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Disease
Symptom
Drug
Enzyme
Compound
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Target Concepts:
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Query: UNIPROT:P61278 (
somatostatin
)
22,083
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
The antiproliferative activity of two new
somatostatin
(SS) analogs:
ASS
-51 and
ASS
-52 have been tested in this study. We assessed their ability to inhibit the DNA synthesis in normal colon crypt cells and in the cells of chemically (dimethylhydrazine)-induced colon cancer in the rats. The incorporation of bromodeoxyuridine (BrDU) into appropriate cell nuclei was used as an index of DNA synthesis. It was found that: 1) Only
ASS
-51 significantly decreases the colon crypt cell proliferation in the rat when compared to controls. Since both analogs were previously shown to inhibit GH release, these data indicate that the antiproliferogenic effect of
ASS
-51 is independent of the inhibition of GH release. 2) Both examined analogs did not significantly effect the BrDU incorporation into cell nuclei of chemically-induced colon cancer.
...
PMID:Effects of new somatostatin analogs on the cell proliferation of colonic crypts and colonic cancers in rats. 810 12
The effects of
somatostatin
analogues octreotide (SMS 201-995),
ASS
-51 and
ASS
-52 on [3H]-thymidine incorporation into DNA of the murine colon 38 cancer cells in vitro were investigated. It was found that SMS 201-995 and
ASS
-51 inhibited the tritiated thymidine incorporation in a dose-dependent manner. In contrast, analogue
ASS
-52 in spite of a very similar structure to
ASS
-51, which differed from the latter only by one CH2OH group, was devoid of remarkable antiproliferative activity. These results indicate that slight modification of the molecule of
somatostatin
analogues may deeply influence their antiproliferative activity.
...
PMID:Differential effects of somatostatin analogues on proliferation of murine colonic cancer cells in vitro. 941 16
The in vivo effects of three new analogs of
somatostatin
(
ASS
-51,
ASS
-52 and
ASS
-53 analogs) on GH, insulin and glucagon were studied in WKY rats. The solid phase method was used for the synthesis of
ASS
. Octreotide and
ASS
were given iv. in a dose of 0.05 &mgr;g/kg per animal in a time-dependent manner.
ASS
-52 and
ASS
-53 were longer acting and more potent
somatostatin
analogs when compared to octreotide in producing the inhibition of GH.
ASS
-51 was found to be the most potent and selective inhibitor of insulin and glucagon release. Our results show that the increased inhibitory effect and the higher selectivity of the new
somatostatin
analogs may result from the differences in their chemical structure.
ASS
-52 is most active in inhibiting GH release. The mechanism by which
ASS
-52 inhibits preferentially GH release may involve the opioid system and the activation of GABA-ergic receptors. In studies in vitro
ASS
-52 inhibited GH release from pituitary cells" culture.
...
PMID:New analogs of somatostatin: inhibiting effectively GH, glucagon and insulin levels. 1146 19