Combinatorial Chemistry & High Throughput Screening - Volume 9, Issue 3, 2006

Although discovered a few decades ago, growth hormone - releasing hormone (GHRH) was thought until recently to have only a single function, namely the regulation of growth hormone release from the pituitary. However, new evidence has provided strong support to the notion that additional physiological and patho-physiological processes, and including carcinogenesis, might be regulated by GHRH. Recently, interest Read More

The development of antagonists of growth hormone (GH) - releasing hormone (GH-RH) is reviewed. GH-RH antagonists bind with a high affinity to pituitary receptors for GH-RH and inhibit the release of GH in vitro and in vivo. The main applications of GH-RH antagonists would be for tumor therapy. The antitumor effects of GH-RH antagonists are exerted in part indirectly through the inhibition of the secretion of pituitary GH Read More

Growth hormone-releasing factor was discovered in 1982 by Guillemin and has been subjected to intense investigations because of its huge potential applications. The major concerns encountered with the native molecules were their short half-lives in vivo in many species including man, precluding the practical use of these peptides for medical or production purposes. Many efforts to produce analogs of shorter length, m Read More

Growth hormone secretagogues (GHSs) are synthetic molecules that stimulate and amplify pulsatile pituitary growth hormone release, via a separate pathway distinct from GH releasing hormone/somatostatin. The activity of GHSs is not fully specific for GH secretion; some GHSs also have slight releasing activity on other pituitary hormones and mediate GH independent biological activities. The first GHSs were discovered in Read More

Novel DNA-based technologies were recently introduced for various purposes, such as screening of targets identified from genomic projects, shuffled molecules for vaccination, or to direct the in vivo production of hormones and other peptides for therapeutic or preventative applications. We have used a plasmid-based technology to deliver growth hormone releasing hormone (GHRH) to various animal species for screenin Read More

Hypothalamic hormones physiologically regulate pulsatile release of growth hormone (GH) from the anterior pituitary gland. Since the discovery of these hormones in the 1970s, several new chemically synthesized peptidyl and nonpeptidyl derivatives have been proved to stimulate and amplify GH secretion, and this series of molecules has been named the growth hormone secretagogues (GHSs). One of these compounds led to Read More

Growth hormone releasing hormone is one of the hormones secreted from the hypothalamus. Because of its potential applications in agriculture and medicine, its short half-life and its expensive chemical synthesis, an analog with high GHRH activity and prolonged half-life was sought after. The fusion partner gene with 127 amino acid residues of the C-terminus from L-asparaginase was recombined with asp-pro-hGHRH(1-44 Read More

The advent of microarray technologies has dramatically accelerated the functional study of proteins, including enzymes (catalomics) in a proteome. Herein, we review recent advances and exciting new developments of microarrays in high-throughput functional proteomics.

Virtual filtering and screening of combinatorial libraries have recently gained attention as methods complementing the high-throughput screening and combinatorial chemistry. These chemoinformatic techniques rely heavily on quantitative structure-activity relationship (QSAR) analysis, a field with established methodology and successful history. In this review, we discuss the computational methods for building QSAR models. W Read More

A new strategy to obtain pure ionic liquid support with a high loading (3 mmol/g) of primary amino groups is reported. The compatibility of the imidazolium unit was demonstrated with DIC or DCC coupling reactions of protected amino acids and with classical cleavage of BOC or Fmoc protecting groups. In addition, this is the first report of a traceless ionic liquid support based on a silicon linker with a high loading (3 mm Read More

Dr. Hippokratis Kiaris received his B.Sc. in 1993 from the Department of Biology at the University of Athens and his Ph.D. in 1996 from the University of Crete, Greece. His post doctoral training was accomplished in the laboratories of the Nobel Laureate, Professor Andrew V. Schally at Tulane University, New Orleans, LA and Professor Spyros Artavanis-Tsakonas, Harvard Medical School, Boston, MA, USA. Since 2003 he jo Read More