TY - JOUR
T1 - Effect of thyroid hormone analogues on the displacement of 125I-L-triiodothyronine from hepatic and heart nuclei in vivo
T2 - Possible relationship to hormonal activity
AU - Oppenheimer, J. H.
AU - Schwartz, H. L.
AU - Dillman, W.
AU - Surks, M. I.
N1 - Funding Information:
EFFECT OF THYROID HORMONE ANALOGUES ON THE DISPLACEMENT OF 1251-L-TRIIODOTHYRONINE FROM HEPATIC AND HEART NUCLEI IN VIVO: POSSIBLE RELATIONSHIP TO HORMONAL ACTIVITY. J.H. Oppenheimer, H.L. Schwartz, W. Dillman and M.I. Surks*. Endocrine Laboratory, Division of Endocrinology, Department of Medicine, Montefiore Hospital and Medical Center and Albert Einstein College of Medicine, Bronx, New York 10467. Supported by NIH Grant 15421-13 6 Dept. of Defense Contract DA-49-193-MD-2967. "Recipient, Research Career Development Award K04 AM 19502-01111.
PY - 1973/12/10
Y1 - 1973/12/10
N2 - The capacity of iodotyrosines and iodothyronine analogues to displace tracer[125I] L-3,5,3′ triiodothyronine from specific nuclear binding sites in rat liver and heart was related to the displacement capacity of nonradioactive triiodothyronine. Iodotyrosines and L-3,3′,5′ triiodothyronine ("reverse T3") were devoid of displacement activity. Analogues with 3,5 substitution in the "inner" ring and single "bulk" substitution in the 3′ position in the phenolic ring exhibited the strongest displacement activity. When the distribution, fractional removal rates and metabolic conversion of the analogues were taken into account, displacement activity appeared to correlate well with the reported thyromimetic activity. These results support the biologic relevance of the nuclear sites.
AB - The capacity of iodotyrosines and iodothyronine analogues to displace tracer[125I] L-3,5,3′ triiodothyronine from specific nuclear binding sites in rat liver and heart was related to the displacement capacity of nonradioactive triiodothyronine. Iodotyrosines and L-3,3′,5′ triiodothyronine ("reverse T3") were devoid of displacement activity. Analogues with 3,5 substitution in the "inner" ring and single "bulk" substitution in the 3′ position in the phenolic ring exhibited the strongest displacement activity. When the distribution, fractional removal rates and metabolic conversion of the analogues were taken into account, displacement activity appeared to correlate well with the reported thyromimetic activity. These results support the biologic relevance of the nuclear sites.
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U2 - 10.1016/0006-291X(73)91177-7
DO - 10.1016/0006-291X(73)91177-7
M3 - Article
C2 - 4357424
AN - SCOPUS:0015818846
SN - 0006-291X
VL - 55
SP - 544
EP - 550
JO - Biochemical and Biophysical Research Communications
JF - Biochemical and Biophysical Research Communications
IS - 3
ER -