Edward M. Devine

Anti-WISP1 (MTX-463) as a Novel Potential Therapy for Idiopathic Pulmonary Fibrosis

Gordon E. Dower, Benjamin T. Wilks, Christopher W. Espelin, Sudip Nepal et autres

Inhibition of farnesyltransferase with A-176120, a novel and potent farnesyl pyrophosphate analogue

Sajid Khan Tahir, Wen‐Zhen Gu, H.-C Zhang, Juan H. Leal et autres

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Second-Generation Peptidomimetic Inhibitors of Protein Farnesyltransferase Demonstrating Improved Cellular Potency and Significant in Vivo Efficacy

Stephen J. O’Connor, Kenneth J. Barr, Le Wang, Bryan K. Sorensen et autres

The synthesis and evaluation of analogues of previously reported farnesyltransferase inhibitors, pyridyl benzyl ether 3 and pyridylbenzylamine 4, are described. Substitution of 3 at the 5-position of the core aryl ring resulted in inhibitors of equal or less potency against the enzyme …

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Potent and Selective Non-Cysteine-Containing Inhibitors of Protein Farnesyltransferase

David J. Augeri, Stephen J. O’Connor, Dave Janowick, Bruce G. Szczepankiewicz et autres

Potent and selective non-thiol-containing inhibitors of protein farnesyltransferase are described. FTI-276 (1) was transformed into pyridyl ether analogue 19. The potency of pyridyl ether 19 was improved by modification of the biphenyl core to that of an o-tolyl substituted biphenyl core to …

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HPLC and PDMS analysis of cleavage products aid in the design of small, stable ANP analogues

Edward M. Devine, Alexander M. Buko, Steven Cepa, Steven K. Davidsen et autres

The degradation of a prototypical small analogue of atrial natriuretic peptide (ANP) has been studied using HPLC and mass spectrometric techniques. These studies revealed that removal of the N-terminal amino acid was the primary catabolic event in vitro. Based on this information …

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Small atrial natriuretic peptide analogs: design, synthesis, and structural requirements for guanylate cyclase activation

Thomas W von Geldern, Todd W. Rockway, Steven K. Davidsen, Gerald P. Budzik et autres

Structure/activity studies on atrial natriuretic peptide ANP (1-28) have highlighted three portions of the native molecule as necessary for its biological responses. We have linked these three regions and excised the remaining segments to produce a family of small analogues (less than …

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Ring expansion leads to enhanced potency in small atrial natriuretic peptide (ANP) analogs

Thomas W von Geldern, Todd W. Rockway, Steven K. Davidsen, Gerald P. Budzik et autres

Truncated atrial natriuretic factor analogs retain full agonist activity

William H. Holleman, Gerald P. Budzik, Edward M. Devine, David M. Pollock et autres

The synthesis, receptor binding, and agonist activity of a series of truncated atrial natriuretic analogs (ANF) are described. These analogs incorporate two portions of the native 28 amino peptide, the eight amino acids C-terminal to Cys7, and two amino acids from the …

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Characterization and Partial Purification of Endothelin-Converting Enzyme in Rat Lung

Jinshyun R. Wu‐Wong, Edward M. Devine, Gerald P. Budzik, Terry J. Opgenorth

Endothelin-1 (ET-1) was originally identified in the culture supernatant of porcine aortic endothelial cells. From the deduced amino acid sequence, a biosynthetic pathway has been proposed that a prepro- form of porcine ET-1 is initially processed by dibasic pair proteolysis to a …

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Characterization of endothelin converting enzyme in rat lung

Jinshyun R. Wu‐Wong, Gerald P. Budzik, Edward M. Devine, Terry J. Opgenorth

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Conformationally constrained peptide analogs of atrial natriuretic factor (ANF)

Todd W. Rockway, Edward T. Olejniczak, Edward M. Devine, Gerald P. Budzik et autres

Structure-activity relationships of atrial natriuretic factor (ANF) receptor agonists

Todd W. Rockway, Peter J. Connolly, Edward M. Devine, Gerald P. Budzik et autres