Abstract：
:A new analogue of recombinant human growth hormone (hGH), hGH des(1-6,14) was expressed in Escherichia coli, refolded and purified to homogeneity. The mutation decreased the hormone's ability to bind lactogenic and somatogenic receptors through its site 1, and almost completely abolished its ability to bind these receptors through site 2, as evidenced by both binding and gel-filtration experiments. More specifically, the binding to prolactin receptors (PRLRs) from various species or their soluble recombinant extracellular domains (ECDs) was decreased 1.5-4-fold, whereas the binding to hGH receptor (hGHR) was decreased 10-85-fold. These changes caused an almost total loss of hormone agonistic activity in several in vitro bioassays and subsequently, the hGH des(1-6,14) analogue acquired antagonistic properties. This antagonistic activity was dependent upon modification of site 1. In those cases in which the binding was reduced only slightly, e.g. binding to rabbit PRLRs, hGH des(1-6,14) acted as a strong antagonist, whereas in others in which the binding of site 1 was reduced to a higher degree, such as other PRLRs and, in particular, hGHR, the antagonistic activity was correspondingly weaker. Circular dichroism spectra of the analogue suggested that these changes do not result from a decrease in overall alpha-helix content, but rather from minor local structural modifications at the N-terminus.
journal_name
Mol Cell Endocrinoljournal_title
Molecular and cellular endocrinologyauthors
Tchelet A,Vogel T,Helman D,Guy R,Neospouolus C,Goffin V,Djiane J,Gertler Adoi
10.1016/s0303-7207(97)00084-1subject
Has Abstractpub_date
1997-06-20 00:00:00pages
141-52issue
1-2eissn
0303-7207issn
1872-8057pii
S0303-7207(97)00084-1journal_volume
130pub_type
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