Peptide receptor targeting in cancer: the somatostatin paradigm

F Barbieri, A Bajetto, A Pattarozzi… - … journal of peptides, 2013‏ - Wiley Online Library
Peptide receptors involved in pathophysiological processes represent promising therapeutic
targets. Neuropeptide somatostatin (SST) is produced by specialized cells in a large number …

Somatostatin, somatostatin analogs and somatostatin receptor dynamics in the biology of cancer progression

M Ruscica, M Arvigo, L Steffani… - Current molecular …, 2013‏ - benthamdirect.com
The pharmacological effects (ie, inhibition of endocrine secretion and cell proliferation)
mediated by the hormone somatostatin (SRIF) are derived from its universal high-affinity …

Stereoselective synthesis of P-stereogenic aminophosphines: ring opening of bulky oxazaphospholidines

T Leon, A Riera, X Verdaguer - Journal of the American Chemical …, 2011‏ - ACS Publications
A highly diastereoselective and efficient synthesis of P-stereogenic bulky alkyl and aryl
aminophosphines that relies on ring opening of tert-butyl-oxazaphospholidine 2 is …

MaxPHOS Ligand: PH/NH Tautomerism and Rhodium‐Catalyzed Asymmetric Hydrogenations

E Cristóbal‐Lecina, P Etayo, S Doran… - … synthesis & catalysis, 2014‏ - Wiley Online Library
MaxPHOS is an active and robust P‐stereogenic ligand for asymmetric catalysis. The
presence of an NH bridge between the two phosphine moieties allows the NH/PH …

A tetradecapeptide somatostatin dicarba-analog: Synthesis, structural impact and biological activity

P Martín-Gago, R Ramón, E Aragón… - Bioorganic & medicinal …, 2014‏ - Elsevier
We described here the first tetradecapeptide somatostatin-analogue where the disulfide
bridge has been replaced by a carbon–carbon double bond. This analogue was prepared …

Fine-tuning the [Pi]-[Pi]. Aromatic interactions in peptides: somatostatin analogues containing mesityl alanine

P Martín-Gago, M Gomez-Caminals… - … Edition, 2012, vol. 51 …, 2012‏ - diposit.ub.edu
Going through the motions: Somatostatin analogues having greater conformational rigidity
than somatostatin have been prepared by substituting Phe residues in the native sequence …

Nickel (II) and palladium (II) complexes of the small-bite-angle P-stereogenic diphosphine ligand MaxPHOS and its monosulfide

A Grabulosa, S Doran, G Brandariz, G Muller… - …, 2014‏ - ACS Publications
Coordination studies of the optically pure diphosphine ligand (t-Bu) 2P (NH) P (t-
BuMe)(MaxPHOS) and its monosulfide with several Pd and Ni moieties are described …

[HTML][HTML] Insights into structure-activity relationships of somatostatin analogs containing mesitylalanine

P Martín-Gago, E Aragón, M Gomez-Caminals… - Molecules, 2013‏ - mdpi.com
The non-natural amino acid mesitylalanine (2, 4, 6-trimethyl-L-phenylalanine; Msa) has an
electron-richer and a more conformationally restricted side-chain than that of its natural …

Synthetic peptide analogs of somatostatin: trends in the synthesis of and prospects in the search for new anticancer drugs

AN Balaev, VN Osipov, DS Khachatryan - Pharmaceutical Chemistry …, 2015‏ - Springer
The native hormone somatostatin plays an important role in vivo by acting on multiple
targets via a family of five receptors to produce a broad spectrum of biological effects. Some …

N-Imidazolebenzyl-histidine Substitution in Somatostatin and in Its Octapeptide Analogue Modulates Receptor Selectivity and Function

J Erchegyi, R Cescato, B Waser, JE Rivier… - Journal of medicinal …, 2011‏ - ACS Publications
Despite 3 decades of focused chemical, biological, structural, and clinical developments,
unusual properties of somatostatin (SRIF, 1) analogues are still being uncovered. Here we …