3rtp: Difference between revisions
No edit summary |
No edit summary |
||
Line 1: | Line 1: | ||
{{STRUCTURE_3rtp| PDB=3rtp | SCENE= }} | |||
===Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration=== | |||
{{ABSTRACT_PUBMED_21813278}} | |||
==Disease== | |||
[[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. | |||
==Function== | |||
[[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> | |||
==About this Structure== | |||
[[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]. | |||
==Reference== | |||
<references group="xtra"/><references/> | |||
[[Category: Homo sapiens]] | |||
[[Category: Mitogen-activated protein kinase]] | |||
[[Category: Artis, D R.]] | |||
[[Category: Bard, F.]] | |||
[[Category: Bowers, S.]] | |||
[[Category: Chan, W.]] | |||
[[Category: Chen, L.]] | |||
[[Category: Dryer, M.]] | |||
[[Category: Galemmo, R A.]] | |||
[[Category: Goldbach, E.]] | |||
[[Category: Griswold-Prenne, I.]] | |||
[[Category: Hom, R K.]] | |||
[[Category: Konradi, A W.]] | |||
[[Category: Lin, M.]] | |||
[[Category: Lorentzen, C.]] | |||
[[Category: Neitz, R J.]] | |||
[[Category: Pan, H.]] | |||
[[Category: Peterson, B.]] | |||
[[Category: Powell, K.]] | |||
[[Category: Probst, G D.]] | |||
[[Category: Quincy, Q.]] | |||
[[Category: Quinn, K P.]] | |||
[[Category: Ren, Z.]] | |||
[[Category: Ruslim, L.]] | |||
[[Category: Samant, B.]] | |||
[[Category: Sauer, J.]] | |||
[[Category: Sealy, J M.]] | |||
[[Category: Sham, H L.]] | |||
[[Category: Tonn, G.]] | |||
[[Category: Truong, A P.]] | |||
[[Category: Wong, K.]] | |||
[[Category: Wright, S.]] | |||
[[Category: Yao, N.]] | |||
[[Category: Yednock, T A.]] | |||
[[Category: Zhang, H.]] | |||
[[Category: Zmolek, W.]] | |||
[[Category: Jnk inhibitor]] | |||
[[Category: Neurodegeneration]] | |||
[[Category: Pharmacokinetic property]] | |||
[[Category: Transferase-transferase inhibitor complex]] |