Literature DB >> 20540510

Bivalent diketopiperazine-based tropomysin receptor kinase C (TrkC) antagonists.

Jing Liu1, Fouad Brahimi, H Uri Saragovi, Kevin Burgess.   

Abstract

Bivalent molecules containing two beta-turn mimics with side chains that correspond to hot-spots on the neurotrophin NT-3 were prepared. Binding assays showed the mimetics to be selective TrkC ligands, and biological assays showed one mimetic to be an antagonist of the TrkC receptor.

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Year:  2010        PMID： 20540510      PMCID： PMC2907676          DOI： 10.1021/jm100148d

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  20 in total

1.  Genuine monovalent ligands of TrkA nerve growth factor receptors reveal a novel pharmacological mechanism of action.

Authors:  S Maliartchouk; T Debeir; N Beglova; A C Cuello; K Gehring; H U Saragovi
Journal:  J Biol Chem       Date:  2000-04-07       Impact factor: 5.157

2.  Solid-phase SN2 macrocyclization reactions to form beta-turn mimics.

Authors:  Y Feng; M Pattarawarapan; Z Wang; K Burgess
Journal:  Org Lett       Date:  1999-07-15       Impact factor: 6.005

Review 3.  Neurotrophin small-molecule mimetics.

Authors:  Y Xie; F M Longo
Journal:  Prog Brain Res       Date:  2000       Impact factor: 2.453

4.  New templates for syntheses of ring-fused, C(10) beta-turn peptidomimetics leading to the first reported small-molecule mimic of neurotrophin-3.

Authors:  Mookda Pattarawarapan; Maria Clara Zaccaro; Uri H Saragovi; Kevin Burgess
Journal:  J Med Chem       Date:  2002-09-26       Impact factor: 7.446

Review 5.  Neurotrophin signaling via Trks and p75.

Authors:  W J Friedman; L A Greene
Journal:  Exp Cell Res       Date:  1999-11-25       Impact factor: 3.905

6.  Nerve growth factor (NGF) loop 4 dimeric mimetics activate ERK and AKT and promote NGF-like neurotrophic effects.

Authors:  Y Xie; M A Tisi; T T Yeo; F M Longo
Journal:  J Biol Chem       Date:  2000-09-22       Impact factor: 5.157

Review 7.  Neurotrophin signal transduction in the nervous system.

Authors:  D R Kaplan; F D Miller
Journal:  Curr Opin Neurobiol       Date:  2000-06       Impact factor: 6.627

8.  Entry to new conformationally constrained amino acids. First synthesis of 3-unsubstituted 4-alkyl-4-carboxy-2-azetidinone derivatives via an intramolecular N(alpha)-C(alpha)-cyclization strategy.

Authors:  G Gerona-Navarro; M A Bonache; R Herranz; M T García-López; R González-Muñiz
Journal:  J Org Chem       Date:  2001-05-18       Impact factor: 4.354

Review 9.  Small molecule Trk receptor agonists and other neurotrophic factor mimetics.

Authors:  Scott J Pollack; Sarah J Harper
Journal:  Curr Drug Targets CNS Neurol Disord       Date:  2002-02

10.  A peptidomimetic of NT-3 acts as a TrkC antagonist.

Authors:  Fouad Brahimi; Andrey Malakhov; Hong Boon Lee; Mookda Pattarawarapan; Lubijca Ivanisevic; Kevin Burgess; H Uri Saragovi
Journal:  Peptides       Date:  2009-07-30       Impact factor: 3.750
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  9 in total

1.  Design, synthesis, and validation of a β-turn mimetic library targeting protein-protein and peptide-receptor interactions.

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2.  Diastereoselective synthesis of diketopiperazine bis-α,β-epoxides.

Authors:  Shin Ando; Amy L Grote; Kazunori Koide
Journal:  J Org Chem       Date:  2011-01-20       Impact factor: 4.354

3.  Cyclic cis-Locked Phospho-Dipeptides Reduce Entry of AβPP into Amyloidogenic Processing Pathway.

Authors:  Carolyn L Fisher; Ross J Resnick; Soumya De; Lucila A Acevedo; Kun Ping Lu; Frank C Schroeder; Linda K Nicholson
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4.  Low molecular weight, non-peptidic agonists of TrkA receptor with NGF-mimetic activity.

Authors:  D Scarpi; D Cirelli; C Matrone; G Castronovo; P Rosini; E G Occhiato; F Romano; L Bartali; A M Clemente; G Bottegoni; A Cavalli; G De Chiara; P Bonini; P Calissano; A T Palamara; E Garaci; M G Torcia; A Guarna; F Cozzolino
Journal:  Cell Death Dis       Date:  2012-07-05       Impact factor: 8.469

5.  Combinatorial assembly of small molecules into bivalent antagonists of TrkC or TrkA receptors.

Authors:  Fouad Brahimi; Eunhwa Ko; Andrey Malakhov; Kevin Burgess; H Uri Saragovi
Journal:  PLoS One       Date:  2014-03-06       Impact factor: 3.240

Review 6.  Cyclic Dipeptides: The Biological and Structural Landscape with Special Focus on the Anti-Cancer Proline-Based Scaffold.

Authors:  Joanna Bojarska; Adam Mieczkowski; Zyta M Ziora; Mariusz Skwarczynski; Istvan Toth; Ahmed O Shalash; Keykavous Parang; Shaima A El-Mowafi; Eman H M Mohammed; Sherif Elnagdy; Maha AlKhazindar; Wojciech M Wolf
Journal:  Biomolecules       Date:  2021-10-14

7.  Developing bivalent ligands to target CUG triplet repeats, the causative agent of myotonic dystrophy type 1.

Authors:  Yuan Fu; Kali A Miller; Lien Nguyen; Amin Haghighat Jahromi; Long M Luu; Anne M Baranger; Steven C Zimmerman
Journal:  J Med Chem       Date:  2013-11-21       Impact factor: 7.446

8.  The diketopiperazine-fused tetrahydro-β-carboline scaffold as a model peptidomimetic with an unusual α-turn secondary structure.

Authors:  Francesco Airaghi; Andrea Fiorati; Giordano Lesma; Manuele Musolino; Alessandro Sacchetti; Alessandra Silvani
Journal:  Beilstein J Org Chem       Date:  2013-01-22       Impact factor: 2.883

9.  Targeted PDT agent eradicates TrkC expressing tumors via photodynamic therapy (PDT).

Authors:  Chin Siang Kue; Anyanee Kamkaew; Hong Boon Lee; Lip Yong Chung; Lik Voon Kiew; Kevin Burgess
Journal:  Mol Pharm       Date:  2014-12-09       Impact factor: 4.939
  9 in total

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