Structure-function study of gemini derivatives with two different side chains at C-20, Gemini-0072 and Gemini-0097.
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ABSTRACT:
SUBMITTER: Huet T
PROVIDER: S-EPMC3236830 | biostudies-literature | 2011
REPOSITORIES: biostudies-literature
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Structure-function study of gemini derivatives with two different side chains at C-20, Gemini-0072 and Gemini-0097.
Huet Tiphaine T Maehr Hubert H Lee Hong Jin HJ Uskokovic Milan R MR Suh Nanjoo N Moras Dino D Rochel Natacha N
MedChemComm 20110101 5
Derivatives of vitamin D(3) containing a second side-chain emanating at C-20 are known as gemini and act as vitamin D receptor agonists. Recently, two of these, namely Gemini-0072 and the epimeric Gemini-0097, were selected for further studies in view of their high biological activities and lack of hypercalcemic effects. We now show that the two analogs recruit coactivator SRC-1 better than the parental gemini and act as VDR superagonists. The crystal structures of complexes of zVDR with Gemini- ...[more]
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