2gmx

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[[Image:2gmx.gif|left|200px]]
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{{Seed}}
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[[Image:2gmx.png|left|200px]]
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{{STRUCTURE_2gmx| PDB=2gmx | SCENE= }}
{{STRUCTURE_2gmx| PDB=2gmx | SCENE= }}
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'''Selective Aminopyridine-Based C-Jun N-terminal Kinase inhibitors with cellular activity'''
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===Selective Aminopyridine-Based C-Jun N-terminal Kinase inhibitors with cellular activity===
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==Overview==
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The c-Jun N-terminal kinases (JNK-1, -2, and -3) are members of the mitogen activated protein (MAP) kinase family of enzymes. They are activated in response to certain cytokines, as well as by cellular stresses including chemotoxins, peroxides, and irradiation. They have been implicated in the pathology of a variety of different diseases with an inflammatory component including asthma, stroke, Alzheimer's disease, and type 2 diabetes mellitus. In this work, high-throughput screening identified a JNK inhibitor with an excellent kinase selectivity profile. Using X-ray crystallography and biochemical screening to guide our lead optimization, we prepared compounds with inhibitory potencies in the low-double-digit nanomolar range, activity in whole cells, and pharmacokinetics suitable for in vivo use. The new compounds were over 1,000-fold selective for JNK-1 and -2 over other MAP kinases including ERK2, p38alpha, and p38delta and showed little inhibitory activity against a panel of 74 kinases.
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The line below this paragraph, {{ABSTRACT_PUBMED_16759099}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 16759099 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16759099}}
==About this Structure==
==About this Structure==
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==Reference==
==Reference==
Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity., Szczepankiewicz BG, Kosogof C, Nelson LT, Liu G, Liu B, Zhao H, Serby MD, Xin Z, Liu M, Gum RJ, Haasch DL, Wang S, Clampit JE, Johnson EF, Lubben TH, Stashko MA, Olejniczak ET, Sun C, Dorwin SA, Haskins K, Abad-Zapatero C, Fry EH, Hutchins CW, Sham HL, Rondinone CM, Trevillyan JM, J Med Chem. 2006 Jun 15;49(12):3563-80. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/16759099 16759099]
Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity., Szczepankiewicz BG, Kosogof C, Nelson LT, Liu G, Liu B, Zhao H, Serby MD, Xin Z, Liu M, Gum RJ, Haasch DL, Wang S, Clampit JE, Johnson EF, Lubben TH, Stashko MA, Olejniczak ET, Sun C, Dorwin SA, Haskins K, Abad-Zapatero C, Fry EH, Hutchins CW, Sham HL, Rondinone CM, Trevillyan JM, J Med Chem. 2006 Jun 15;49(12):3563-80. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/16759099 16759099]
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Synthesis and SAR of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as novel, selective c-Jun N-terminal kinase inhibitors., Liu M, Xin Z, Clampit JE, Wang S, Gum RJ, Haasch DL, Trevillyan JM, Abad-Zapatero C, Fry EH, Sham HL, Liu G, Bioorg Med Chem Lett. 2006 May 15;16(10):2590-4. Epub 2006 Mar 9. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/16527482 16527482]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Mitogen-activated protein kinase]]
[[Category: Mitogen-activated protein kinase]]
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[[Category: Jnk1]]
[[Category: Jnk1]]
[[Category: Protein kinase jnk1 inhibitor]]
[[Category: Protein kinase jnk1 inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 05:17:23 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 09:01:12 2008''

Revision as of 06:01, 29 July 2008

Image:2gmx.png

Template:STRUCTURE 2gmx

Selective Aminopyridine-Based C-Jun N-terminal Kinase inhibitors with cellular activity

Template:ABSTRACT PUBMED 16759099

About this Structure

2GMX is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity., Szczepankiewicz BG, Kosogof C, Nelson LT, Liu G, Liu B, Zhao H, Serby MD, Xin Z, Liu M, Gum RJ, Haasch DL, Wang S, Clampit JE, Johnson EF, Lubben TH, Stashko MA, Olejniczak ET, Sun C, Dorwin SA, Haskins K, Abad-Zapatero C, Fry EH, Hutchins CW, Sham HL, Rondinone CM, Trevillyan JM, J Med Chem. 2006 Jun 15;49(12):3563-80. PMID:16759099

Synthesis and SAR of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as novel, selective c-Jun N-terminal kinase inhibitors., Liu M, Xin Z, Clampit JE, Wang S, Gum RJ, Haasch DL, Trevillyan JM, Abad-Zapatero C, Fry EH, Sham HL, Liu G, Bioorg Med Chem Lett. 2006 May 15;16(10):2590-4. Epub 2006 Mar 9. PMID:16527482

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