Showing papers by "Fernando Pelaez published in 1993"
TL;DR: Two newZaragozic acids D and D2 have been isolated from the keratinophilic fungus Amauroascus niger and inhibit farnesyl transferase with IC50 values of 100 nM, while zaragoZic acids A and B are less potent.
Abstract: Two new zaragozic acids, D and D 2 , have been isolated from the keratinophilic fungus Amauroascus niger. Zaragozic acids D [4] and D 2 [5] are related to the previously describe zaragozic acids A [1], B [2], and C [3] and are potent inhibitors of squalene synthase. Furthermore, all the zaragozic acids (A, B, C, D, and D 2 ) ate also active against farnesyl transferase. Zaragozic acids D and D 2 inhibit farnesyl transferase with IC 50 values of 100 nM, while zaragozic acids A and B are less potent
54 citations
TL;DR: Chaetomellic acids A and B, isolated from Chaetomella acutiseta, are specific inhibitors of farnesyl-protein transferase that do not inhibit geranylgeranyl transferase type 1 or squalene synthase.
Abstract: Chaetomellic acids A and B, isolated from Chaetomella acutiseta, are specific inhibitors of farnesyl-protein transferase that do not inhibit geranylgeranyl transferase type 1 or squalene synthase. Chaetomellic acids A and B are reversible inhibitors, resemble farnesyl diphosphate and probably inhibit FPTase by substituting for farnesyl diphosphate. Chaetomellic acid production appears to be widespread within the genus Chaetomella.
49 citations
TL;DR: In this article, a novel bistropolone, pycnidione (1), was isolated by bioassay guided fractionation from fermentations of a Phoma sp., the structure was determined by spectroscopic methods and single crystal X-ray diffraction.
46 citations
Patent•
11 Mar 1993TL;DR: In this article, a compound of Structural Formula I has been shown to have endothelin antagonist activity and is therefore useful in treating cardiovascular disorders, such as hypertension, congestive heart failure, postischemic renal failure vasospasm, cerebral and cardia ischemia, myocardial infarction inflammatory diseases, Raynaud's disease, endotoxin shock and asthma.
Abstract: Fermentation processes for the production of a compound of the Structural Formula I ##STR1## The compound of Structural Formula I has been shown to have endothelin antagonist activity and is therefore useful in treating cardiovascular disorders, such as hypertension, congestive heart failure, postischemic renal failure vasospasm, cerebral and cardia ischemia, myocardial infarction inflammatory diseases, Raynaud's disease, endotoxin shock and asthma.
25 citations
TL;DR: In this paper, a novel bistropolone, pycnidione (1), was isolated by bioassay guided fractionation from fermentations of a Phoma sp., the structure was determined by spectroscopic methods and single crystal X-ray diffraction.
Abstract: A novel bistropolone, pycnidione (1), was isolated by bioassay guided fractionation from fermentations of a Phoma sp.. The structure was determined by spectroscopic methods and single crystal X-ray diffraction.
3 citations
Patent•
22 Sep 1993TL;DR: A compound of the formula 1:STR1## is produced via fermentation of a fungal isolate ATCC no. 74235 as mentioned in this paper, and a process for production of the compound, a pharmaceutical composition and a method of treatment.
Abstract: A compound of the formula 1: ##STR1## is produced via fermentation of a fungal isolate ATCC no. 74235. The organism is included herein, as well as a process for production of the compound, a pharmaceutical composition and a method of treatment.
2 citations
TL;DR: The zaragozic acid C (1) has been shown to be a potent inhibitor of squalene synthase as mentioned in this paper, achieving an apparent K i of 45 ± 15 pM.
Abstract: The novel zaragozic acid C ( 1 ) has been isolated as a potent inhibitor of squalene synthase. It was found to be a competitive inhibitor of rat liver squalene synthase with an apparent K i of 45 ± 15 pM, and a broad spectrum antifungal agent against both yeast and filamentous fungi.
1 citations