PMID- 7536037
OWN - NLM
STAT- MEDLINE
DCOM- 19950517
LR  - 20200107
IS  - 0006-2960 (Print)
IS  - 1520-4995 (Electronic)
IS  - 0006-2960 (Linking)
VI  - 34
IP  - 15
DP  - 1995 Apr 18
TI  - Synthesis and interaction of fluorescent thapsigargin derivatives with the 
      sarcoplasmic reticulum ATPase membrane-bound region.
PG  - 5137-42
AB  - Fluorescent derivatives of thapsigargin (TG) were synthesized by replacing the 
      C8-butanoyl chain with a dansyl (DTG) or eosin (ETG) moiety. DTG and ETG retain 
      the inhibitory effect of TG on the sarcoplasmic reticulum (SR) ATPase, displaying 
      a 2 and 10 microM Ki, respectively. Steady state and lifetime fluorescence 
      measurements are consistent with energy transfer between tryptophanyl residues 
      assigned to the ATPase membrane-bound region and DTG. This phenomenon exhibits 
      saturation behavior, occurs in the presence of DTG concentrations producing 
      ATPase inhibition, and is partially prevented by inhibitory concentrations of TG. 
      Although long range conformational effects of TG binding affect the fluorescence 
      properties of endogenous tryptophans as well as of a fluorescein 
      5'-isothiocyanate (FITC) label of the ATPase extramembranous region, no 
      significant energy transfer was detected between DTG and the FITC label. It is 
      concluded that the inhibitors partition within the membrane and the binding 
      domain resides within or near the membrane-bound region of the ATPase.
FAU - Hua, S
AU  - Hua S
AD  - Department of Biological Chemistry, School of Medicine, University of Maryland, 
      Baltimore 21201, USA.
FAU - Malak, H
AU  - Malak H
FAU - Lakowicz, J R
AU  - Lakowicz JR
FAU - Inesi, G
AU  - Inesi G
LA  - eng
GR  - P41 RR008119/RR/NCRR NIH HHS/United States
GR  - RR-08119/RR/NCRR NIH HHS/United States
GR  - HL27867-13/HL/NHLBI NIH HHS/United States
GR  - GM-35154/GM/NIGMS NIH HHS/United States
PT  - Journal Article
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - United States
TA  - Biochemistry
JT  - Biochemistry
JID - 0370623
RN  - 0 (Dansyl Compounds)
RN  - 0 (Fluorescent Dyes)
RN  - 0 (Sesquiterpenes)
RN  - 0 (dansylthapsigargin)
RN  - 0 (eosinthapsigargin)
RN  - 67526-95-8 (Thapsigargin)
RN  - 8DUH1N11BX (Tryptophan)
RN  - EC 7.2.2.10 (Calcium-Transporting ATPases)
RN  - I223NX31W9 (Fluorescein-5-isothiocyanate)
RN  - TDQ283MPCW (Eosine Yellowish-(YS))
SB  - IM
MH  - Animals
MH  - Calcium-Transporting ATPases/*antagonists & inhibitors
MH  - Dansyl Compounds/chemical synthesis/chemistry/*pharmacology
MH  - Eosine Yellowish-(YS)/*analogs & derivatives/chemical 
      synthesis/chemistry/pharmacology
MH  - Fluorescein-5-isothiocyanate/chemistry
MH  - Fluorescent Dyes/chemical synthesis/chemistry/*pharmacology
MH  - In Vitro Techniques
MH  - Rabbits
MH  - Sarcoplasmic Reticulum/*enzymology
MH  - Sesquiterpenes/chemical synthesis/chemistry/*pharmacology
MH  - Spectrometry, Fluorescence
MH  - *Thapsigargin/*analogs & derivatives
MH  - Tryptophan/chemistry
PMC - PMC6943342
MID - NIHMS1065607
EDAT- 1995/04/18 00:00
MHDA- 1995/04/18 00:01
PMCR- 2020/01/06
CRDT- 1995/04/18 00:00
PHST- 1995/04/18 00:00 [pubmed]
PHST- 1995/04/18 00:01 [medline]
PHST- 1995/04/18 00:00 [entrez]
PHST- 2020/01/06 00:00 [pmc-release]
AID - 10.1021/bi00015a026 [doi]
PST - ppublish
SO  - Biochemistry. 1995 Apr 18;34(15):5137-42. doi: 10.1021/bi00015a026.