Synthesis and sst(2) binding profiles of new [Tyr(3)]octreotate analogs

Journal of Peptide Science : an Official Publication of the European Peptide Society
Christos PetrouPaul Cordopatis

Abstract

One of the main objectives of our current work is the development of new somatostatin analogs that would retain the general characteristics of [Tyr(3)]octreotate (Tate) while showing potential for clinical application. In this respect, study of their interaction with the sst(2) is crucial in providing preliminary structure-activity relationships data. In the present work we report on the synthesis and the preliminary biological evaluation of a total of 15 new structurally modified [Tyr(3)]octreotate analogs. The binding affinities were determined during competition binding assays in sst(2)-positive rat acinar pancreatic AR4-2J cell membranes using [(125)I-Tyr(3)]octreotide as the radioligand.

References

Sep 4, 1975·The New England Journal of Medicine·D J KoerkerC J Goodner
Jan 1, 1992·Annual Review of Physiology·M J Lewin
Mar 1, 1990·International Journal of Peptide and Protein Research·G B Fields, R L Noble
Jul 2, 1981·Nature·D F VeberR Hirschmann
Dec 22, 1983·The New England Journal of Medicine·S Reichlin
Mar 1, 1994·International Journal of Cancer. Journal International Du Cancer·J C ReubiJ Laissue
Dec 1, 1995·Cellular and Molecular Neurobiology·T Reisine
May 26, 1998·Reviews of Physiology, Biochemistry and Pharmacology·W Meyerhof
Aug 6, 1999·Frontiers in Neuroendocrinology·Y C Patel
Mar 29, 2001·Chemotherapy·C BousquetC Susini
Jan 5, 2002·Annals of Oncology : Official Journal of the European Society for Medical Oncology·L J Hofland, S W Lamberts
Apr 20, 2002·Seminars in Nuclear Medicine·Marion De JongEric P Krenning
May 25, 2002·European Journal of Nuclear Medicine and Molecular Imaging·Theodosia MainaEfstratios Chiotellis
Oct 18, 2002·Biopolymers·Sylvie Froidevaux, Alex N Eberle
Jul 8, 2003·European Journal of Nuclear Medicine and Molecular Imaging·Clemens DecristoforoRoy Moncayo

❮ Previous
Next ❯

Citations


❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.