Peptoids as endothelin receptor antagonists

Dasgupta, Falguni; Gangadhar, N.; Miriyala, Bruhaspathy; Verma, A. K.; Sarin, Simi; Mukherjee, Ashish K.

doi:10.1016/s0960-894x(01)00009-9

Cited by 4 publications

(3 citation statements)

References 28 publications

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“…222 While most regulators were rationally designed based on natural peptide ligands, [223][224][225][226][227][228] some researchers have applied combinatorial peptoid libraries to identify receptor agonists and antagonists capable of modulating cellular signaling pathways using microarray-assisted high-throughput screening methods. [229][230][231][232] Kodadek et al synthesized an OBOC library to identify regulators of the orexin receptor 1, a potential target for treating insomnia, diabetes, and drug addiction. They exposed their library to differentially labeled cells with or without the receptor of interest to identify hit compounds.…”

Section: Combinatorial Hit Compounds Address Distinct Components Of Protein Complexes and Ribonucleic Acidsmentioning

confidence: 99%

Bio-instructive materials on-demand – combinatorial chemistry of peptoids, foldamers, and beyond

et al. 2021

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Section: Combinatorial Hit Compounds Address Distinct Components Of Protein Complexes and Ribonucleic Acidsmentioning

confidence: 99%

Bio-instructive materials on-demand – combinatorial chemistry of peptoids, foldamers, and beyond

et al. 2021

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“…(21)). In an effort [123] to quickly discover a new lead based on the available information the minimum structural motif was perceived as one with a carboxylic residue suitably juxtaposed. The simplest of them was envisaged as N,Ndisubstituted amino acids i.e., peptoids.…”

Section: Miscellaneousmentioning

confidence: 99%

Endothelin Receptor Antagonists: An Overview of Their Synthesis and Structure-Activity Relationship

Iqbal¹,

Sanghi²,

Das

2005

MRMC

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Endothelins (ETs) are potent vasoconstrictor peptides and are associated with several disease states like pulmonary hypertension, systemic hypertension and heart failure. Endothelin-1 (ET-1) is the first member of the family and it has the receptor subtypes known as ETA and ETB. The receptors ETA and ETB are attractive new therapeutic targets for diseases associated with elevated ET-1 levels. Several studies have thus led to the discovery of selective ETA receptor antagonists as well as non-selective ETA/ETB antagonists. The preclinical and clinical studies have clearly established that these antagonists are effective in the treatment of essential hypertension, pulmonary hypertension, heart failure and atherosclerosis. The advances in this area have resulted in the FDA approval of the orally active dual antagonist Bosentan for pulmonary hypertension in 2001. This review highlights the synthesis and structure-activity of the endothelin receptor antagonists and covers the literature in this area up to 2001.

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“…Ciba (Japan) discovered IRL1722, essentially a N-acylated Trp, a lead, which was optimized to give IRL2659 with high activity (ET B 0.23 nM, ET A 54 nM). More recently, in an attempt to come up with new leads, several N, N-disubstituted Tyr and Trp were synthesized to give the first series of peptoids as ETantagonists [47].…”

Section: Et and Et Antagonistsmentioning

confidence: 99%

Endothelin Receptor Antagonists - An Overview

Dasgupta¹,

Mukherjee²,

Gangadhar³

2002

CMC

Self Cite

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In thirteen years since the appearance of Endothelin (ET) on the international scene, possibility of its involvement in a variety of diseases has attracted the attention of medicinal chemists in search of novel therapeutics for various cardiovascular diseases (CVDs). Discovery of pharmaceutical agents which either block the generation of ET from its precursor or antagonize its binding to cellular receptor, should not only provide means to assess the physiological role of ET, but lead to useful therapy for conditions associated with altered production or responsiveness to ET. In this review article, we have attempted to present in a classified format, the kaleidoscope of ET receptor antagonists that have emerged through structure activity relationship studies using the parent peptide as well as from screening of various compound libraries. By all indications, the variety and range of small molecules that are currently under investigation continues to open up newer opportunities and lures fresh groups of scientists into this research arena. Presently a number of these compounds are in the clinics, being evaluated for their beneficial effects in a range of human pathologies such as essential hypertension and chronic heart failure.

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Peptoids as endothelin receptor antagonists

Cited by 4 publications

References 28 publications

Bio-instructive materials on-demand – combinatorial chemistry of peptoids, foldamers, and beyond

Bio-instructive materials on-demand – combinatorial chemistry of peptoids, foldamers, and beyond

Endothelin Receptor Antagonists: An Overview of Their Synthesis and Structure-Activity Relationship

Endothelin Receptor Antagonists - An Overview

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