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001-es BibID:	BIBFORM005093
Első szerző:	Panyi György (biofizikus)
Cím:	K+ channel blockers : novel tools to inhibit T cell activation leading to specific immunosuppression / Panyi, G., Possani, L. D., Rodriguez de la Vega R. C., Gaspar, R., Varga, Z.
Dátum:	2006
ISSN:	381-6128 (Print)
Megjegyzések:	During the last two decades since the identification and characterization of T cell potassium channels great advances have been made in the understanding of the role of these channels in T cell functions, especially in antigen-induced activation. Their limited tissue distribution and the recent discovery that different T cell subtypes carrying out distinct immune functions show specific expression levels of these channels have made T cell potassium channels attractive targets for immunomodulatory drugs. Many toxins of various animal species and a structurally diverse array of small molecules inhibiting these channels with varying affinity and selectivity were found and their successful use in immunosuppression in vivo was also demonstrated. Better understanding of the topological differences between potassium channel pores, detailed knowledge of toxin and small-molecule structures and the identification of the binding sites of blocking compounds make it possible to improve the selectivity and affinity of the lead compounds by introducing modifications based on structural information. In this review the basic properties and physiological roles of the voltage-gated Kv1.3 and the Ca2+-activated IKCa1 potassium channels are discussed along with an overview of compounds inhibiting these channels and approaches aiming at producing more efficient modulators of immune functions for the treatment of diseases like sclerosis multiplex and type I diabetes.
Tárgyszavak:	Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban Amino Acid Sequence Animal Animals Binding Sites Biophysics chemistry Cnidarian Venoms Drug Design drug effects Humans Hungary immunology Immunosuppression Immunosuppressive Agents Intermediate-Conductance Calcium-Activated Potassium Channels Ion Channel Gating Kv1.3 Potassium Channel Lymphocyte Activation metabolism Models, Molecular Molecular Sequence Data Molecular Structure pharmacology Potassium Potassium Channel Blockers Potassium Channels Protein Conformation Pyrazoles Quinolines Research Structure-Activity Relationship Support T-Lymphocytes Toxins
Megjelenés:	Current Pharmaceutical Design. - 12 : 18 (2006), p. 2199-2220. -
További szerzők:	Possani, Lourival Domingos Rodriguez de la Vega, Ricardo C. Gáspár Rezső (1944-) (biofizikus) Varga Zoltán (1969-) (biofizikus, szakfordító)
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