(Q34563752)

3 August 2017

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title

Targeting proteases: successes, failures and future prospects (English)

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3 August 2017

Boris Turk

1

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publication date

1 September 2006

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Nature Reviews Drug Discovery

3 August 2017

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3 August 2017

5

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3 August 2017

9

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3 August 2017

785-799

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https://scigraph.springernature.com/pub.10.1038/nrd2092

3 August 2017

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Regulating cysteine protease activity: essential role of protease inhibitors as guardians and regulators

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Bowman-Birk inhibitor abates proteasome function and suppresses the proliferation of MCF7 breast cancer cells through accumulation of MAP kinase phosphatase-1.

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Urokinase-type plasminogen activator (uPA) and its receptor (uPAR): development of antagonists of uPA/uPAR interaction and their effects in vitro and in vivo

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Intracellular and extracellular cathepsin B facilitate invasion of MCF-10A neoT cells through reconstituted extracellular matrix in vitro

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Identification of a Potent and Selective Noncovalent Cathepsin S Inhibitor

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Arylaminoethyl amides as inhibitors of the cysteine protease cathepsin K-investigating P1' substituents

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Searching for new allosteric sites in enzymes

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Discovery of an allosteric site in the caspases

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Small-molecule antagonists of apoptosis suppressor XIAP exhibit broad antitumor activity

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Importance of the hinge region between alpha-helix F and the main part of serpins, based upon identification of the epitope of plasminogen activator inhibitor type 1 neutralizing antibodies

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Therapeutic potential of renin inhibitors in the management of cardiovascular disorders

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31 March 2020

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31 March 2020

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31 March 2020

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Dipeptidyl-peptidase IV hydrolyses gastric inhibitory polypeptide, glucagon-like peptide-1(7-36)amide, peptide histidine methionine and is responsible for their degradation in human serum

31 March 2020

1 reference

Degradation of glucose-dependent insulinotropic polypeptide and truncated glucagon-like peptide 1 in vitro and in vivo by dipeptidyl peptidase IV

31 March 2020

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Enhanced insulin secretion and improved glucose tolerance in mice lacking CD26.

31 March 2020

1 reference

Improved glucose tolerance via enhanced glucose-dependent insulin secretion in dipeptidyl peptidase IV-deficient Fischer rats

31 March 2020

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Inhibitors of dipeptidyl peptidase IV: a novel approach for the prevention and treatment of Type 2 diabetes?

31 March 2020

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31 March 2020

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31 March 2020

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31 March 2020

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31 March 2020

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Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes

31 March 2020

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31 March 2020

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Deficiency of CD26 results in a change of cytokine and immunoglobulin secretion after stimulation by pokeweed mitogen.

31 March 2020

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Pycnodysostosis, a lysosomal disease caused by cathepsin K deficiency

31 March 2020

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Impaired osteoclastic bone resorption leads to osteopetrosis in cathepsin-K-deficient mice

31 March 2020

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Cathepsin K Knockout Mice Develop Osteopetrosis Due to a Deficit in Matrix Degradation but Not Demineralization

31 March 2020

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Accelerated turnover of metaphyseal trabecular bone in mice overexpressing cathepsin K

31 March 2020

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Molecular cloning of human cDNA for cathepsin K: novel cysteine proteinase predominantly expressed in bone

31 March 2020

1 reference

Potent and selective inhibition of human cathepsin K leads to inhibition of bone resorption in vivo in a nonhuman primate

31 March 2020

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Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.

31 March 2020

1 reference

Revised definition of substrate binding sites of papain-like cysteine proteases

31 March 2020

1 reference

Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity

31 March 2020

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6. Cathepsin K inhibitors: their potential as anti-osteoporosis agents

31 March 2020

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31 March 2020

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Antimetastatic activity of a novel mechanism-based gelatinase inhibitor

31 March 2020

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A highly specific inhibitor of matrix metalloproteinase-9 rescues laminin from proteolysis and neurons from apoptosis in transient focal cerebral ischemia.

31 March 2020

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Potent mechanism-based inhibitors for matrix metalloproteinases

31 March 2020

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Early diagnosis of osteoarthritis using cathepsin B sensitive near-infrared fluorescent probes

31 March 2020

1 reference

The major cysteine proteinase of Trypanosoma cruzi: a valid target for chemotherapy of Chagas disease

31 March 2020

1 reference

On the size of the active site in proteases. I. Papain

31 March 2020

1 reference

A caspase-activated DNase that degrades DNA during apoptosis, and its inhibitor ICAD

31 March 2020

1 reference

Complementation cloning of S2P, a gene encoding a putative metalloprotease required for intramembrane cleavage of SREBPs

31 March 2020

1 reference

Ubiquitination and deubiquitination: targeting of proteins for degradation by the proteasome

31 March 2020

1 reference

Structure of human dipeptidyl peptidase I (cathepsin C): exclusion domain added to an endopeptidase framework creates the machine for activation of granular serine proteases

31 March 2020

1 reference

The serpins are an expanding superfamily of structurally similar but functionally diverse proteins. Evolution, mechanism of inhibition, novel functions, and a revised nomenclature

31 March 2020

1 reference

Mechanism of inhibition of the human matrix metalloproteinase stromelysin-1 by TIMP-1

31 March 2020

1 reference

Mechanism of XIAP-mediated inhibition of caspase-9

31 March 2020

1 reference

X-linked IAP is a direct inhibitor of cell-death proteases

31 March 2020

1 reference

Lysosomal cysteine proteases: more than scavengers

31 March 2020

1 reference

Major histocompatibility complex class II-associated p41 invariant chain fragment is a strong inhibitor of lysosomal cathepsin L

31 March 2020

1 reference

31 March 2020

Identifiers

DOI

10.1038/NRD2092

1 reference

3 August 2017

1 reference

PubMed ID

16955069