3rtp

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'''Unreleased structure'''
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{{STRUCTURE_3rtp| PDB=3rtp | SCENE= }}
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===Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration===
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{{ABSTRACT_PUBMED_21813278}}
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The entry 3rtp is ON HOLD until sometime in the future
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==Disease==
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[[http://www.uniprot.org/uniprot/MK10_HUMAN MK10_HUMAN]] Defects in MAPK10 are a cause of epileptic encephalopathy Lennox-Gastaut type (EELG) [MIM:[http://omim.org/entry/606369 606369]]. Epileptic encephalopathies of the Lennox-Gastaut group are childhood epileptic disorders characterized by severe psychomotor delay and seizures. Note=A chromosomal aberration involving MAPK10 has been found in a single patient. Translocation t(Y;4)(q11.2;q21) which causes MAPK10 truncation.
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Authors: Bowers, S., Truong, A.P., Neitz, R.J., Hom, R.K., Sealy, J.M., Probst, G.D., Quincy, Q., Peterson, B., Chan, W., Galemmo Jr., R.A., Konradi, A.W., Sham, H.L., Pan, H., Lin, M., Yao, N., Artis, D.R., Zhang, H., Chen, L., Dryer, M., Samant, B., Zmolek, W., Wong, K., Lorentzen, C., Goldbach, E., Tonn, G., Quinn, K.P., Sauer, J., Wright, S., Powell, K., Ruslim, L., Ren, Z., Bard, F., Yednock, T.A., Griswold-Prenne, I.
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==Function==
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[[http://www.uniprot.org/uniprot/MK10_HUMAN MK10_HUMAN]] Serine/threonine-protein kinase involved in various processes such as neuronal proliferation, differentiation, migration and programmed cell death. Extracellular stimuli such as proinflammatory cytokines or physical stress stimulate the stress-activated protein kinase/c-Jun N-terminal kinase (SAP/JNK) signaling pathway. In this cascade, two dual specificity kinases MAP2K4/MKK4 and MAP2K7/MKK7 phosphorylate and activate MAPK10/JNK3. In turn, MAPK10/JNK3 phosphorylates a number of transcription factors, primarily components of AP-1 such as JUN and ATF2 and thus regulates AP-1 transcriptional activity. Plays regulatory roles in the signaling pathways during neuronal apoptosis. Phosphorylates the neuronal microtubule regulator STMN2. Acts in the regulation of the beta-amyloid precursor protein/APP signaling during neuronal differentiation by phosphorylating APP. Participates also in neurite growth in spiral ganglion neurons.<ref>PMID:11718727</ref>
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Description: Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration
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==About this Structure==
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[[3rtp]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RTP OCA].
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==Reference==
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<references group="xtra"/><references/>
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[[Category: Homo sapiens]]
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[[Category: Mitogen-activated protein kinase]]
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[[Category: Artis, D R.]]
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[[Category: Bard, F.]]
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[[Category: Bowers, S.]]
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[[Category: Chan, W.]]
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[[Category: Chen, L.]]
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[[Category: Dryer, M.]]
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[[Category: Galemmo, R A.]]
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[[Category: Goldbach, E.]]
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[[Category: Griswold-Prenne, I.]]
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[[Category: Hom, R K.]]
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[[Category: Konradi, A W.]]
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[[Category: Lin, M.]]
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[[Category: Lorentzen, C.]]
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[[Category: Neitz, R J.]]
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[[Category: Pan, H.]]
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[[Category: Peterson, B.]]
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[[Category: Powell, K.]]
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[[Category: Probst, G D.]]
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[[Category: Quincy, Q.]]
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[[Category: Quinn, K P.]]
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[[Category: Ren, Z.]]
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[[Category: Ruslim, L.]]
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[[Category: Samant, B.]]
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[[Category: Sauer, J.]]
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[[Category: Sealy, J M.]]
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[[Category: Sham, H L.]]
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[[Category: Tonn, G.]]
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[[Category: Truong, A P.]]
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[[Category: Wong, K.]]
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[[Category: Wright, S.]]
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[[Category: Yao, N.]]
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[[Category: Yednock, T A.]]
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[[Category: Zhang, H.]]
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[[Category: Zmolek, W.]]
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[[Category: Jnk inhibitor]]
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[[Category: Neurodegeneration]]
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[[Category: Pharmacokinetic property]]
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[[Category: Transferase-transferase inhibitor complex]]

Revision as of 07:40, 8 May 2013

Template:STRUCTURE 3rtp

Contents

Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration

Template:ABSTRACT PUBMED 21813278

Disease

[MK10_HUMAN] Defects in MAPK10 are a cause of epileptic encephalopathy Lennox-Gastaut type (EELG) [MIM:606369]. Epileptic encephalopathies of the Lennox-Gastaut group are childhood epileptic disorders characterized by severe psychomotor delay and seizures. Note=A chromosomal aberration involving MAPK10 has been found in a single patient. Translocation t(Y;4)(q11.2;q21) which causes MAPK10 truncation.

Function

[MK10_HUMAN] Serine/threonine-protein kinase involved in various processes such as neuronal proliferation, differentiation, migration and programmed cell death. Extracellular stimuli such as proinflammatory cytokines or physical stress stimulate the stress-activated protein kinase/c-Jun N-terminal kinase (SAP/JNK) signaling pathway. In this cascade, two dual specificity kinases MAP2K4/MKK4 and MAP2K7/MKK7 phosphorylate and activate MAPK10/JNK3. In turn, MAPK10/JNK3 phosphorylates a number of transcription factors, primarily components of AP-1 such as JUN and ATF2 and thus regulates AP-1 transcriptional activity. Plays regulatory roles in the signaling pathways during neuronal apoptosis. Phosphorylates the neuronal microtubule regulator STMN2. Acts in the regulation of the beta-amyloid precursor protein/APP signaling during neuronal differentiation by phosphorylating APP. Participates also in neurite growth in spiral ganglion neurons.[1]

About this Structure

3rtp is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

  1. ↑ Neidhart S, Antonsson B, Gillieron C, Vilbois F, Grenningloh G, Arkinstall S. c-Jun N-terminal kinase-3 (JNK3)/stress-activated protein kinase-beta (SAPKbeta) binds and phosphorylates the neuronal microtubule regulator SCG10. FEBS Lett. 2001 Nov 16;508(2):259-64. PMID:11718727

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