Related Experiment Video
Updated: May 6, 2026

In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues
Published on: March 21, 2017
Effective antagonists of luteinizing hormone releasing hormone modified at position one
A Janecka1, T Janecki, C Bowers
1Institute for Biomedical Research, The University of Texas at Austin, 78712, Austin, Texas, USA.
Abstract:
The amino acid, D-2-naphthylalanine, has been used by many investigators as a substituent for position one of antagonists of LHRH. We have newly designed substituents for position one in which the carboxy groups of 2-naphthoic acid, 3-quinoline- and 2-quinoxaline-carboxylic acids are linked to the five amino acids, DAla, DThr, DNVal, DSer, and Gly. The substituents in positions 2-10 were DpClPhe(2), DPal(3), Ser(4), PicLys(5), DPicLys(6), Leu(7), ILys(8), Pro(9), DAlaNH2 (10).Remarkably, DThr, acylated on the amino group by 3-quinolinecarboxylic acid or by 3-quinoxalinecarboxylic acid, and introduced into position one of a relatively potent antagonist, gave a new class of antagonists of LHRH, which released as little histamine as yet recorded, and yet possessed reasonable antiovulatory activity and greatly improved solubility.These structure-activity results advance the basic knowledge of understanding the structural features of such decapeptides which cause antiovulatory activity and histamine release.
Related Concept Videos
Hormones of the Pituitary Gland
The most abundantly secreted hormone from the anterior lobe is the growth hormone, which controls overall growth by...
Target Cell Response to Hormones
Notably, the cellular response can be regulated by altering the number of receptors expressed in the cell. For example, prolonged exposure to elevated hormone levels results in a gradual decline or down-regulation in the number of receptors for that specific hormone on the cell surface. Conversely, in response to low hormone levels, cells may use up-regulation, producing an...
Transducer Mechanism: Nuclear Receptors
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
Antiasthma Drugs: Leukotriene Modifiers
Leukotriene modifiers work through two distinct mechanisms:
Drug-Receptor Interaction: Antagonist
Antagonists can be classified as competitive or noncompetitive based on their...

