Allosteric Regulation of the Hormone and Growth Factor Receptors
A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Immunology".
Deadline for manuscript submissions: closed (31 July 2023) | Viewed by 2363
Special Issue Editors
Interests: signal transduction; allosteric site; allosteric regulator; positive allosteric modulator; negative allosteric modulator; hormone; growth factor; cytokine; heterotrimeric G-protein; adenylyl cyclase; G-protein-coupled receptor; tyrosine kinase receptor; cytokine receptor; receptor complex; insulin; leptin; interleukin; epidermal growth factor; central nervous system; endocrine system; neurodegeneration
Special Issues, Collections and Topics in MDPI journals
Interests: signal transduction; allosteric site; allosteric regulator; positive allosteric modulator; negative allosteric modulator; hormone; growth factor; cytokine; heterotrimeric G-protein; adenylyl cyclase; G-protein-coupled receptor; tyrosine kinase receptor; cytokine receptor; receptor complex; insulin; leptin; interleukin; epidermal growth factor; central nervous system; endocrine system; neurodegeneration
Special Issue Information
Dear Colleagues,
Hormones, growth factors, cytokines, and other signaling molecules, by specifically binding to the orthosteric (high-affinity) site of G protein-coupled receptors (GPCRs), tyrosine kinases receptors and cytokine receptors, cause their activation and mediate the transmission of an external signal to intracellular signaling cascades. As a result, an adequate cellular response to hormonal stimuli is ensured. At the same time, the regulation of the activity of these receptors can be carried out by interacting with allosteric regulators, which specifically, but with a lower affinity, interact with allosteric sites localized in the extracellular, intracellular, and transmembrane domains of the receptors. These sites are targets for compounds with the activity of the positive (PAM), negative (NAM) and silent (SAM) allosteric modulators, as well as for compounds with the activity of the full and inverse allosteric agonists. At present, a large number of endogenous allosteric regulators and modulators have been identified, including metal cations, lipids, steroid hormones, amino acids, peptides, proteins, etc. The most important role in the etiology and pathogenesis of autoimmune diseases belongs to specific antibodies that specifically interact with receptor allosteric sites. In recent years, an intensive search and study of new allosteric regulators have been carried out, which is due to significant progress in establishing the structural and functional organization of receptor allosteric sites. They have a number of significant advantages over orthosteric site ligands (high specificity for closely related receptors, bias agonism, moderate activation or inhibition of the receptor), and are also able to modulate the regulatory effects of orthosteric agonists and influence the stability of homo- and heterooligomeric receptor complexes.
A Special Issue of the International Journal of Molecular Sciences is devoted to the prospects and unresolved problems of allosteric regulation of receptors, and the main topics will be: (1) search, design and development of allosteric regulators of GPCRs, tyrosine kinases receptors and cytokine receptors, (2) molecular mechanisms of action of the endogenous and artificial allosteric regulators, (3) structure and functions of receptor allosteric sites, (4) the allosteric control of receptor oligomerization; (5) allosteric regulators/modulators-based drugs; (6) effects of allosteric regulators on cellular processes, (7) impaired allosteric regulation and diseases. The content of Special Issue is not limited to these topics.
Authors are invited to submit original and review articles for publication in this Special Issue of IJMS.
Prof. Dr. Alexander Shpakov
Dr. Kira V. Derkach
Guest Editors
Manuscript Submission Information
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Keywords
- signal transduction
- allosteric site
- allosteric regulator
- positive allosteric modulator
- negative allosteric modulator
- hormone
- growth factor
- cytokine
- heterotrimeric G-protein
- adenylyl cyclase
- G-protein-coupled receptor
- tyrosine kinase receptor
- cytokine receptor
- receptor complex
- insulin
- leptin
- interleukin
- epidermal growth factor
- central nervous system
- endocrine system
- neurodegeneration
