Target type: biologicalprocess
Any process that activates or increases the frequency, rate or extent of tau-protein kinase activity. [GO_REF:0000059, GOC:sjp, GOC:TermGenie, PMID:15897157, PMID:22986780]
Positive regulation of tau-protein kinase activity is a complex biological process that involves a series of molecular events leading to the activation of tau-protein kinases. These kinases play a crucial role in regulating the phosphorylation of tau protein, a microtubule-associated protein that plays a vital role in neuronal function. Dysregulation of tau phosphorylation is implicated in several neurodegenerative diseases, including Alzheimer's disease.
**Key steps involved in positive regulation of tau-protein kinase activity:**
1. **Binding of Kinase Activator:** Certain molecules, known as kinase activators, bind to the kinase and induce conformational changes, leading to activation. These activators can include small molecules, proteins, or even post-translational modifications like phosphorylation.
2. **Releasing of Inhibitory Domains:** Some kinases have inhibitory domains that prevent their activity. Kinase activators can bind to these domains and release them, allowing the kinase to become active.
3. **Post-Translational Modifications:** Post-translational modifications, such as phosphorylation or acetylation, can also regulate kinase activity. These modifications can alter the conformation or binding affinity of the kinase, leading to increased activity.
4. **Scaffold Proteins:** Scaffold proteins can bring together kinase and its substrate, facilitating the phosphorylation process. This brings the kinase and its substrate into close proximity, increasing the probability of phosphorylation.
5. **Signaling Pathways:** Kinase activity is often regulated by upstream signaling pathways. These pathways can activate kinases through a cascade of phosphorylation events.
6. **Changes in Cellular Environment:** Changes in the cellular environment, such as stress or nutrient availability, can also affect kinase activity. These changes can trigger signaling pathways that ultimately lead to kinase activation.
**Overall, the positive regulation of tau-protein kinase activity is a multi-faceted process involving a diverse range of molecular mechanisms. This regulation is critical for maintaining neuronal function and preventing neurodegenerative diseases. Further research is needed to fully understand the complexities of this process and to develop therapeutic interventions for diseases related to tau-protein kinase dysregulation.**'
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Protein | Definition | Taxonomy |
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Heat shock protein HSP 90-alpha | A heat shock protein HSP 90-alpha that is encoded in the genome of human. [PRO:DAN] | Homo sapiens (human) |
Compound | Definition | Classes | Roles |
---|---|---|---|
n(6),n(6)-dimethyladenine | N(6),N(6)-dimethyladenine : A tertiary amine that is adenine substituted at N-6 by geminal methyl groups. | tertiary amine | |
ns 1619 | NS 1619 : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which the hydrogens at positions 1 and 5 are replaced are replaced by 2-hydroxy-5-(trifluoromethyl)phenyl and trifluoromethyl groups, respectively. It is an opener/activator of the large-conductance calcium-activated potassium channel (Bkca). NS 1619: structure given in first source | (trifluoromethyl)benzenes; benzimidazoles; phenols | potassium channel opener |
vorinostat | vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL). Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME. | dicarboxylic acid diamide; hydroxamic acid | antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor |
adenosine diphosphate | Adenosine Diphosphate: Adenosine 5'-(trihydrogen diphosphate). An adenine nucleotide containing two phosphate groups esterified to the sugar moiety at the 5'-position. | adenosine 5'-phosphate; purine ribonucleoside 5'-diphosphate | fundamental metabolite; human metabolite |
2-aminopyrimidine | aminopyrimidine : A member of the class of pyrimidines that is pyrimidine substituted by at least one amino group and its derivatives. pyrimidin-2-amine : An aminopyrimidine carrying an amino group at position 2. | aminopyrimidine | |
2-chloroadenosine | 5-chloroformycin A: structure given in first source | purine nucleoside | |
indazoles | Indazoles: A group of heterocyclic aromatic organic compounds consisting of the fusion of BENZENE and PYRAZOLES. | indazole | |
ethamivan | etamivan : Phenol substituted at C-2 and C-4 by a methoxy group and an N,N-diethylaminocarbonyl group respectively. A respiratory stimulant drug related to nikethamide, it has now fallen largely into disuse. ethamivan: minor descriptor (65-72); major descriptor (73-86); on-line search BENZAMIDES (66-86); INDEX MEDICUS search BENZAMIDES (65-72); ETHAMIVAN (73-86) | methoxybenzenes; phenols | |
9-fluorenone | fluoren-9-one : The simplest member of the class fluoren-9-ones that is 9H-fluorene bearing an oxo substituent at position 9. | fluoren-9-ones | fungal xenobiotic metabolite |
alpha-aminopyridine | alpha-aminopyridine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #485 aminopyridine : Compounds containing a pyridine skeleton substituted by one or more amine groups. | ||
silybin | silibinin : A flavonolignan isolated from milk thistle, Silybum marianum, that has been shown to exhibit antioxidant and antineoplastic activities. | aromatic ether; benzodioxine; flavonolignan; polyphenol; secondary alpha-hydroxy ketone | antineoplastic agent; antioxidant; hepatoprotective agent; plant metabolite |
adenosine | quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit | adenosines; purines D-ribonucleoside | analgesic; anti-arrhythmia drug; fundamental metabolite; human metabolite; vasodilator agent |
4-aminopyrimidine | aminopyrimidine | ||
2-acetylamino-3-chloro-1,4-naphthoquinone | 2-acetylamino-3-chloro-1,4-naphthoquinone: structure in first source | ||
2-aminopyrazine | pyrazines | ||
catalposide | |||
adenosine-5'-carboxylic acid | purine nucleoside | ||
hydroxybenzindazole | hydroxybenzindazole: structure | ||
adenosine 5'-carboxamide | adenosine 5'-carboxamide: structure | ||
5-benzyloxytryptophan | |||
isopentaquine | |||
5'-n-methylcarboxamideadenosine | 5'-N-methylcarboxamideadenosine: RN given refers to (beta-D)-isomer | ||
n-methyladenosine | N-methyladenosine: is a inhibitor of cell differentiation N(6)-methyladenosine : A methyladenosine compound with one methyl group attached to N(6) of the adenine nucleobase. | methyladenosine | |
deguelin | deguelin : A rotenone that is 13,13a-dihydro-3H-chromeno[3,4-b]pyrano[2,3-h]chromen-7(7aH)-one substituted by methoxy groups at positions 9 and 10, and by two methyl groups at position 3 (the 7aS,13aS-stereoisomer). It exists in abundant quantities in the bark, roots, and leaves of the Leguminosae family of plants and reported to exert anti-tumour effects in various cancers. deguelin: a natural product from Mundulea sericea; RN refers to (7aS-cis)-isomer; structure given in first source | aromatic ether; diether; organic heteropentacyclic compound; rotenones | angiogenesis inhibitor; anti-inflammatory agent; antineoplastic agent; antiviral agent; apoptosis inducer; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; mitochondrial NADH:ubiquinone reductase inhibitor; plant metabolite |
2-(4-morpholinyl)-4h-1-benzopyran-4-one | 2-(4-morpholinyl)-4H-1-benzopyran-4-one: an aminochromone; exhibits both antiproliferative and antichemotactic activity in vitro | ||
adenosine 5'-phosphoramidate | adenosine 5'-phosphoramidate : The phosphoramadite analogue of AMP. | organic phosphoramidate | Mycoplasma genitalium metabolite |
adenosine-5'-(n-ethylcarboxamide) | Adenosine-5'-(N-ethylcarboxamide): A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity. N-ethyl-5'-carboxamidoadenosine : A derivative of adenosine in which the 5'-hydroxymethyl group is replaced by an N-ethylcarboxamido group. | adenosines; monocarboxylic acid amide | adenosine A1 receptor agonist; adenosine A2A receptor agonist; antineoplastic agent; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; vasodilator agent |
8-(2-chloro-3,4,5-trimethoxybenzyl)-2-fluoro-9-pent-4-yn-1-yl-9H-purin-6-amine | 8-(2-chloro-3,4,5-trimethoxybenzyl)-2-fluoro-9-pent-4-yn-1-yl-9H-purin-6-amine : A member of the class of 6-aminopurines that is 2-fluoroadenine carrying additional 2-chloro-3,4,5-trimethoxybenzyl and pent-4-yn-1-yl substituents at positions 8 and 9 respectively. | 6-aminopurines; acetylenic compound; methoxybenzenes; monochlorobenzenes; organofluorine compound | antineoplastic agent; Hsp90 inhibitor |
cct018159 | CCT-018159 : A member of the class of pyrazoles that is 1H-pyrazole carrying 1,4-benzodioxane-6-yl and 5-ethyl-2,4-dihydroxyphenyl substituents at positions 4 and 5 respectively. CCT018159: structure in first source | benzodioxine; pyrazoles; resorcinols | antineoplastic agent; apoptosis inducer; Hsp90 inhibitor |
adenosine-5'-(N-propyl)carboxamide | adenosine-5'-(N-propyl)carboxamide : A monocarboxylic acid amide that is the propyl amide of adenosine 5'-carboxylic acid. | adenosines; monocarboxylic acid amide | |
ver-49009 | 5-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)pyrazole-3-carboxamide : An aromatic amide obtained by formal condensation of the carboxy group of 5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)pyrazole-3-carboxylic acid with the amino group of ethylamine. VER-49009: inhibits heat shock protein 90 molecular chaperone; structure in first source | aromatic amide; monochlorobenzenes; monomethoxybenzene; pyrazoles; resorcinols | Hsp90 inhibitor |
geldanamycin | 1,4-benzoquinones; ansamycin; carbamate ester; organic heterobicyclic compound | antimicrobial agent; antineoplastic agent; antiviral agent; cysteine protease inhibitor; Hsp90 inhibitor | |
17-(dimethylaminoethylamino)-17-demethoxygeldanamycin | 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin: structure in first source alvespimycin : A 19-membered macrocyle that is geldanamycin in which the methoxy group attached to the benzoquinone moiety has been replaced by a 2-(N,N-dimethylamino)ethylamino group. | 1,4-benzoquinones; ansamycin; carbamate ester; secondary amino compound; tertiary amino compound | Hsp90 inhibitor |
derrubone | derrubone: an inhibitor of the Hsp90 protein folding machinery from Derris robusta; structure in first source | isoflavanones | |
monorden | monorden: inhibits HSP90 Heat-Shock Proteins, DNA topoisomerase VI and human Topoisomerase II | cyclic ketone; enone; epoxide; macrolide antibiotic; monochlorobenzenes; phenols | antifungal agent; metabolite; tyrosine kinase inhibitor |
tanespimycin | CP 127374: analog of herbimycin A | 1,4-benzoquinones; ansamycin; carbamate ester; organic heterobicyclic compound; secondary amino compound | antineoplastic agent; apoptosis inducer; Hsp90 inhibitor |
1-aminoadenosine | 1-aminoadenosine: structure | ||
9h-purine-9-propanamine, 6-amino-8-((6-iodo-1,3-benzodioxol-5-yl)thio)-n-(1-methylethyl)- | 9H-purine-9-propanamine, 6-amino-8-((6-iodo-1,3-benzodioxol-5-yl)thio)-N-(1-methylethyl)-: an epichaperome (purine-scaffold) inhibitor; structure in first source | ||
reblastatin | reblastatin: structure in first source | ||
5'-amino-5'-deoxyadenosine | |||
gambogic acid | gambogic acid: RN given refers to (1R-(1alpha,1(Z),3abeta,5alpha,11beta,14aS*))-isomer | pyranoxanthones | metabolite |
ipi 493 | 17-aminogeldanamycin: structure in first source | ||
n-cyclopropyl adenosine-5'-carboxamide | |||
ec 144 | EC 144: structure in first source | ||
snx-7081 | SNX-7081: Anti-Inflammatory Agent; structure in first source | ||
6-o-coumaroylcatalpol | cinnamate ester | ||
at 13387 | (2,4-dihydroxy-5-isopropylphenyl)-(5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl)methanone: structure in first source onalespib : A member of the class of isoindoles that is isoindole in which the amino group has been acylated by a 2,4-dihydroxy-5-isopropylbenzoyl group and in which position 5 of the isoidole moiety has been substituted by a (4-methylpiperazin-1-yl)methyl group. A second-generation Hsp90 inhibitor. | benzamides; isoindoles; N-alkylpiperazine; resorcinols; tertiary carboxamide | antineoplastic agent; Hsp90 inhibitor |
cnf 2024 | 2-aminopurines; aromatic ether; organochlorine compound; pyridines | antineoplastic agent; Hsp90 inhibitor | |
snx 2112 | SNX 2112: an orally available small molecule Hsp90 inhibitor; structure in first source | ||
debio 0932 | CUDC 305: an Hsp90 inhibitor with antineoplastic activity; structure in first source | ||
pf 04929113 | |||
ch5164840 | CH5164840: biotin-labeled version of 17-dimethylaminoethylamino-17-demethoxygeldanamycin (17-DMAG) | ||
novobiocin | novobiocin : A coumarin-derived antibiotic obtained from Streptomyces niveus. Novobiocin: An antibiotic compound derived from Streptomyces niveus. It has a chemical structure similar to coumarin. Novobiocin binds to DNA gyrase, and blocks adenosine triphosphatase (ATPase) activity. (From Reynolds, Martindale The Extra Pharmacopoeia, 30th ed, p189) | carbamate ester; ether; hexoside; hydroxycoumarin; monocarboxylic acid amide; monosaccharide derivative; phenols | antibacterial agent; antimicrobial agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; Escherichia coli metabolite; hepatoprotective agent |
tas-116 | |||
2-(3,4-dimethoxyphenyl)-1-(5-methoxy-2,2-dimethyl-2h-chromen-6-yl)ethanone | 2-(3,4-dimethoxyphenyl)-1-(5-methoxy-2,2-dimethyl-2H-chromen-6-yl)ethanone: an Hsp90 inhibitor; structure in first source | ||
ver-246608 | VER-246608: inhibits pyruvate dehydrogenase kinase; structure in first source | ||
ver-50589 | VER-50589: inhibits heat shock protein 90 molecular chaperone; structure in first source | ||
ver 52296 | luminespib : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-(2,4-dihydroxy-5-isopropylphenyl)-4-[4-(morpholin-4-ylmethyl)phenyl]-1,2-oxazole-3-carboxylic acid with the amino group of ethylamine. | aromatic amide; isoxazoles; monocarboxylic acid amide; morpholines; resorcinols | angiogenesis inhibitor; antineoplastic agent; Hsp90 inhibitor |
sta 9090 | ring assembly; triazoles | ||
nms-e973 | NMS-E973: structure in first source |