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Cover Picture: Discovery of Riociguat (BAY 63‐2521): A Potent, Oral Stimulator of Soluble Guanylate Cyclase for the Treatment of Pulmonary Hypertension (ChemMedChem 5/2009)
Author(s) -
Mittendorf Joachim,
Weigand Stefan,
AlonsoAlija Cristina,
Bischoff Erwin,
Feurer Achim,
Gerisch Michael,
Kern Armin,
Knorr Andreas,
Lang Dieter,
Muenter Klaus,
Radtke Martin,
Schirok Hartmut,
Schlemmer KarlHeinz,
Stahl Elke,
Straub Alexander,
Wunder Frank,
Stasch JohannesPeter
Publication year - 2009
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200990020
Subject(s) - riociguat , gucy1a3 , guanosine triphosphate , cyclic guanosine monophosphate , sildenafil , guanosine monophosphate , guanosine , gucy1b3 , guanylate cyclase , nitric oxide , chemistry , soluble guanylyl cyclase , second messenger system , pulmonary hypertension , signal transduction , pharmacology , enzyme , gtp' , medicine , biochemistry , guanylate cyclase 2c , nucleotide , gene
The cover picture shows a schematic representation of soluble guanylate cyclase (sGC). This key signal‐transduction enzyme is typically found as a heterodimer, consisting of a larger α‐subunit and a smaller haeme‐binding β‐subunit. It is activated by the ubiquitous messenger nitric oxide and catalyzes the conversion of guanosine‐5′‐triphosphate (GTP) into the second messenger cyclic guanosine‐3′,5′‐monophosphate (cGMP). The depicted compound is riociguat, which was identified as a potent, oral sGC stimulator and is currently being investigated in phase III clinical trials for the treatment of pulmonary hypertension. For more details, see the Full Paper by J. Mittendorf et al. on p. 853 ff.