RCSB PDB - 4EJN: Crystal structure of autoinhibited form of AKT1 in complex with N-(4-(5-(3-acetamidophenyl)-2-(2-aminopyridin...
RAC-alpha serine/threonine-protein kinase. A. 446. Homo sapiens. Mutation(s): 3 Gene Names: AKT1, PKB, RAC. EC: 2.7.11.1. ... to identify and optimize small molecule Akt1 inhibitors that act through a mechanism distinct from that observed for kinase ...
RCSB PDB - 2BZK: CRYSTAL STRUCTURE OF THE HUMAN PIM1 IN COMPLEX WITH AMPPNP AND PIMTIDE
PROTO-ONCOGENE SERINE THREONINE PROTEIN KINASE PIM1. B. 313. Homo sapiens. Mutation(s): 1 Gene Names: PIM1. EC: 2.7.1.37 (PDB ...
RCSB PDB - 2YEX: Synthesis and evaluation of triazolones as checkpoint kinase 1 inhibitors
Synthesis and evaluation of triazolones as checkpoint kinase 1 inhibitors ... SERINE/THREONINE-PROTEIN KINASE CHK1. A. 276. Homo sapiens. Mutation(s): 0 Gene Names: CHEK1, CHK1. EC: 2.7.11.1. ... Checkpoint kinase 1 (Chk1, CHEK1) is a Ser/Thr protein kinase that plays a key role in mediating the cellular response to DNA- ... Checkpoint kinase 1 (Chk1, CHEK1) is a Ser/Thr protein kinase that plays a key role in mediating the cellular response to DNA- ...
RCSB PDB - 2XKF: Structure of Nek2 bound to aminopyrazine compound 2
SERINE/THREONINE-PROTEIN KINASE NEK2. A. 279. Homo sapiens. Mutation(s): 0 Gene Names: NEK2, NEK2A, NLK1. EC: 2.7.11.1. ... inactive conformation of the kinase which to the best of our knowledge has not been reported for other types of kinase ... We report herein the first systematic exploration of inhibitors of the mitotic kinase Nek2. Starting from HTS hit aminopyrazine ... We report herein the first systematic exploration of inhibitors of the mitotic kinase Nek2. Starting from HTS hit aminopyrazine ...
RCSB PDB - 4FZD: Crystal structure of MST4-MO25 complex with WSF motif
C-terminal peptide from Serine/threonine-protein kinase MST4. C. 5. Homo sapiens. Mutation(s): 0 Gene Names: STK26, MASK, MST4 ... The kinase domain of MST4 forms a specific homodimer that is required for trans-autophosphorylation. MO25-stimulated activation ... Mammalian STE20-like kinase MST4 regulates multiple cellular aspects such as cell polarity and proliferation. MST4 acts ... MO25 directly interacts with MST4 to promote its kinase activity. Here, we report the crystal structure of MST4 in complex with ...
RCSB PDB - 3P9J: Aurora A kinase domain with phthalazinone pyrazole inhibitor
Aurora A kinase domain with phthalazinone pyrazole inhibitor ... Serine/threonine-protein kinase 6. A. 268. Homo sapiens. ... Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of aurora-a kinase.. Prime, M.E., Courtney, S. ... We report a novel class of Aurora kinase inhibitors based upon a phthalazinone pyrazole scaffold. The development of the ... The inhibition of Aurora kinases in order to arrest mitosis and subsequently inhibit tumor growth via apoptosis of ...
RCSB PDB - 4NZW: Crystal Structure of STK25-MO25 Complex
Serine/threonine-protein kinase 25. B. 295. Homo sapiens. Mutation(s): 1 Gene Names: SOK1, STK25, YSK1. EC: 2.7.11.1. ... The tumor suppressor kinase LKB1 and germinal center kinases (GCKs) are key regulators of various cellular functions. The ... Here, our structural studies of MO25-related kinases reveal that MO25 binds to and activates GCK kinases or pseudokinase ... Structural insights into regulatory mechanisms of MO25-mediated kinase activation.. Hao, Q., Feng, M., Shi, Z., Li, C., Chen, M ...
RCSB PDB - 1PME: STRUCTURE OF PENTA MUTANT HUMAN ERK2 MAP KINASE COMPLEXED WITH A SPECIFIC INHIBITOR OF HUMAN P38 MAP KINASE
STRUCTURE OF PENTA MUTANT HUMAN ERK2 MAP KINASE COMPLEXED WITH A SPECIFIC INHIBITOR OF HUMAN P38 MAP KINASE ... Mitogen-activated protein (MAP) kinases are serine/threonine kinases that mediate intracellular signal transduction pathways. ... Mutagenesis data suggested a single residue difference at threonine 106 between p38 and other MAP kinases is sufficient to ... A single amino acid substitution makes ERK2 susceptible to pyridinyl imidazole inhibitors of p38 MAP kinase.. Fox, T., Coll, J. ...
RCSB PDB - 1UNQ: High resolution crystal structure of the Pleckstrin Homology Domain Of Protein Kinase B/Akt Bound To Ins(1,3,4...
High resolution crystal structure of the Pleckstrin Homology Domain Of Protein Kinase B/Akt Bound To Ins(1,3,4,5)- ... RAC-ALPHA SERINE/THREONINE KINASE. A. 125. Homo sapiens. Mutation(s): 0 Gene Names: AKT1, PKB, RAC. EC: 2.7.1 (PDB Primary Data ... Protein kinase B (PKB/Akt) is a key regulator of cell growth, proliferation and metabolism. It possesses an N-terminal ... High resolution crystal structure of the Pleckstrin Homology Domain Of Protein Kinase B/Akt Bound To Ins(1,3,4,5)- ...
RCSB PDB - 3RPV: CDK2 in complex with inhibitor RC-2-88
Cyclin-dependent kinases (CDKs) are serine/threonine protein kinases that act as key regulatory elements in cell cycle ... Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases.. Schonbrunn, E., Betzi, S., ... The profiling of compound 51 against a panel of 339 kinases revealed high selectivity for CDKs, with preference for CDK2 and ...
RCSB PDB - 3R9H: CDK2 in complex with inhibitor RC-2-142
Cyclin-dependent kinases (CDKs) are serine/threonine protein kinases that act as key regulatory elements in cell cycle ... Cyclin-dependent kinases (CDKs) are serine/threonine protein kinases that act as key regulatory elements in cell cycle ... Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases.. Schonbrunn, E., Betzi, S., ... The profiling of compound 51 against a panel of 339 kinases revealed high selectivity for CDKs, with preference for CDK2 and ...
RCSB PDB - 1UNG: Structural mechanism for the inhibition of CDK5-p25 by roscovitine, aloisine and indirubin.
The cyclin-dependent kinases (CDK) CDK1, CDK2, CDK4, and CDK6 are serine/threonine protein kinases targeted in cancer therapy ... The cyclin-dependent kinases (CDK) CDK1, CDK2, CDK4, and CDK6 are serine/threonine protein kinases targeted in cancer therapy ... CELL DIVISION PROTEIN KINASE 5. A, B. 292. Homo sapiens. Mutation(s): 1 Gene Names: CDK5, CDKN5, PSSALRE. EC: 2.7.11.22 (PDB ... CYCLIN-DEPENDENT KINASE 5 ACTIVATOR 1. C [auth D],. D [auth E]. 208. Homo sapiens. Mutation(s): 0 Gene Names: CDK5R1, CDK5R, ...
RCSB PDB - 3D0E: Crystal structure of human Akt2 in complex with GSK690693
RAC-beta serine/threonine-protein kinase. A, B. 335. Homo sapiens. Mutation(s): 1 Gene Names: AKT2. EC: 2.7.11.1. ... An X-ray cocrystal structure was solved with 3g and the kinase domain of AKT2, confirming that 3g bound in the ATP binding ... Therefore, inhibitors of AKT kinase activity might be useful as monotherapy for the treatment of tumors with activated AKT. ... a novel inhibitor of AKT kinase.. Heerding, D.A., Rhodes, N., Leber, J.D., Clark, T.J., Keenan, R.M., Lafrance, L.V., Li, M., ...
RCSB PDB - 4FK3: B-Raf Kinase V600E Oncogenic Mutant in Complex with PLX3203
B-Raf Kinase V600E Oncogenic Mutant in Complex with PLX3203 ... Serine/threonine-protein kinase B-raf. A, B. 292. Homo sapiens ... is the most frequent oncogenic protein kinase mutation known. Furthermore, inhibitors targeting "active" protein kinases have ... PLX4720 preferentially inhibits the active B-Raf(V600E) kinase compared with a broad spectrum of other kinases, and potent ... Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity.. Tsai, J., T Lee, J., Wang, W. ...
data 5HYX
Probable LRR receptor-like serine/threonine-protein kinase At4g26540 (E.C.2.7.11.1) ; _struct.pdbx_model_details ? _struct.pdbx ... Probable LRR receptor-like serine/threonine-protein kinase At4g26540 69202.875 1 2.7.11.1 V64T, G81E, M82K, D83Q, N104Q UNP ... y SERINE ? C3 H7 N O3 105.093 THR L-peptide linking y THREONINE ? C4 H9 N O3 119.119 TRP L-peptide linking y TRYPTOPHAN ... protein 4897 _refine_hist.pdbx_number_atoms_nucleic_acid 0 # loop_ _refine_ls_restr.pdbx_refine_id _refine_ls_restr.type _ ...
Annotations: 7W7X
Protein tyrosine and serine/threonine kinase (PK_Tyr_Ser-Thr). Protein tyrosine and serine/threonine kinase. Protein ... Serine/threonine-protein kinases, tyrosine-protein kinases, and dual specificity protein kinases (e.g. MEK - phosphorylates ... X: Protein kinase/SAICAR synthase/ATP-grasp (From Homology). H: Protein kinase/SAICAR synthase/ATP-grasp. T: Protein kinase. F ... X: Protein kinase/SAICAR synthase/ATP-grasp (From Homology). H: Protein kinase/SAICAR synthase/ATP-grasp. T: Protein kinase. F ...
RCSB PDB - 6G51: Cryo-EM structure of a late human pre-40S ribosomal subunit - State D
Serine/threonine-protein kinase RIO2. W [auth v]. 552. Homo sapiens. Mutation(s): 0 Gene Names: RIOK2, RIO2. EC: 2.7.11.1. ... Receptor of activated protein C kinase 1. LA [auth g]. 317. Homo sapiens. Mutation(s): 0 Gene Names: RACK1, GNB2L1, HLC7, PIG21 ... 40S ribosomal protein S3. Z [auth D]. 243. Homo sapiens. Mutation(s): 0 Gene Names: RPS3, OK/SW-cl.26. EC: 4.2.99.18. ... 40S ribosomal protein S4, X isoform. F [auth E]. 263. Homo sapiens. Mutation(s): 0 Gene Names: RPS4X, CCG2, RPS4, SCAR. ...
data 3BV2
SERINE/THREONINE-PROTEIN KINASE, KINASE, TRANSFERASE, P38 MAP KINASE, Alternative splicing, ATP-binding, Cytoplasm, Nucleotide- ... Mitogen-activated protein kinase p38 alpha, MAP kinase p38 alpha, Cytokine suppressive anti-inflammatory drug-binding protein, ... CSAID-binding protein, CSBP, MAX-interacting protein 2, MAP kinase MXI2, SAPK2A ; # _entity_poly.entity_id 1 _entity_poly.type ... y SERINE ? C3 H7 N O3 105.093 THR L-peptide linking y THREONINE ? C4 H9 N O3 119.119 TRP L-peptide linking y TRYPTOPHAN ...
data 5L8L
Serine/threonine-protein kinase 15,Serine/threonine-protein kinase 6,Serine/threonine-protein kinase aurora-A ; # loop_ _entity ... y SERINE ? C3 H7 N O3 105.093 SO4 non-polymer . SULFATE ION ? O4 S -2 96.063 THR L-peptide linking y THREONINE ? C4 H9 ... Aurora-A kinase domain in complex with vNAR-D01 (crystal form 1) _struct.pdbx_descriptor Aurora kinase A (E.C.2.7.11.1), New ... Aurora/IPL1-related kinase 1,hARK1,Breast tumor-amplified kinase, ... Aurora kinase A 32964.637 1 2.7.11.1 C290A, C393A ? ? 2 ...
data 1IAN
SERINE/THREONINE-PROTEIN KINASE _struct_keywords.text PROTEIN SER/THR-KINASE, SERINE/THREONINE-PROTEIN KINASE, SERINE- ... THREONINE-PROTEIN KINASE complex # loop_ _struct_asym.id _struct_asym.pdbx_blank_PDB_chainid_flag _struct_asym.pdbx_modified _ ... y SERINE ? C3 H7 N O3 105.093 THR L-peptide linking y THREONINE ? C4 H9 N O3 119.119 TRP L-peptide linking y TRYPTOPHAN ... HUMAN P38 MAP KINASE INHIBITOR COMPLEX _struct.pdbx_descriptor P38 MAP KINASE, 4-[5-(3-IODO-PHENYL)-2-(4-METHANESULFINYL- ...
RCSB PDB - 6BFN: Crystal structure of human IRAK1
Interleukin 1 (IL-1) receptor-associated kinases (IRAKs) are serine/threonine kinases that play critical roles in initiating ... which in turn recruit IRAKs via the death domains in these proteins to form the Myddosome complex, leading to IRAK kinase ... IRAK4 kinase domain. Collectively, these data indicate a two-step kinase activation process in which the IRAK4 kinase domain ... While the IRAK4 kinase domain is capable of homodimerization in the unphosphorylated state, we found that the IRAK1 kinase ...
RCSB PDB - 1Q5K: crystal structure of Glycogen synthase kinase 3 in complexed with inhibitor
crystal structure of Glycogen synthase kinase 3 in complexed with inhibitor ... Glycogen synthase kinase 3 (GSK3) is a serine/threonine kinase that has been implicated in pathological conditions such as ... protects N2A neuroblastoma cells against cell death mediated by inhibition of the phosphatidylinositol 3-kinase/protein kinase ... Glycogen synthase kinase-3 beta. A, B. 414. Homo sapiens. Mutation(s): 0 Gene Names: GSK3B. EC: 2.7.1.37 (PDB Primary Data), ...
RCSB PDB - 3D15: Crystal structure of mouse Aurora A (Asn186-|Gly, Lys240-|Arg, Met302-|Leu) in complex with 1-(3-chloro-phenyl...
serine/threonine kinase 6. A. 272. Mus musculus. Mutation(s): 3 Gene Names: Aurka, Stk6, Aik, Airk, Ark1, Aura, Ayk1, Btak, ... Find proteins for P97477 (Mus musculus). Explore P97477 Go to UniProtKB: P97477 ... Discovery of a potent and selective aurora kinase inhibitor.. Oslob, J.D., Romanowski, M.J., Allen, D.A., Baskaran, S., Bui, M. ... This communication describes the discovery of a novel series of Aurora kinase inhibitors. Key SAR and critical binding elements ...
RCSB PDB - 1BL6: THE COMPLEX STRUCTURE OF THE MAP KINASE P38/SB216995
THE COMPLEX STRUCTURE OF THE MAP KINASE P38/SB216995 ... or other serine/threonine kinases. Although these compounds are ... PROTEIN (MAP KINASE P38). A. 379. Homo sapiens. Mutation(s): 0 Gene Names: MAPK14, CSBP, CSBP1, CSBP2, CSPB1, MXI2, SAPK2A. EC ... The mitogen-activated protein (MAP) kinases are important signaling molecules that participate in diverse cellular events and ... In contrast, the activation of the MAP kinase ERK2 (extracellular-signal-regulated kinase 2) leads to cellular differentiation ...
Annotations: 7NYG
regulation of cyclin-dependent protein kinase activity. *regulation of cyclin-dependent protein serine/threonine kinase ... negative regulation of protein metabolic process. *negative regulation of protein modification by small protein conjugation or ... Protein Family Annotation Pfam Database Homepage. Chains. Accession. Name. Description. Comments. Source. ... Proteins containing the Rel homology domain (RHD) are eukaryotic transcription factors. The RHD is composed of two structural ...
data 2V22
KINASE, CYCLIN, ACTIVE, MITOSIS, INHIBITION, PHOSPHORYLATION, NUCLEOTIDE-BINDING, SERINE/THREONINE-PROTEIN KINASE, CELL CYCLE, ... P33 PROTEIN KINASE, CYCLIN-DEPENDENT KINASE 2 2 CYCLIN-A # loop_ _entity_poly.entity_id _entity_poly.type _entity_poly.nstd_ ... y SERINE ? C3 H7 N O3 105.093 THR L-peptide linking y THREONINE ? C4 H9 N O3 119.119 TRP L-peptide linking y TRYPTOPHAN ... CELL DIVISION PROTEIN KINASE 2 (E.C.2.7.1.37), CYCLIN-A2 _struct.pdbx_model_details ? _struct.pdbx_CASP_flag ? _struct.pdbx_ ...
RCSB PDB - 2WIH: STRUCTURE OF CDK2-CYCLIN A WITH PHA-848125
... showing good potency as inhibitor of CDKs but being poorly selective against a panel of serine-threonine and tyrosine kinases, ... CELL DIVISION PROTEIN KINASE 2. A, C. 309. Homo sapiens. Mutation(s): 0 Gene Names: CDK2, CDKN2. EC: 2.7.1.37 (PDB Primary Data ... The discovery of a novel class of inhibitors of cyclin dependent kinases (CDKs) is described. Starting from compound 1, ... Orally Available Cyclin Dependent Kinase Inhibitor.. Brasca, M.G., Amboldi, N., Ballinari, D., Cameron, A.D., Casale, E., Cervi ...
PDB-101: Molecule of the Month: Insulin Receptor
Regulation of insulin sensitivity by serine/threonine phosphorylation of insulin receptor substrate proteins IRS1 and IRS2. ... The tyrosine kinase portion of the receptor is itself a dynamic protein with many moving parts. The active site binds to ATP ... Two copies of the protein chains come together on the outside of the cell to form the receptor site that binds to insulin. This ... You can use the Protein Feature View for insulin receptor at the RCSB PDB to determine which portion of the receptor is ...
data 1JEG
C-SRC KINASE, PROTEIN-TYROSINE KINASE CYL # loop_ _entity_poly.entity_id _entity_poly.type _entity_poly.nstd_linkage _entity_ ... y SERINE ? C3 H7 N O3 105.093 THR L-peptide linking y THREONINE ? C4 H9 N O3 119.119 TRP L-peptide linking y TRYPTOPHAN ... TYROSINE-PROTEIN KINASE CSK 9198.627 1 2.7.1.112 ? SH3 domain ? 2 polymer man HEMATOPOIETIC CELL PROTEIN-TYROSINE ... protein-peptide complex, tyrosine phosphatase, kinase, TRANSFERASE-HYDROLASE COMPLEX # loop_ _struct_asym.id _struct_asym.pdbx ...
data 2A0B
... y SERINE ? C3 H7 N O3 105.093 THR L-peptide linking y THREONINE ? C4 H9 N O3 119.119 TRP L-peptide linking y TRYPTOPHAN ... Crystallization and Preliminary X-Ray Analysis of a Histidine Kinase Domain of the Anaerobic Sensor Protein Arcb from ... PROTEIN WAS CRYSTALLIZED FROM 12.5% PEGMME 550, 5 MM ZNSO4, 50 MM ACETIC ACID/SODIUM ACETATE BUFFER, PH 4.1 # _diffrn.id 1 _ ... protein 956 _refine_hist.pdbx_number_atoms_nucleic_acid 0 _refine_hist.pdbx_number_atoms_ligand 1 _refine_hist.number_atoms_ ...