Proteins > Serine/threonine-protein kinase ULK2
Page last updated: 2024-08-07 21:18:27
Serine/threonine-protein kinase ULK2
A serine/threonine-protein kinase ULK2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q8IYT8]
Synonyms
EC 2.7.11.1;
Unc-51-like kinase 2
Research
Bioassay Publications (9)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (11.11) | 29.6817 |
| 2010's | 6 (66.67) | 24.3611 |
| 2020's | 2 (22.22) | 2.80 |
Compounds (72)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| staurosporine | Homo sapiens (human) | IC50 | 0.0032 | 2 | 2 |
| bx795 | Homo sapiens (human) | IC50 | 0.3100 | 1 | 1 |
| mrt67307 | Homo sapiens (human) | IC50 | 0.0897 | 3 | 3 |
| sbi-0206965 | Homo sapiens (human) | IC50 | 1.6918 | 5 | 5 |
Drugs with Activation Measurements
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
UNC-51-like Kinase 1: From an Autophagic Initiator to Multifunctional Drug Target.Journal of medicinal chemistry, , Aug-09, Volume: 61, Issue:15, 2018
Discovery and structure of a new inhibitor scaffold of the autophagy initiating kinase ULK1.Bioorganic & medicinal chemistry, , Sep-01, Volume: 23, Issue:17, 2015
Design, Synthesis, and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer.Journal of medicinal chemistry, , 12-10, Volume: 63, Issue:23, 2020
Discovery of 5-bromo-4-phenoxy-N-phenylpyrimidin-2-amine derivatives as novel ULK1 inhibitors that block autophagy and induce apoptosis in non-small cell lung cancer.European journal of medicinal chemistry, , Dec-15, Volume: 208, 2020
UNC-51-like Kinase 1: From an Autophagic Initiator to Multifunctional Drug Target.Journal of medicinal chemistry, , Aug-09, Volume: 61, Issue:15, 2018
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|
| protein serine/threonine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:bf, MetaCyc:PROTEIN-KINASE-RXN, PMID:2956925] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| protein serine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989] |
Located In
This protein is located in 2 target(s):
| Target | Category | Definition |
|---|
| cytoplasmic vesicle membrane | cellular component | The lipid bilayer surrounding a cytoplasmic vesicle. [GOC:mah] |
| phagophore assembly site membrane | cellular component | A cellular membrane associated with the phagophore assembly site. [GOC:mah, GOC:rph, PMID:16874040, PMID:17382324] |
Active In
This protein is active in 5 target(s):
| Target | Category | Definition |
|---|
| phagophore assembly site membrane | cellular component | A cellular membrane associated with the phagophore assembly site. [GOC:mah, GOC:rph, PMID:16874040, PMID:17382324] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| phagophore assembly site | cellular component | Punctate structures proximal to the endoplasmic reticulum which are the sites where the Atg machinery assembles upon autophagy induction. [GOC:elh, PMID:11689437, PMID:12048214, PMID:12554655] |
| autophagosome | cellular component | A double-membrane-bounded compartment that engulfs endogenous cellular material as well as invading microorganisms to target them to the lytic vacuole/lysosome for degradation as part of macroautophagy. [GOC:autophagy, ISBN:0198547684, PMID:11099404] |
Involved In
This protein is involved in 13 target(s):
| Target | Category | Definition |
|---|
| autophagy | biological process | The cellular catabolic process in which cells digest cellular materials, such as organelles and other macromolecular constituents, or non-self materials such as intracellular pathogens. Autophagy serves to provide essential nutrients under conditions of cellular stress; or can remodel intracellular structures during cell differentiation. [GOC:autophagy, ISBN:0198547684, PMID:11099404, PMID:29455577, PMID:9412464] |
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
| response to starvation | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a starvation stimulus, deprivation of nourishment. [GOC:go_curators] |
| protein autophosphorylation | biological process | The phosphorylation by a protein of one or more of its own amino acid residues (cis-autophosphorylation), or residues on an identical protein (trans-autophosphorylation). [ISBN:0198506732] |
| collateral sprouting | biological process | The process in which outgrowths develop from the shafts of existing axons. [GOC:dgh, GOC:dph, GOC:jid, GOC:lm] |
| autophagy of mitochondrion | biological process | The autophagic process in which mitochondria are delivered to a type of vacuole and degraded in response to changing cellular conditions. [GOC:autophagy, PMID:15798367, PMID:19289147, PMID:23065344] |
| axon extension | biological process | Long distance growth of a single axon process involved in cellular development. [GOC:BHF, GOC:dgh, GOC:dph, GOC:jid, GOC:lm, GOC:rl] |
| reticulophagy | biological process | The selective autohagy process in which parts of the endoplasmic reticulum are loaded into autophagosomes, delivered to the vacuole, and degraded in response to changing cellular conditions. [GOC:autophagy, GOC:dph, PMID:22481944, PMID:24060720, PMID:26040717] |
| peptidyl-serine phosphorylation | biological process | The phosphorylation of peptidyl-serine to form peptidyl-O-phospho-L-serine. [RESID:AA0037] |
| positive regulation of autophagy | biological process | Any process that activates, maintains or increases the rate of autophagy. Autophagy is the process in which cells digest parts of their own cytoplasm. [GOC:dph, GOC:tb] |
| piecemeal microautophagy of the nucleus | biological process | Degradation of a cell nucleus by microautophagy. [GOC:autophagy, GOC:jp, PMID:18701704] |
| negative regulation of collateral sprouting | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of collateral sprouting. [GOC:dgh, GOC:dph, GOC:jid, GOC:lm] |
| autophagosome assembly | biological process | The formation of a double membrane-bounded structure, the autophagosome, that occurs when a specialized membrane sac, called the isolation membrane, starts to enclose a portion of the cytoplasm. [GOC:autophagy, PMID:9412464] |