Analogs of Calcitriol

© 2018 Elsevier Inc. All rights reserved. The paracrine function of 1,25(OH)2D3(calcitriol) has stimulated an extensive exploration of the structure-function relationships of this secosteroid molecule to develop analogs with a clear dissociation between antiproliferative, prodifferentiating, and immunomodulatory properties on the one hand and calcemic in vivo activity on the other hand. A diverse collection of nonsteroidal and nonsecosteroidal analogs has been studied and demonstrated that the classical core structure of 1,25(OH)2D3is not needed for a genomic vitamin D-like effect. Some of these analogs have been identified with a very interesting selectivity profile favoring antiproliferative, prodifferentiating, and immunomodulatory properties with low systemic calcemic effects. Such analogs should be or are further explored as therapeutic agents for topical (e.g., psoriasis) or systemic administration (e.g., immune disorders or cancer).

ISBN:9780128099643

Publication year:2017