many metabolic bone diseases has indeed become more obvious. In addition, other improvements in medicine, such as hemodialysis for the preservation of renal failure patients, have permitted the development of other consequences of diseased kidneys, one of which is the appearance of renal osteodystrophy. Finally, the appearance of several genetic disorders in the area of metabolic bone disease has been underscored by the solution of other pediatric diseas~s of much more serious consequences. These emerging problems all suggest that much remains to be learned concerning the sys temic control of bone, both as a structural organ and as a reservoir for the important elements of calcium and phosphorus so essential for the support of life in complex multicellular organisms of which man is the most important. As will be demonstrated in the historical portion of this manuscript, the existence of the three most important humoral factors regulating bone metabolism and func tion are now known.
Download or read book Vitamin D in Chronic Kidney Disease written by Pablo A. Ureña Torres and published by Springer. This book was released on 2016-09-21 with total page 583 pages. Available in PDF, EPUB and Kindle. Book excerpt: Vitamin D deficiency, circulating levels lower than 15 ng/ml, is an epidemic disease worldwide with more than a billion people suffering of it in the beginning of the 21-century. Besides its impact on mineral and bone metabolism, these low vitamin D levels are also associated with a diversity of non-skeletal complications, among them cardiovascular disease, diabetes mellitus, multiple sclerosis, cancer, tuberculosis, and immune system dysfunction. Chronic Kidney Disease is also a very common disease, affecting more than 10% of the world population, ranging from stage 1 to stage 5 before dialysis. Approximately 1% of the population in industrialized countries is affected by end-stage renal disease (ESRD), needing a renal replacement therapy either hemodialysis or peritoneal dialysis, and ultimately by renal transplantation. Those CKD patients are more susceptible to exhibit reduced vitamin D stocks. Consequently, more than eighty percent of CKD patients have either insufficient or deficient vitamin D levels for multiple reasons.
Download or read book Vitamin D written by David Feldman and published by Elsevier. This book was released on 2005-01-25 with total page 1970 pages. Available in PDF, EPUB and Kindle. Book excerpt: Vitamin D, a steroid hormone, has mainly been known for its effects on bone and osteoporosis. The current therapeutic practices expand into such markets as cancer research, pediatrics, nephrology, dermatology, immunology, and genetics. This second edition includes over 100 chapters covering everything from chemistry and metabolism to mechanisms of action, diagnosis and management, new analogs, and emerging therapies. This complete reference works is a must have resource for anyone working in endocrinology, osteology, bone biology, or cancer research.*Most comprehensive, up-to-date two-volume set on Vitamin D*New chapters on squamous cell cancer, brain cancer, thyroid cancer and many more*Further sections on emerging uses for treatments of auto-immune diseases and diabetes*Over 600 illustrations and figures available on CD
Download or read book Mechanisms of Hormone Action written by P Karlson and published by Elsevier. This book was released on 2013-10-22 with total page 288 pages. Available in PDF, EPUB and Kindle. Book excerpt: Mechanisms of Hormone Action: A NATO Advanced Study Institute focuses on the action mechanisms of hormones, including regulation of proteins, hormone actions, and biosynthesis. The selection first offers information on hormone action at the cell membrane and a new approach to the structure of polypeptides and proteins in biological systems, such as the membranes of cells. Discussions focus on the cell membrane as a possible locus for the hormone receptor; gaps in understanding of the molecular organization of the cell membrane; and a possible model of hormone action at the membrane level. The text also ponders on insulin and regulation of protein biosynthesis, including insulin and protein biosynthesis, insulin and nucleic acid metabolism, and proposal as to the mode of action of insulin in stimulating protein synthesis. The publication elaborates on the action of a neurohypophysial hormone in an elasmobranch fish; the effect of ecdysone on gene activity patterns in giant chromosomes; and action of ecdysone on RNA and protein metabolism in the blowfly, Calliphora erythrocephala. Topics include nature of the enzyme induction, ecdysone and RNA metabolism, and nature of the epidermis nuclear RNA fractions isolated by the Georgiev method. The selection is a valuable reference for readers interested in the mechanisms of hormone action.
Download or read book Characterization of 1 alpha 25 dihydroxyvitamin D3 stimulated Anti apoptotic Molecular Signaling in Osteoblasts written by Xiaoyu Zhang and published by . This book was released on 2007 with total page 306 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Vitamin D and Human Health written by Simon Spedding and published by MDPI. This book was released on 2019-02-21 with total page 307 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book is a printed edition of the Special Issue "Vitamin D and Human Health" that was published in Nutrients
Download or read book A Critical Evaluation of Vitamin D written by Sivakumar Joghi Thatha Gowder and published by . This book was released on 2017-04-12 with total page 334 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Principles of Bone Biology written by John P. Bilezikian and published by Academic Press. This book was released on 2008-09-29 with total page 2074 pages. Available in PDF, EPUB and Kindle. Book excerpt: Principles of Bone Biology provides the most comprehensive, authoritative reference on the study of bone biology and related diseases. It is the essential resource for anyone involved in the study of bone biology. Bone research in recent years has generated enormous attention, mainly because of the broad public health implications of osteoporosis and related bone disorders. - Provides a "one-stop" shop. There is no need to search through many research journals or books to glean the information one wants...it is all in one source written by the experts in the field - The essential resource for anyone involved in the study of bones and bone diseases - Takes the reader from the basic elements of fundamental research to the most sophisticated concepts in therapeutics - Readers can easily search and locate information quickly as it will be online with this new edition
Download or read book Calcium regulating Hormones written by Hirotoshi Morii and published by . This book was released on 1991 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt:
