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Literature DB >> 21168329

New furin inhibitors based on weakly basic amidinohydrazones.

Frank Sielaff¹, Manuel E Than, Dorian Bevec, Iris Lindberg, Torsten Steinmetzer.

Abstract

A novel series of amidinohydrazone-derived furin inhibitors was prepared; the most potent compounds 17 and 21 inhibit furin with K(i) values of 0.46 and 0.59μM, respectively. In contrast to inhibitor 17, which still contains a guanidino residue, compound 21 possesses only weakly basic amidinohydrazone groups. Copyright Â

Entities: Chemical Disease Gene Species

Mesh：

Substances：
Amidines
Hydrazones
Furin

Year: 2010 PMID： 21168329 PMCID： PMC4737580 DOI： 10.1016/j.bmcl.2010.11.092

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

16 in total

1. Specific inhibition of c-Raf activity by semapimod induces clinical remission in severe Crohn's disease.

Authors: Mark Löwenberg; Auke Verhaar; Bernt van den Blink; Fibo ten Kate; Sander van Deventer; Maikel Peppelenbosch; Daniel Hommes
Journal: J Immunol Date: 2005-08-15 Impact factor: 5.422

2. 2,6-Dichlorobenzylidene amino guanidine acetate (Wy-8678). A new hypotensive agent.

Authors: T Baum; D K Eckfeld; N Metz; J L Dinish; G Rowles; R Van Pelt; A T Shropshire; S P Fernandez; M I Gluckman; W F Bruce
Journal: Experientia Date: 1969-10-15

Review 3. Inhibitors of proprotein convertases.

Authors: Ajoy Basak
Journal: J Mol Med (Berl) Date: 2005-10-08 Impact factor: 4.599

4. Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.

Authors: P Ulrich; A Cerami
Journal: J Med Chem Date: 1984-01 Impact factor: 7.446

5. An inhibitor of macrophage arginine transport and nitric oxide production (CNI-1493) prevents acute inflammation and endotoxin lethality.

Authors: M Bianchi; P Ulrich; O Bloom; M Meistrell; G A Zimmerman; H Schmidtmayerova; M Bukrinsky; T Donnelley; R Bucala; B Sherry
Journal: Mol Med Date: 1995-03 Impact factor: 6.354

6. Inhibition of furin/proprotein convertase-catalyzed surface and intracellular processing by small molecules.

Authors: Tomoko Komiyama; Julia M Coppola; Martha J Larsen; Marcian E van Dort; Brian D Ross; Robert Day; Alnawaz Rehemtulla; Robert S Fuller
Journal: J Biol Chem Date: 2009-03-30 Impact factor: 5.157

7. The crystal structure of the proprotein processing proteinase furin explains its stringent specificity.

Authors: Stefan Henrich; Angus Cameron; Gleb P Bourenkov; Reiner Kiefersauer; Robert Huber; Iris Lindberg; Wolfram Bode; Manuel E Than
Journal: Nat Struct Biol Date: 2003-07

8. The guanylhydrazone CNI-1493: an inhibitor with dual activity against malaria-inhibition of host cell pro-inflammatory cytokine release and parasitic deoxyhypusine synthase.

Authors: Sabine Specht; Salem Ramadan Sarite; Ilona Hauber; Joachim Hauber; Ulf F Görbig; Chris Meier; Dorian Bevec; Achim Hoerauf; Annette Kaiser
Journal: Parasitol Res Date: 2008-02-07 Impact factor: 2.289

Review 4. Why All the Fury over Furin?

Authors: Essam Eldin A Osman; Alnawaz Rehemtulla; Nouri Neamati
Journal: J Med Chem Date: 2021-08-02 Impact factor: 7.446

4 in total

New furin inhibitors based on weakly basic amidinohydrazones.

1. Specific inhibition of c-Raf activity by semapimod induces clinical remission in severe Crohn's disease.

2. 2,6-Dichlorobenzylidene amino guanidine acetate (Wy-8678). A new hypotensive agent.

Review 3. Inhibitors of proprotein convertases.

4. Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.

5. An inhibitor of macrophage arginine transport and nitric oxide production (CNI-1493) prevents acute inflammation and endotoxin lethality.

6. Inhibition of furin/proprotein convertase-catalyzed surface and intracellular processing by small molecules.

7. The crystal structure of the proprotein processing proteinase furin explains its stringent specificity.

8. The guanylhydrazone CNI-1493: an inhibitor with dual activity against malaria-inhibition of host cell pro-inflammatory cytokine release and parasitic deoxyhypusine synthase.

9. Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics.

Review 10. Cutting back on pro-protein convertases: the latest approaches to pharmacological inhibition.

1. Highly potent inhibitors of proprotein convertase furin as potential drugs for treatment of infectious diseases.

2. Purification of the proprotein convertase furin by affinity chromatography based on PC-specific inhibitors.

3. Dichlorophenylpyridine-Based Molecules Inhibit Furin through an Induced-Fit Mechanism.

Review 4. Why All the Fury over Furin?