29 research outputs found
Inhibition of angiogenic initiation and disruption of newly established human vascular networks by juice
from Morinda citrifolia (noni
Plasma Pancreastatin Levels Predict the Outcome of Surgical Cytoreduction in Neuroendocrine Tumors of the Small Bowel
Role of Plasma Pancreastatin in Predicting Prognosis Following R0/R1 Surgical Cytoreduction in Small Bowel Neuroendocrine Tumors
Combination capecitabine/temozolomide (CAPTEM) in patients with neuroendocrine tumors (NETs): A single institution review.
A Pilot Phase 2 Study of Albumin-Bound Rapamycin Nanoparticles, ABI-009, in Patients With Metastatic, Unresectable, Low or Intermediate Grade Neuroendocrine Tumors (NETs) of the Lung or Gastroenteropancreatic System
Novel Synthesis of Various Orthogonally Protected C\u3csup\u3eα\u3c/sup\u3e-Methyllysine Analogues and Biological Evaluation of a Vapreotide Analogue Containing (\u3cem\u3eS\u3c/em\u3e)-α-Methyllysine
Prochiral malonic diesters containing a quaternary carbon center have been successfully transformed into a diverse set of tBoc-Fmoc-α2,2-methyllysine-OH analogues through chiral malonic half-ester intermediates obtained via enzymatic (Pig Liver Esterase, PLE) hydrolysis. The variety of chiral half-ester intermediates, which vary from 1 to 6 methylene units in the side chain, are achieved in moderate to high optical purity and in good yields. The PLE hydrolysis of malonic diesters with various side chain lengths appears to obey the Jones\u27s PLE model according to the stereochemical configurations of the resulting chiral half-esters. The established synthetic strategy allows the construction of both enantiomers of α2,2-methyllysine analogues, and a (S)-β2,2-methyllysine analogue from a common synthon by straightforward manipulation of protecting groups. Two different straightforward and cost effective synthetic strategies are described for the synthesis of α2,2-methyllysine analogues. The described strategies should find significant usefulness in preparing novel peptide libraries with unnatural lysine analogues. A Vapreotide analogue incorporating (S)-α2,2-methyllysine was prepared. However, the Vapreotide analogue with (S)-α-methyl-α-lysine is found to lose its specific binding to somatostatin receptor subtype 2 (SSTR2)