Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:3.4.24.55 (
PTR
)
433
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Cyclo(PheN2-Tyr-D-Trp-Lys-Val-PheC3)-Thr-NH2 (
PTR
3046), a backbone-cyclic somatostatin analogue, was synthesized by solid-phase methodology. The binding characteristics of
PTR
3046 to the different somatostatin receptors, expressed in CHO cells, indicate high selectivity to the SSTR5 receptor.
PTR
3046 is highly stable against enzymatic degradation as determined in vitro by incubation with rat renal homogenate and human serum. The biological activity of
PTR
3046 in vivo was determined in rats.
PTR
3046 inhibits
bombesin
- and caerulein-induced amylase and lipase release from the pancreas without inhibiting growth hormone or glucagon release. The major conformation of
PTR
3046 in CD3OH, as determined by NMR, is defined by a type II' beta-turn at D-Trp-Lys and a cis amide bond at Val-PheC3.
...
PMID:A backbone-cyclic, receptor 5-selective somatostatin analogue: synthesis, bioactivity, and nuclear magnetic resonance conformational analysis. 952 66
