Protease inhibitors in the clinic.

Protease inhibitors in the clinic. Research Abstract Details 

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Protease inhibitors in the clinic. Abstract Text:

This review describes the clinical status (based on available information) of experimental drugs that inhibit enzymes called proteases, or more precisely a sub-class of proteases called peptidases that catalyse the hydrolysis of polypeptide main chain amide bonds. These peptidases are classified by the key catalytic residue in the active site of the enzyme that effects hydrolysis, namely aspartic, serine, cysteine, metallo or threonine proteases. In this review we show structures for 108 inhibitors of these enzymes and update the clinical disposition of over 100 inhibitors that have been considered worthy enough by pharmaceutical, biotechnology or academic researchers and their financial backers to be trialed in humans as prospective medicines. We outline some of their chemical and pharmacological characteristics and compare the current status of protease inhibitors in the clinic with what was observed about 5 years ago (Leung et al, J. Med. Chem. 2000, 43, 305-341). We assess the progress of protease inhibitors into man, predict their futures, and outline some of the hurdles that have been overcome and that still remain for this promising class of new therapeutic agents.

Protease inhibitors in the clinic. Publishing Authors By Initials

For similar proteins: tissue inhibitor of metalloproteinases research abstracts see: proteins: tissue inhibitor of metalloproteinases research

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Protease inhibitors in the clinic. Journal Published:

PUBLICATION TYPE: Review

Journal: Medicinal chemistry (Sh?riqah (United Arab Emirate

VOLUME: 1

Page Numbers: 71-104

Journal Abbreviation:

ISSN: 1573-4064

DAY: 26

MONTH: Jan

YEAR: 2005

Protease inhibitors in the clinic. Information

Number of References: 245

LANGUAGE: eng

NlmUniqueID: 101240303

Protease inhibitors in the clinic. Keywords Mesh Terms:

KEYWORDS: Tissue Inhibitor of Metalloproteinases

MESH TERMS: pharmacology

Chemical & Substance for Abstract: Protease inhibitors in the clinic. Information

Substance Name: Aspartic Endopeptidases

Registry Number: EC 3.4.23.-

Grant and Affiliation Information for Protease inhibitors in the clinic.

AFFILIATION: Centre for Drug Design and Development, Institute for Molecular Bioscience, University of Queensland, Brisbane, Qld 4072, Australia. d.fairlie@imb.uq.edu.au.

Country: United Arab Emirates

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MEDLINETA: Med Chem

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