𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Vitamin D: Structure-function analyses and the design of analogs

✍ Scribed by William H. Okamura; J. Antonio Palenzuela; Joaquin Plumet; M. Mark Midland

Publisher
John Wiley and Sons
Year
1992
Tongue
English
Weight
736 KB
Volume
49
Category
Article
ISSN
0730-2312

No coin nor oath required. For personal study only.

✦ Synopsis

There is continuing and emerging new interest in the development of vitamin D analogs resulting from the recognition that analogs of 1 cw,25-dihydroxyvitamin D3 [I ~x,25-(0H)~D~] may be therapeutically useful. Side chain analogs of this steroid hormone are of particular interest because a family of lead structures have recently emerged for possible use in the treatment of certain types of cancers and skin diseases. Because of the chaotic array of side chain structures which exhibit useful therapeutic indices for these purposes, a more systematic approach towards developing intelligible structure-function information needs development. Accordingly, a method has been devised to analyze analogs as to their side chain topology based on identifying specific occupancy volumes through conformational analysis. Dot maps have been constructed as an indication of the volume in space which the side chain of 1 ( ~, 2 5 -( 0 H ) ~-D ~ or analogs is permitted to occupy. Volume exclusion analyses based on comparison of structural and biological data for la,25-(OH)2-D3 and analogs are anticipated to lead to a more cogent model for drug design. A cautionary note on the limitations of this approach is discussed.

📜 SIMILAR VOLUMES

Structure–function relationships of vita
Structure–function relationships of vitamin D including ligand recognition by the vitamin D receptor
✍ Sachiko Yamada; Masato Shimizu; Keiko Yamamoto 📂 Article 📅 2003 🏛 John Wiley and Sons 🌐 English ⚖ 829 KB

## Abstract First, the general structure and function of nuclear receptors (NRs) are described briefly to help our understanding of the mechanism of action of vitamin D mediated by the vitamin D receptor (VDR), a member of the NRs. Then we discuss the structure–function relationship (SFR) of vitami

Expression, structure-function, and mole
Expression, structure-function, and molecular modeling of vitamin D P450s
✍ J.L. Omdahl; E.V. Bobrovnikova; A. Annalora; P. Chen; R. Serda 📂 Article 📅 2002 🏛 John Wiley and Sons 🌐 English ⚖ 137 KB

## Abstract Although vitamin D~3~ is a natural product of a sunlight‐mediated process in the skin, the secosteroid's biological function is dependent upon specific cytochrome P450 enzymes that mediate the parent vitamin's bioactivation and inactivation. Cytochrome P450C1 (CYP27B1) is the regulatory

Rationale for active vitamin D and analo
Rationale for active vitamin D and analogs in the treatment of osteoporosis
✍ Yasuho Nishii 📂 Article 📅 2002 🏛 John Wiley and Sons 🌐 English ⚖ 114 KB

## Abstract In 1981, Chugai Pharmaceutical succeeded in marketing alfacalcidol, a prodrug of calcitriol, as a therapeutic agent for renal osteodystrophy. In 1983, Chugai succeeded in extending the application of alfacalcidol to the treatment of osteoporosis as well. Clinicians in Japan have accepte