The interaction site for tamoxifen aziridine with the bovine estrogen receptor

Journal Article · Tue Aug 15 04:00:00 EDT 1989 · Journal of Biological Chemistry; (USA)

OSTI ID:5547308

Ratajczak, T; Wilkinson, S P; Brockway, M J; Haehnel, R M; Moritz, R L; Begg, G S; Simpson, R J ^[1]

---

1. Univ. of Western Australia, Subiaco

Calf uterine estrogen receptor was covalently labeled with ({sup 3}H)tamoxifen aziridine during affinity chromatography purification. After carboxymethylation, affinity labeled receptor was digested with trypsin under limit conditions and the labeled peptides were fractionated by reversed-phase high performance liquid chromatography into one major and two minor components. Sequence analysis of the dominant labeled fragment indicated the facile cleavage of label during Edman degradation but identified two peptides, both derived from the extreme carboxyl terminus of the steroid-binding domain. The 17 residues of one peptide were fully conserved in all estrogen receptors. This fragment contained five nucleophilic amino acids and was considered as the more favored interaction site for tamoxifen aziridine. A corresponding region of the glucocorticoid receptor has recently been identified as one of three major contact sites for glucocorticoids. A comparison of amino acid physical characteristics in the hormone-binding domains of human estrogen and glucocorticoid receptors demonstrated an excellent structural correlation between the two regions and delineated elements in the estrogen receptor which may be directly involved in estradiol binding.

• OSTI ID: 5547308
• Journal Information: Journal of Biological Chemistry; (USA), Journal Name: Journal of Biological Chemistry; (USA) Vol. 264:23; ISSN JBCHA; ISSN 0021-9258
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AMINO ACID SEQUENCE
ANIMALS
BIOCHEMICAL REACTION KINETICS
BODY
CHROMATOGRAPHY
ESTROGENS
FEMALE GENITALS
FRACTIONATION
HORMONES
HYDROGEN COMPOUNDS
ISOTOPE APPLICATIONS
KINETICS
MAMMALS
MAN
MEMBRANE PROTEINS
MOLECULAR BIOLOGY
MOLECULAR STRUCTURE
MOLECULAR WEIGHT
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PRIMATES
PROTEIN STRUCTURE
PROTEINS
REACTION KINETICS
RECEPTORS
SEPARATION PROCESSES
STEROID HORMONES
TAMOXIFEN
TRACER TECHNIQUES
TRITIUM COMPOUNDS
UTERUS
VERTEBRATES