Chem Biol Drug Des. 2007 Sep;70(3):268-72.

Bipiperidinyl carboxylic acid amides as potent, selective, and functionally active CCR4 antagonists.

Kuhn CF, Bazin M, Philippe L, Zhang J, Tylaska L, Miret J, Bauer PH.

Source

Pfizer Research Technology Center, 620 Memorial Drive, Cambridge, MA 02139, USA. cyrille.f.kuhn@pfizer.com

Abstract

A cell-based assay for the chemokine G-protein-coupled receptor CCR4 was developed, and used to screen a small-molecule compound collection in a multiplex format. A series of bipiperidinyl carboxylic acid amides amenable to parallel chemistry were derived that were potent and selective antagonists of CCR4. One prototype compound was shown to be active in a functional model of chemotaxis, making it a useful chemical tool to explore the role of CCR4 in asthma, allergy, diabetes, and cancer.

PMID:: 17718722; [PubMed - indexed for MEDLINE]

MeSH Terms, Substances

MeSH Terms

Substances

LinkOut - more resources

Full Text Sources

Other Literature Sources

Labome Researcher Resource - ExactAntigen/Labome

Chemical Information

BindingDB

Supplemental Content

Save items

Related citations in PubMed

Racemic and chiral lactams as potent, selective and functionally active CCR4 antagonists. [Bioorg Med Chem Lett. 2004]
Racemic and chiral lactams as potent, selective and functionally active CCR4 antagonists.
Newhouse B, Allen S, Fauber B, Anderson AS, Eary CT, Hansen JD, Schiro J, Gaudino JJ, Laird E, Chantry D, et al. Bioorg Med Chem Lett. 2004 Nov 15; 14(22):5537-42.
Optimization of CCR4 antagonists: side-chain exploration. [Bioorg Med Chem Lett. 2006]
Optimization of CCR4 antagonists: side-chain exploration.
Purandare AV, Wan H, Gao A, Somerville J, Burke C, Vaccaro W, Yang X, McIntyre KW, Poss MA. Bioorg Med Chem Lett. 2006 Jan 1; 16(1):204-7. Epub 2005 Oct 19.
Core exploration in optimization of chemokine receptor CCR4 antagonists. [Bioorg Med Chem Lett. 2007]
Core exploration in optimization of chemokine receptor CCR4 antagonists.
Purandare AV, Wan H, Somerville JE, Burke C, Vaccaro W, Yang X, McIntyre KW, Poss MA. Bioorg Med Chem Lett. 2007 Feb 1; 17(3):679-82. Epub 2006 Nov 2.
Review Antagonists of CCR4 as immunomodulatory agents. [Curr Top Med Chem. 2006]
Review Antagonists of CCR4 as immunomodulatory agents.
Purandare AV, Somerville JE. Curr Top Med Chem. 2006; 6(13):1335-44.
Review Unravelling the mechanisms underpinning chemokine receptor activation and blockade by small molecules: a fine line between agonism and antagonism? [Biochem Soc Trans. 2007]
Review Unravelling the mechanisms underpinning chemokine receptor activation and blockade by small molecules: a fine line between agonism and antagonism?
Wise E, Pease JE. Biochem Soc Trans. 2007 Aug; 35(Pt 4):755-9.

See reviews... See all...

Cited by 2 PubMed Central articles

Treatment of allergic asthma: modulation of Th2 cells and their responses. [Respir Res. 2011]
Treatment of allergic asthma: modulation of Th2 cells and their responses.
Bosnjak B, Stelzmueller B, Erb KJ, Epstein MM. Respir Res. 2011 Aug 25; 12:114. Epub 2011 Aug 25.
Review Current status and challenges of cytokine pharmacology. [Br J Pharmacol. 2009]
Review Current status and challenges of cytokine pharmacology.
Zídek Z, Anzenbacher P, Kmonícková E. Br J Pharmacol. 2009 Jun; 157(3):342-61. Epub 2009 Apr 3.

Related information

Related Citations
Calculated set of PubMed citations closely related to the selected article(s) retrieved using a word weight algorithm. Related articles are displayed in ranked order from most to least relevant, with the “linked from” citation displayed first.
Compound (MeSH Keyword)
PubChem chemical compound records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.
Substance (MeSH Keyword)
PubChem chemical substance (submitted) records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.
Cited in PMC
Full-text articles in the PubMed Central Database that cite the current articles.

Recent activity

Clear Turn Off Turn On

Bipiperidinyl carboxylic acid amides as potent, selective, and functionally acti...
Bipiperidinyl carboxylic acid amides as potent, selective, and functionally active CCR4 antagonists.
Chem Biol Drug Des. 2007 Sep ;70(3):268-72.

PubMed
Circannual periodicity of migraine?
Circannual periodicity of migraine?
Eur J Neurol. 2007 Sep ;14(9):983-8.

PubMed
Auricular acupuncture treatment for insomnia: a systematic review.
Auricular acupuncture treatment for insomnia: a systematic review.
J Altern Complement Med. 2007 Jul-Aug ;13(6):669-76.

PubMed
The membrane-proximal fusion domain of HIV-1 GP41 reveals sequence-specific and ...
The membrane-proximal fusion domain of HIV-1 GP41 reveals sequence-specific and fine-tuning mechanism of membrane binding.
J Biomol Struct Dyn. 2007 Oct ;25(2):195-205.

PubMed
A novel major groove binding site in B-form DNA for ethidium cation.
A novel major groove binding site in B-form DNA for ethidium cation.
J Biomol Struct Dyn. 2007 Oct ;25(2):119-25.

PubMed

Your browsing activity is empty.

Activity recording is turned off.

Turn recording back on

PubMed

Result Filters

Display Settings:

Send to: