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Target Concepts:
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Query: DrugBank:EXPT01586 (
G418
)
2,237
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Somatostatin (SS) is known to have an antiproliferative effect on cell growth via somatostatin receptors (SSTR). The purpose of this study was to transfect cell lines with human
SSTR2
and determine the subsequent effect on cell growth in response to SSTR agonist. Heterologous Chinese hamster ovary (CHO-K1) and human embryonic kidney 293 (HEK) cells were transfected with
SSTR2
cDNA using lipofectin. Stable transformants were selected by
G418
and confirmed by 125I-SS binding and RT-PCR. Binding studies were performed in the presence of 10(-6) to 10(-12) M SS-14, SS-28, SS analogue RC-160,
SSTR2
agonist NC-9-74, and SSTR5 agonist DC-37-39. Cell growth was determined by counting cell numbers after 48 hr incubation in the presence of 10(-6) to 10(-12) M
SSTR2
agonist NC-9-74. Binding of 125I-SS-14 to transfected CHO and transfected HEK293 cells showed that the cells had high affinity for SS-14, SS-28, NC-9-74, and RC-160 but low affinity for DC-37-39. Incubation with 10(-6) to 10(-12) M NC-9-74, showed that 1 nM to 1 microM NC-9-74 significantly inhibited transfected HEK293 cell growth but did not affect growth on transfected CHO cells (n = 4 for each dose, P < 0.01). The two cell lines transfected with the human
SSTR2
showed similar high affinity for SS-14, SS-28, RC-160, and
SSTR2
agonist but not SSTR5 agonist. The
SSTR2
agonist NC-9-74 significantly inhibited transfected HEK293 cell growth but not CHO cells. These data suggest that activation of
SSTR2
was more efficiently coupled to the signal transduction pathway of antiproliferation in the transfected HEK293 cells.
...
PMID:Activation of human somatostatin receptor type 2 causes inhibition of cell growth in transfected HEK293 but not in transfected CHO cells. 927 Dec 72