FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2129337629> ?p ?o ?g. }

• W2129337629 endingPage "117" @default.
• W2129337629 startingPage "103" @default.
• W2129337629 abstract "Linkage of a 11beta-chloromethyl group to estradiol-17beta (E2) dramatically increases the binding affinity of the steroid for the estrogen receptor (ER) with the formation of a quasi-irreversible steroid-receptor complex. We have synthesized the two isomers of 11beta-chloromethyl-17alpha-iodovinyl-estradiol (E-CMIV and Z-CMIV) by a novel route. Both derivatives demonstrated high binding affinity and selectivity for ER (RBAs: ER = 820 and 1008; SHBG = 1.2 and 0.25, respectively; E2 = 100). On the basis of X-ray crystallographic data for Z-CMIV and its precursor, we have postulated that Z-CMIV might interact strongly with aromatic amino-acids within a hydrophobic groove of the ER hormone binding domain (HBD) that incorporates pockets corresponding to the 11beta and 17alpha steroid substituents. The binding properties of Z-CMIV labeled with 125I were investigated, especially its ability to detect and quantify altered ER forms with low binding affinity for E2. Sucrose density gradient analysis revealed that Z-CMIV has a higher activation potency than E2 as it converts a higher proportion of non-activated monomers in the cytosol into activated monomers with the potential to dimerize. In in vitro (MCF-7 cells) and in vivo (rat uterus) determinations of estrogenic activity, Z-CMIV was as potent as E2 in increasing progesterone receptor (PgR) concentrations and decreasing ER levels and in stimulating uterine growth. [125I]-Z-CMIV could open the way to new applications in the diagnosis and therapy of ER-positive breast cancers, especially those containing altered (variant) ERs." @default.
• W2129337629 created "2016-06-24" @default.
• W2129337629 creator A5017377435 @default.
• W2129337629 creator A5017654335 @default.
• W2129337629 creator A5029342831 @default.
• W2129337629 creator A5043813927 @default.
• W2129337629 creator A5046997582 @default.
• W2129337629 creator A5058240202 @default.
• W2129337629 creator A5066527595 @default.
• W2129337629 creator A5082934839 @default.
• W2129337629 date "1996-09-01" @default.
• W2129337629 modified "2023-09-27" @default.
• W2129337629 title "Synthesis, structure and biological properties of Z-17α-(2-iodovinyl)-11β-chloromethyl estradiol-17β (Z-CMIV), a high affinity ligand for the characterization of estrogen receptor-positive tumors" @default.
• W2129337629 cites W1968425544 @default.
• W2129337629 cites W1983649348 @default.
• W2129337629 cites W1986898144 @default.
• W2129337629 cites W1991025172 @default.
• W2129337629 cites W1992988804 @default.
• W2129337629 cites W1994842495 @default.
• W2129337629 cites W1997082598 @default.
• W2129337629 cites W2009652784 @default.
• W2129337629 cites W2009810465 @default.
• W2129337629 cites W2016674616 @default.
• W2129337629 cites W2022666359 @default.
• W2129337629 cites W2023690921 @default.
• W2129337629 cites W2029028017 @default.
• W2129337629 cites W2031494992 @default.
• W2129337629 cites W2041190166 @default.
• W2129337629 cites W2042901562 @default.
• W2129337629 cites W2044658849 @default.
• W2129337629 cites W2046109253 @default.
• W2129337629 cites W2052132909 @default.
• W2129337629 cites W2055773540 @default.
• W2129337629 cites W2056755200 @default.
• W2129337629 cites W2061625266 @default.
• W2129337629 cites W2061648353 @default.
• W2129337629 cites W2071000246 @default.
• W2129337629 cites W2082899881 @default.
• W2129337629 cites W2093758418 @default.
• W2129337629 cites W2094341910 @default.
• W2129337629 cites W2132268003 @default.
• W2129337629 cites W2170273915 @default.
• W2129337629 cites W2326278607 @default.
• W2129337629 cites W3005306837 @default.
• W2129337629 cites W4231214341 @default.
• W2129337629 doi "https://doi.org/10.1016/s0960-0760(96)00007-6" @default.
• W2129337629 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/9009243" @default.
• W2129337629 hasPublicationYear "1996" @default.
• W2129337629 type Work @default.
• W2129337629 sameAs 2129337629 @default.
• W2129337629 citedByCount "14" @default.
• W2129337629 countsByYear W21293376292012 @default.
• W2129337629 countsByYear W21293376292017 @default.
• W2129337629 countsByYear W21293376292018 @default.
• W2129337629 crossrefType "journal-article" @default.
• W2129337629 hasAuthorship W2129337629A5017377435 @default.
• W2129337629 hasAuthorship W2129337629A5017654335 @default.
• W2129337629 hasAuthorship W2129337629A5029342831 @default.
• W2129337629 hasAuthorship W2129337629A5043813927 @default.
• W2129337629 hasAuthorship W2129337629A5046997582 @default.
• W2129337629 hasAuthorship W2129337629A5058240202 @default.
• W2129337629 hasAuthorship W2129337629A5066527595 @default.
• W2129337629 hasAuthorship W2129337629A5082934839 @default.
• W2129337629 hasConcept C116569031 @default.
• W2129337629 hasConcept C121608353 @default.
• W2129337629 hasConcept C126322002 @default.
• W2129337629 hasConcept C134018914 @default.
• W2129337629 hasConcept C170493617 @default.
• W2129337629 hasConcept C181199279 @default.
• W2129337629 hasConcept C185592680 @default.
• W2129337629 hasConcept C202751555 @default.
• W2129337629 hasConcept C2777164284 @default.
• W2129337629 hasConcept C2780902042 @default.
• W2129337629 hasConcept C530470458 @default.
• W2129337629 hasConcept C55493867 @default.
• W2129337629 hasConcept C71240020 @default.
• W2129337629 hasConcept C71315377 @default.
• W2129337629 hasConcept C71924100 @default.
• W2129337629 hasConcept C84606932 @default.
• W2129337629 hasConcept C86803240 @default.
• W2129337629 hasConcept C98539663 @default.
• W2129337629 hasConcept C98717036 @default.
• W2129337629 hasConceptScore W2129337629C116569031 @default.
• W2129337629 hasConceptScore W2129337629C121608353 @default.
• W2129337629 hasConceptScore W2129337629C126322002 @default.
• W2129337629 hasConceptScore W2129337629C134018914 @default.
• W2129337629 hasConceptScore W2129337629C170493617 @default.
• W2129337629 hasConceptScore W2129337629C181199279 @default.
• W2129337629 hasConceptScore W2129337629C185592680 @default.
• W2129337629 hasConceptScore W2129337629C202751555 @default.
• W2129337629 hasConceptScore W2129337629C2777164284 @default.
• W2129337629 hasConceptScore W2129337629C2780902042 @default.
• W2129337629 hasConceptScore W2129337629C530470458 @default.
• W2129337629 hasConceptScore W2129337629C55493867 @default.
• W2129337629 hasConceptScore W2129337629C71240020 @default.
• W2129337629 hasConceptScore W2129337629C71315377 @default.
• W2129337629 hasConceptScore W2129337629C71924100 @default.
• W2129337629 hasConceptScore W2129337629C84606932 @default.

• next