[edit] Some Kinases Collections

extracted from [1]

[edit] CMGC Group

http://eneumann.org/exhibit/kinase_demo/item#p38%20(alpha%2Cbeta%2Cgamma%2Cdelta) p38 (alpha,beta,gamma,delta) Kinase http://eneumann.org/exhibit/kinase_demo/item#p38%20(alpha%2Cbeta%2Cgamma%2Cdelta) p38 (alpha,beta,gamma,delta) Cancer Inflammation CMGC Four closely related isoforms (alpha,beta,gamma,delta) involved in apoptosis and stress reponses. Mediate actions of pro-inflammatory cytokines, inhibitors under development to treat inflammation, autoimmunity, diabetes, and cancer (Medline:12725866, 12783612, 12790339). Inhibitors: doramapimod/BIRB-796 (Boehringer Ingelheim, Phase 2-3 for psoriasis, crohn's disease and arthritis), SCIO-469, SCIO-323 (Scios, Phase 1 arthritis), AMG-548 (Amgen), ARQ-101 (ArQule), CDP-11 (Celltech), VX-702 (Vertex, Phase 2 acute coronary syndrome). OMIM Gene Id: 600289, 602898, 602899, 602399.warning.png"Four closely related isoforms (alpha,beta,gamma,delta) involved in apoptosis and stress reponses. Mediate actions of pro-inflammatory cytokines, inhibitors under development to treat inflammation, autoimmunity, diabetes, and cancer (Medline:12725866, 12783612, 12790339). Inhibitors: doramapimod/BIRB-796 (Boehringer Ingelheim, Phase 2-3 for psoriasis, crohn's disease and arthritis), SCIO-469, SCIO-323 (Scios, Phase 1 arthritis), AMG-548 (Amgen), ARQ-101 (ArQule), CDP-11 (Celltech), VX-702 (Vertex, Phase 2 acute coronary syndrome). OMIM Gene Id: 600289, 602898, 602899, 602399." cannot be used as a page name in this wiki. 602399 http://eneumann.org/exhibit/kinase_demo/kinases_vu.html#p38%20(alpha%2Cbeta%2Cgamma%2Cdelta)

http://eneumann.org/exhibit/kinase_demo/item#CDK6 CDK6 Kinase Mutant_Gene http://eneumann.org/exhibit/kinase_demo/item#CDK6 CDK6 cyclin-dependent kinase 6 Cancer CMGC Overexpressed and/or disrupted by translocation in leukemias, lymphomas and other cancers and amplified in gliomas (Medline:9102208) and rodent cancers (Medline:12538879, 11719459). OMIM Gene Id: 603368. 603368 Overexpression Translocation L Dom ALL T MLLT10 7q21-q22 Somatic 7 CDK6 1021 http://eneumann.org/exhibit/kinase_demo/kinases_vu.html#CDK6

http://eneumann.org/exhibit/kinase_demo/item#CDK9 CDK9 Kinase http://eneumann.org/exhibit/kinase_demo/item#CDK9 CDK9 Viral infection Cardiovascular CMGC Transcriptional elongation factor and cofactor for HIV Tat protein, RNAi against CDK9 blocks HIV replication, and inhibitors also block varicella zoster replication. Mediates signals leading to cardiac hypertrophy (Medline:12695656). Inhibitor: Flavopiridol. OMIM Gene Id: 603251.warning.png"Transcriptional elongation factor and cofactor for HIV Tat protein, RNAi against CDK9 blocks HIV replication, and inhibitors also block varicella zoster replication. Mediates signals leading to cardiac hypertrophy (Medline:12695656). Inhibitor: Flavopiridol. OMIM Gene Id: 603251." cannot be used as a page name in this wiki. 603251 Expression http://eneumann.org/exhibit/kinase_demo/kinases_vu.html#CDK9

http://eneumann.org/exhibit/kinase_demo/item#CDK2 CDK2 Kinase http://eneumann.org/exhibit/kinase_demo/item#CDK2 CDK2 Cancer CMGC Cell cycle checkpoint, and part of the Rb pathway disregulated in most tumors (Medline:12888290). Target of several candidate cancer drugs. However, inhibition does not always prevent cancer cell growth (Medline:12676582), possibly due to CDK redundancy. Inhibitors: BMS-265246, BMS-265246-01 (Bristol-Myers Squibb), R-roscovitine (CYC200, CYC202) (Cyclacel), SU9516 (Sugen), L868276. OMIM Gene Id: 116953.warning.png"Cell cycle checkpoint, and part of the Rb pathway disregulated in most tumors (Medline:12888290). Target of several candidate cancer drugs. However, inhibition does not always prevent cancer cell growth (Medline:12676582), possibly due to CDK redundancy. Inhibitors: BMS-265246, BMS-265246-01 (Bristol-Myers Squibb), R-roscovitine (CYC200, CYC202) (Cyclacel), SU9516 (Sugen), L868276. OMIM Gene Id: 116953." cannot be used as a page name in this wiki. 116953 http://eneumann.org/exhibit/kinase_demo/kinases_vu.html#CDK2

http://eneumann.org/exhibit/kinase_demo/item#GSK3alpha%20and%20GSK3beta GSK3alpha and GSK3beta Kinase http://eneumann.org/exhibit/kinase_demo/item#GSK3alpha%20and%20GSK3beta GSK3alpha and GSK3beta Neurodegeneration Diabetes Cardiovascular CNS CMGC [[Notes:=GSK3alpha and GSK3beta have similar functions and are covered together here. GSK3alpha phophorylates tau, the principal component of neurofibrillary tangles in Alzheimer disease [MIM:104300]. GSK3alpha is also required for maximal production of amyloid plaque peptides by g secretase. A GSK3beta promoter SNP effects progression of bipolar disorder [MIM:125480]. The GSK3 inhibitor, lithium, is used to treat bipolar disorder and is seen to block plaque formation. GSK3 generally opposes the action of insulin, and GSK3 hyperactivity is thought to contribute to insulin resistant (type II) diabetes (Medline:15102436, 15078145). GSK3beta also negatively regulates cardiac hypertrophy (Medline:12039794). A tumor suppressor role is indicated by the oncogenic potential of stabilized b-catenin mutants that lack GSK3 phosphorylation sites, but no oncogenic mutants have been reported. Inhibitor: AR-A014418 (Astra Zeneca). OMIM Gene Id: 606784, 605004.]] 605004 SNP Activated http://eneumann.org/exhibit/kinase_demo/kinases_vu.html#GSK3alpha%20and%20GSK3beta

http://eneumann.org/exhibit/kinase_demo/item#HIPK1 HIPK1 Kinase http://eneumann.org/exhibit/kinase_demo/item#HIPK1 HIPK1 Cancer CMGC Expression elevated in many breast cancer cell lines. Null mice are resistant to carcinogens. Binds the p53 tumor suppressor (Medline:12702766). OMIM Gene Id: 608003. 608003 Overexpression http://eneumann.org/exhibit/kinase_demo/kinases_vu.html#HIPK1

http://eneumann.org/exhibit/kinase_demo/item#HIPK2 HIPK2 Kinase http://eneumann.org/exhibit/kinase_demo/item#HIPK2 HIPK2 Cancer CMGC Possible tumor suppressor. Activates p53 in response to UV light, causing growth arrest and apoptosis. Required for cisplatin-induced apoptosis (Medline:14729469). Downregulated in breast and thyroid carcinomas. OMIM Gene Id: 606868. 606868 Loss-of-heterozygosity Expression http://eneumann.org/exhibit/kinase_demo/kinases_vu.html#HIPK2

http://eneumann.org/exhibit/kinase_demo/item#CDC2%20(CDK1) CDC2 (CDK1) Kinase http://eneumann.org/exhibit/kinase_demo/item#CDC2%20(CDK1) CDC2 (CDK1) Cancer CMGC Cell cycle checkpoint. Activated in many cancers including colon, liver and breast (Medline:10091728, 12100577, 11091571). The DT isoform, which lacks a regulatory region, is expressed in breast cancer. Inhibition in cancer cells may drive cells into apoptosis (Medline:12150824). May also drive cell migration (Medline:12771130). Inhibitors: BMS-265246, BMS-265246-01 (Bristol-Myers Squibb). OMIM Gene Id: 116940.warning.png"Cell cycle checkpoint. Activated in many cancers including colon, liver and breast (Medline:10091728, 12100577, 11091571). The DT isoform, which lacks a regulatory region, is expressed in breast cancer. Inhibition in cancer cells may drive cells into apoptosis (Medline:12150824). May also drive cell migration (Medline:12771130). Inhibitors: BMS-265246, BMS-265246-01 (Bristol-Myers Squibb). OMIM Gene Id: 116940." cannot be used as a page name in this wiki. 116940 Activated Splice-Change http://eneumann.org/exhibit/kinase_demo/kinases_vu.html#CDC2%20(CDK1)

http://eneumann.org/exhibit/kinase_demo/item#Erk5%20(BMK1) Erk5 (BMK1) Kinase http://eneumann.org/exhibit/kinase_demo/item#Erk5%20(BMK1) Erk5 (BMK1) Cancer Cardiovascular CMGC Mouse knockout shows a role in development and integrity of blood vessels. May block apoptosis in endothelial cells (Medline:14670836). Required for transduction of EGF growth signal (Medline: 9790194), constitutively activated in ErbB2-overexpressing breast cancer (Medline: 11739740), and downstream of activated Mek5 in metastatic prostate cancer (Medline: 12618764). Inhibitor: PD98059. OMIM Gene Id: 602521.warning.png"Mouse knockout shows a role in development and integrity of blood vessels. May block apoptosis in endothelial cells (Medline:14670836). Required for transduction of EGF growth signal (Medline: 9790194), constitutively activated in ErbB2-overexpressing breast cancer (Medline: 11739740), and downstream of activated Mek5 in metastatic prostate cancer (Medline: 12618764). Inhibitor: PD98059. OMIM Gene Id: 602521." cannot be used as a page name in this wiki. 602521 Expression http://eneumann.org/exhibit/kinase_demo/kinases_vu.html#Erk5%20(BMK1)

http://eneumann.org/exhibit/kinase_demo/item#JNK3 JNK3 Kinase http://eneumann.org/exhibit/kinase_demo/item#JNK3 JNK3 Cancer CNS CMGC Brain-selective Jnk isoform. Pro-apoptotic gene and potential tumor suppressor. Expression lost in brain tumors (Medline:11322657). May function in neuronal cell death from injury and neurodegeneration, for which inhibitors are being developed (Medline:15501728, 14657393, 14704277). OMIM Gene Id: 602897.warning.png"Brain-selective Jnk isoform. Pro-apoptotic gene and potential tumor suppressor. Expression lost in brain tumors (Medline:11322657). May function in neuronal cell death from injury and neurodegeneration, for which inhibitors are being developed (Medline:15501728, 14657393, 14704277). OMIM Gene Id: 602897." cannot be used as a page name in this wiki. 602897 Expression http://eneumann.org/exhibit/kinase_demo/kinases_vu.html#JNK3

http://eneumann.org/exhibit/kinase_demo/item#JNK1 JNK1 Kinase http://eneumann.org/exhibit/kinase_demo/item#JNK1 JNK1 Cancer Diabetes Inflammation CMGC Activity increased in obesity. Inhibition or mouse knockout increases insulin sensitivity (Medline:12447443). Part of NFκB pathway involved in inflammation and cancer, and signals downstream of Ras, though possibly as an apoptotic negative regulator of growth (Medline:12734425). OMIM Gene Id: 601158.warning.png"Activity increased in obesity. Inhibition or mouse knockout increases insulin sensitivity (Medline:12447443). Part of NFκB pathway involved in inflammation and cancer, and signals downstream of Ras, though possibly as an apoptotic negative regulator of growth (Medline:12734425). OMIM Gene Id: 601158." cannot be used as a page name in this wiki. 601158 http://eneumann.org/exhibit/kinase_demo/kinases_vu.html#JNK1

http://eneumann.org/exhibit/kinase_demo/item#Dyrk1A Dyrk1A Kinase http://eneumann.org/exhibit/kinase_demo/item#Dyrk1A Dyrk1A Cognition CMGC Candidate gene for some aspects of Down's Syndrome: located in DS critical region, and overexpression in mice gives rise to similar neurological abnormalities (Medline: 15198122). OMIM Gene Id: 600855. 600855 http://eneumann.org/exhibit/kinase_demo/kinases_vu.html#Dyrk1A

http://eneumann.org/exhibit/kinase_demo/item#CDK4 CDK4 Kinase Mutant_Gene http://eneumann.org/exhibit/kinase_demo/item#CDK4 CDK4 cyclin-dependent kinase 4 Cancer CMGC Point mutations found in somatic and familial melanoma. Amplified in sarcomas (Medline:9703873, 9935200), glioma (Medline: 14756442) and lymphoma (Medline: 12203778). Amplified, methylated or deleted in head and neck squamous cell carcinoma (Medline: 14586645). Overexpression drives epithelial tumors in mice (Medline: 14647432). Disruption makes mice resistant to cancer (Medline: 12435633). Inhibitor: PD332991 (Onyx). OMIM Gene Id: 123829.warning.png"Point mutations found in somatic and familial melanoma. Amplified in sarcomas (Medline:9703873, 9935200), glioma (Medline: 14756442) and lymphoma (Medline: 12203778). Amplified, methylated or deleted in head and neck squamous cell carcinoma (Medline: 14586645). Overexpression drives epithelial tumors in mice (Medline: 14647432). Disruption makes mice resistant to cancer (Medline: 12435633). Inhibitor: PD332991 (Onyx). OMIM Gene Id: 123829." cannot be used as a page name in this wiki. 123829 Activated Gain-of-function Mutation Amplified Methylation E Dom Mis 12q14 melanoma Germline Familial malignant melanoma 12 CDK4 1019 http://eneumann.org/exhibit/kinase_demo/kinases_vu.html#CDK4