INVESTIGATIONS ON AN ANDROGEN-BINDING COMPONENT FROM COHN'S PLASMA FRACTION IV—4

1975 ◽  
Vol 80 (1_Suppla) ◽  
pp. S122
Author(s):  
W. Miscke ◽  
D. Graesslin ◽  
J. Tamm
Keyword(s):  
Plasma Fraction ◽  
Androgen Binding ◽  
Binding Component

Evidence for an androgen binding component in human placental cytosol

1982 ◽  
Vol 16 (2) ◽  
pp. 311-315 ◽  
Author(s):  
M.A. Younes ◽  
N.F. Besch ◽  
P.K. Besch
Keyword(s):  
Androgen Binding ◽  
Binding Component

ANDROGEN AND OESTROGEN BINDING IN CYTOSOLS OF HUMAN OVARIAN TUMOURS

1981 ◽  
Vol 90 (3) ◽  
pp. 421-431 ◽  
Author(s):  
T. C. HAMILTON ◽  
P. DAVIES ◽  
K. GRIFFITHS
Keyword(s):  
Progesterone Receptor ◽  
Binding Sites ◽  
Sedimentation Coefficient ◽  
Oestrogen Receptors ◽  
Histopathological Classification ◽  
High Affinity ◽  
Ovarian Tumours ◽  
Specific Retention ◽  
Androgen Binding ◽  
Binding Component

The specific retention of androgens and oestrogens by cytoplasmic components of human ovarian tumours was investigated. High-affinity, low-capacity binding of androgens was observed in 88% of tumour specimens and oestrogen binding in 32%. Retention of oestrogens did not occur in the absence of androgen binding. The androgen-binding component, of sedimentation coefficient 7·5–8·5S, showed specificity for 5α-dihydrotestosterone and 17β-hydroxy-17α-methyl-estra-4,9,11-trien-3-one (R1881). In some instances, competition for R1881-binding sites indicated the presence of progesterone receptor-like binding. The data presented suggest strongly the existence of androgen and oestrogen receptors in some ovarian tumours and may be relevant to histopathological classification and therapeutic rationales.

Presence of androgen receptors in the hen hypothalamus and pituitary

1989 ◽  
Vol 120 (2) ◽  
pp. 217-224 ◽  
Author(s):  
Mitsuo Kawashima ◽  
Michiharu Kamiyoshi ◽  
Katuhide Tanaka
Keyword(s):  
Marked Decrease ◽  
Soluble Fraction ◽  
Direct Action ◽  
Insoluble Fraction ◽  
Ovulatory Cycle ◽  
Buffer Solution ◽  
Hypotonic Buffer ◽  
Androgen Binding ◽  
Binding Component

Abstract. Soluble and insoluble fractions in a hypotonic buffer solution of hypothalamic-preoptic and median eminence areas, and of the anterior pituitary of the hen were found to contain a specific androgen binding component having the properties of a receptor. Administration of testosterone in vivo caused a marked decrease in specific [3H]R1881 (a synthetic androgen) bindings in the soluble fraction with a concomitant increase in the bindings in the insoluble fraction, whereas the sum of the bindings did not change. A similar relationship between the bindings of the two fractions was also observed during an ovulatory cycle. The results may provide an evidence for a direct action of androgens on the hen hypothalamus and pituitary.

scholarly journals Development of an Androgen Receptor Inhibitor Targeting the N-Terminal Domain of Androgen Receptor for Treatment of Castration Resistant Prostate Cancer

Cancers ◽  
2021 ◽  
Vol 13 (14) ◽  
pp. 3488
Author(s):  
Fuqiang Ban ◽  
Eric Leblanc ◽  
Ayse Derya Cavga ◽  
Chia-Chi Flora Huang ◽  
Mark R. Flory ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Androgen Receptor ◽  
Splice Variants ◽  
Full Length ◽  
Cancer Resistance ◽  
Castration Resistant Prostate Cancer ◽  
Terminal Domain ◽  
Castration Resistant ◽  
Coregulatory Proteins ◽  
Androgen Binding

Prostate cancer patients undergoing androgen deprivation therapy almost invariably develop castration-resistant prostate cancer. Resistance can occur when mutations in the androgen receptor (AR) render anti-androgen drugs ineffective or through the expression of constitutively active splice variants lacking the androgen binding domain entirely (e.g., ARV7). In this study, we are reporting the discovery of a novel AR-NTD covalent inhibitor 1-chloro-3-[(5-([(2S)-3-chloro-2-hydroxypropyl]amino)naphthalen-1-yl)amino]propan-2-ol (VPC-220010) targeting the AR-N-terminal Domain (AR-NTD). VPC-220010 inhibits AR-mediated transcription of full length and truncated variant ARV7, downregulates AR response genes, and selectively reduces the growth of both full-length AR- and truncated AR-dependent prostate cancer cell lines. We show that VPC-220010 disrupts interactions between AR and known coactivators and coregulatory proteins, such as CHD4, FOXA1, ZMIZ1, and several SWI/SNF complex proteins. Taken together, our data suggest that VPC-220010 is a promising small molecule that can be further optimized into effective AR-NTD inhibitor for the treatment of CRPC.

scholarly journals Properdin: Preparation from Plasma Fraction I of the Cohn Method

1959 ◽  
Vol 234 (4) ◽  
pp. 838-840
Author(s):  
Daniel S. Spicer ◽  
Lois I. Priester ◽  
Edward V.C. Smith ◽  
Benjamin E. Sanders
Keyword(s):  
Plasma Fraction ◽  
Fraction I

scholarly journals A Further Study of a Testosterone-binding Component of Human Pregnancy Serum

1969 ◽  
Vol 244 (5) ◽  
pp. 1373-1380
Author(s):  
W H Pearlman ◽  
I F F Fong ◽  
J H Tou
Keyword(s):  
Human Pregnancy ◽  
Binding Component

scholarly journals Estrogen Receptor β Expression and Apoptosis of Spermatocytes of Mice Overexpressing a Rat Androgen-Binding Protein Transgene1

2004 ◽  
Vol 71 (5) ◽  
pp. 1461-1468 ◽  
Author(s):  
David M. Selva ◽  
Oscar M. Tirado ◽  
Nuria Toràn ◽  
Carlos A. Suárez-Quian ◽  
Jaume Reventos ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Binding Protein ◽  
Estrogen Receptor Β ◽  
Androgen Binding Protein ◽  
Androgen Binding
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