Selectivity (pharmacology)

In pharmacology, selectivity denotes either limited binding to a few molecules ( binding selectivity ) or the production of one or more effects from a spectrum of activity ( functional selectivity ).

If an active ingredient binds more strongly to a target protein and less to others, it binds selectively , e.g. B. binds a transcription factor only to certain DNA sequences . If it binds particularly strongly to one and negligibly weakly to other target proteins, then it binds specifically . If an active ingredient binds to a target protein and thereby sets one of all possible signal transduction processes in motion and thus differs from similar active ingredients, then it has a functionally selective effect . If an active ingredient binds to two different target proteins and causes different effects on them, z. B. on one receptor as a full agonist and on the other as an antagonist , one speaks here of a functionally selective or specific effect.

Individual evidence

↑ A. Tarcsay, GM Keser ?: Is there a link between selectivity and binding thermodynamics profiles? In: Drug discovery today. [electronic publication before going to press] September 2014, ISSN 1878-5832 . doi : 10.1016 / j.drudis.2014.09.014 . PMID 25263698 .

^ Y. Pan, CJ Tsai, B. Ma, R. Nussinov: Mechanisms of transcription factor selectivity. In: Trends in genetics: TIG. Volume 26, Number 2, February 2010, pp. 75-83, ISSN 0168-9525 . doi : 10.1016 / j.tig.2009.12.003 . PMID 20074831 .

[1] A. Tarcsay, GM Keser ?: Is there a link between selectivity and binding thermodynamics profiles? In: Drug discovery today. [electronic publication before going to press] September 2014, ISSN 1878-5832 . doi : 10.1016 / j.drudis.2014.09.014 . PMID 25263698 .

[2] Y. Pan, CJ Tsai, B. Ma, R. Nussinov: Mechanisms of transcription factor selectivity. In: Trends in genetics: TIG. Volume 26, Number 2, February 2010, pp. 75-83, ISSN 0168-9525 . doi : 10.1016 / j.tig.2009.12.003 . PMID 20074831 .