Page last updated: 2024-10-24
regulation of neurotransmitter receptor localization to postsynaptic specialization membrane
Definition
Target type: biologicalprocess
Any process that modulates the frequency, rate or extent of neurotransmitter receptor localization to postsynaptic specialization membrane. [GOC:dos]
The intricate process of neurotransmitter receptor localization at the postsynaptic specialization membrane involves a complex interplay of molecular mechanisms that ensure precise and efficient synaptic transmission. This dynamic process is tightly regulated by a variety of factors, including:
1. **Transcriptional regulation:** The expression levels of neurotransmitter receptor genes are controlled by transcription factors that respond to neuronal activity and developmental cues. This ensures the appropriate amount of receptor protein is produced to meet the demands of the synapse.
2. **Protein trafficking:** Newly synthesized receptors are transported from the endoplasmic reticulum (ER) to the Golgi apparatus where they undergo post-translational modifications, including glycosylation and phosphorylation. From the Golgi, they are packaged into vesicles and transported to the synapse via microtubule-based motor proteins.
3. **Targeting and clustering:** At the synapse, receptors are targeted to the postsynaptic specialization membrane through interactions with scaffolding proteins, such as PSD-95 and gephyrin. These scaffolding proteins act as molecular organizers, clustering receptors and anchoring them to the membrane.
4. **Synaptic plasticity:** Receptor localization is highly dynamic and can be regulated in response to neuronal activity. For example, long-term potentiation (LTP), a form of synaptic strengthening, is associated with increased surface expression of AMPA receptors, while long-term depression (LTD) is associated with decreased surface expression of these receptors.
5. **Endocytosis and degradation:** Receptors are continuously internalized from the postsynaptic membrane via endocytosis. This process is regulated by clathrin-mediated endocytosis, a process that involves the formation of clathrin-coated pits that engulf receptors. Internalized receptors can either be recycled back to the surface or targeted for degradation in lysosomes.
The precise mechanisms regulating receptor localization vary depending on the specific receptor type and the synapse. However, the overarching principle is that these mechanisms ensure that the appropriate number and type of receptors are present at the postsynaptic membrane to allow for efficient and reliable synaptic transmission.'
"
Proteins (5)
| Protein | Definition | Taxonomy |
|---|---|---|
| Growth hormone secretagogue receptor type 1 | A growth hormone secretagogue receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q92847] | Homo sapiens (human) |
| Protein kinase C zeta type | A protein kinase C zeta type that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q05513] | Homo sapiens (human) |
| GTPase HRas | A GTPase HRas that is encoded in the genome of human. [PRO:DNx, UniProtKB:P01112] | Homo sapiens (human) |
| UDP-N-acetylglucosamine--peptide N-acetylglucosaminyltransferase 110 kDa subunit | A UDP-N-acetylglucosamine--peptide N-acetylglucosaminyltransferase 110 kDa subunit that is encoded in the genome of human. [PRO:DNx, UniProtKB:O15294] | Homo sapiens (human) |
| Disintegrin and metalloproteinase domain-containing protein 10 | A disintegrin and metalloproteinase domain-containing protein 10 that is encoded in the genome of human. [PRO:WCB, UniProtKB:O14672] | Homo sapiens (human) |
Compounds (184)
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| edelfosine | 1-octadecyl-2-methylglycero-3-phosphocholine : A glycerophosphocholine that is glycero-3-phosphocholine substituted at positions 1 and 2 by octadecyl and methyl groups respectively. edelfosine : A racemate comprising equimolar amounts of (R)- and (S)-edelfosine. edelfosine: RN given refers to parent cpd | glycerophosphocholine | |
| cgp 52411 | 4,5-dianilinophthalimide : Phthalimide substituted at the 4- and 5-positions by anilino groups. 4,5-dianilinophthalimide: structure given in first source | phthalimides | geroprotector; tyrosine kinase inhibitor |
| bisindolylmaleimide i | bisindolylmaleimide I: a bis(indolyl)maleimide | ||
| bisindolylmaleimide iv | indoles; maleimides | ||
| stallimycin | |||
| n-(2-(methylamino)ethyl)-5-isoquinolinesulfonamide | isoquinolines; sulfonamide | ||
| n-(2-aminoethyl)-5-isoquinolinesulfonamide | |||
| 1-(5-isoquinolinesulfonyl)piperazine | isoquinolines | ||
| fasudil | fasudil : An isoquinoline substituted by a (1,4-diazepan-1-yl)sulfonyl group at position 5. It is a Rho-kinase inhibitor and its hydrochloride hydrate form is approved for the treatment of cerebral vasospasm and cerebral ischemia. fasudil: intracellular calcium antagonist; structure in first source | isoquinolines; N-sulfonyldiazepane | antihypertensive agent; calcium channel blocker; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; geroprotector; neuroprotective agent; nootropic agent; vasodilator agent |
| staurosporine aglycone | staurosporine aglycone: metabolite from culture broth of Nocardiopsis sp.; a neurotrophin antag; inhibits BDNF TrkB receptor | ||
| minaprine | minaprine: Agr 1240 refers to di-HCl; short-acting type A MAO inhibitor (MAOI) of mild potency; structure | morpholines; pyridazines; secondary amine | antidepressant; antiparkinson drug; cholinergic drug; dopamine uptake inhibitor; serotonin uptake inhibitor |
| imatinib | aromatic amine; benzamides; N-methylpiperazine; pyridines; pyrimidines | antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor | |
| suramin | suramin : A member of the class of phenylureas that is urea in which each of the amino groups has been substituted by a 3-({2-methyl-5-[(4,6,8-trisulfo-1-naphthyl)carbamoyl]phenyl}carbamoyl)phenyl group. An activator of both the rabbit skeletal muscle RyR1 and sheep cardiac RyR2 isoform ryanodine receptor channels, it has been used for the treatment of human African trypanosomiasis for over 100 years. Suramin: A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties. | naphthalenesulfonic acid; phenylureas; secondary carboxamide | angiogenesis inhibitor; antinematodal drug; antineoplastic agent; apoptosis inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; GABA antagonist; GABA-gated chloride channel antagonist; purinergic receptor P2 antagonist; ryanodine receptor agonist; trypanocidal drug |
| uridine diphosphate | Uridine Diphosphate: A uracil nucleotide containing a pyrophosphate group esterified to C5 of the sugar moiety. | pyrimidine ribonucleoside 5'-diphosphate; uridine 5'-phosphate | Escherichia coli metabolite; mouse metabolite |
| benzoxazolone | 2-benzoxazolinone : A member of the class of benzoxazoles that is 2,3-dihydro-1,3-benzoxazole carrying an oxo group at position 2. benzoxazolone: RN given refers to parent cpd; structure | benzoxazole | allelochemical; phytoalexin |
| phenidone | phenidone: photographic developer; RN given refers to parent cpd; structure | ||
| tetradecanoylphorbol acetate | phorbol 13-acetate 12-myristate : A phorbol ester that is phorbol in which the hydroxy groups at the cyclopropane ring juction (position 13) and the adjacent carbon (position 12) have been converted into the corresponding acetate and myristate esters. It is a major active constituent of the seed oil of Croton tiglium. It has been used as a tumour promoting agent for skin carcinogenesis in rodents and is associated with increased cell proliferation of malignant cells. However its function is controversial since a decrease in cell proliferation has also been observed in several cancer cell types. phorbol ester : Esters of phorbol, originally found in croton oil (from Croton tiglium, of the family Euphorbiaceae). A number of phorbol esters possess activity as tumour promoters and activate the mechanisms associated with cell growth. Some of these are used in experiments as activators of protein kinase C. Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA. | acetate ester; diester; phorbol ester; tertiary alpha-hydroxy ketone; tetradecanoate ester | antineoplastic agent; apoptosis inducer; carcinogenic agent; mitogen; plant metabolite; protein kinase C agonist; reactive oxygen species generator |
| 4-ethynylbiphenyl | 4-ethynylbiphenyl: structure given in first source | ||
| substance p | peptide | neurokinin-1 receptor agonist; neurotransmitter; vasodilator agent | |
| staurosporine | indolocarbazole alkaloid; organic heterooctacyclic compound | apoptosis inducer; bacterial metabolite; EC 2.7.11.13 (protein kinase C) inhibitor; geroprotector | |
| norharman | beta-carboline : The parent compound of the beta-carbolines, a tricyclic structure comprising an indole ring system ortho- fused to C-3 and C-4 of a pyridine ring. norharman: RN given refers to parent cpd | beta-carbolines; mancude organic heterotricyclic parent | fungal metabolite; marine metabolite |
| rebeccamycin | rebeccamycin : An N-glycosyl compound consisting of a heteropolycyclic ring system with a glucosyl group attached to one of the indolic nitrogens. rebeccamycin: from actinomycete strain C-38,383; structure given in first source | indolocarbazole; N-glycosyl compound; organic heterohexacyclic compound; organochlorine compound | |
| 1-(5-isoquinolinesulfonyl)-2-methylpiperazine dihydrochloride | 1-(5-isoquinolinesulfonyl)-2-methylpiperazine dihydrochloride : A hydrochloride salt prepared from anileridine and two molar equivalents of hydrogen chloride. | hydrochloride | EC 2.7.11.13 (protein kinase C) inhibitor |
| 2-ethynylnaphthalene | 2-ethynylnaphthalene: RN given refers to unlabeled parent cpd | ||
| l 692429 | L 692429: stimulates release of growth hormone; RN refers to (R)-isomer; structure given in first source | ||
| gefitinib | aromatic ether; monochlorobenzenes; monofluorobenzenes; morpholines; quinazolines; secondary amino compound; tertiary amino compound | antineoplastic agent; epidermal growth factor receptor antagonist | |
| lestaurtinib | indolocarbazole | ||
| ilomastat | CS 610: matrix metalloproteinase inhibitor; structure in first source ilomastat : An N-acyl-amino acid obtained by formal condensation of the carboxy group of (2R)-2-[2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoic acid with the amino group of N-methyl-L-tryptophanamide. A cell permeable broad-spectrum matrix metalloproteinase (MMP) inhibitor | hydroxamic acid; L-tryptophan derivative; N-acyl-amino acid | anti-inflammatory agent; antibacterial agent; antineoplastic agent; EC 3.4.24.24 (gelatinase A) inhibitor; neuroprotective agent |
| lonafarnib | lonafarnib : A 4-{2-[4-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl]-2-oxoethyl}piperidine-1-carboxamide that has R configuration. It is used as oral farnesyltransferase inhibitor. lonafarnib: inhibitor of farnesyl protein transferase | 4-{2-[4-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl]-2-oxoethyl}piperidine-1-carboxamide | antineoplastic agent; EC 2.5.1.58 (protein farnesyltransferase) inhibitor |
| vatalanib | monochlorobenzenes; phthalazines; pyridines; secondary amino compound | angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; vascular endothelial growth factor receptor antagonist | |
| ruboxistaurin | ruboxistaurin: inhibits protein kinase C beta; structure in first source | ||
| canertinib | monochlorobenzenes; morpholines; organofluorine compound; quinazolines | antineoplastic agent; tyrosine kinase inhibitor | |
| cyc 202 | seliciclib : 2,6-Diaminopurine carrying benzylamino, (2R)-1-hydroxybutan-2-yl and isopropyl substituents at C-6, C-2-N and N-9 respectively. It is an experimental drug candidate in the family of pharmacological cyclin-dependent kinase (CDK) inhibitors. | 2,6-diaminopurines | antiviral drug; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor |
| sb 203580 | imidazoles; monofluorobenzenes; pyridines; sulfoxide | EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; geroprotector; Hsp90 inhibitor; neuroprotective agent | |
| enzastaurin | indoles; maleimides | ||
| erlotinib | aromatic ether; quinazolines; secondary amino compound; terminal acetylenic compound | antineoplastic agent; epidermal growth factor receptor antagonist; protein kinase inhibitor | |
| l 163191 | |||
| lapatinib | furans; organochlorine compound; organofluorine compound; quinazolines | antineoplastic agent; tyrosine kinase inhibitor | |
| cp 424391 | CP 424391: a growth hormone secretagogue; structure in first source | ||
| sorafenib | (trifluoromethyl)benzenes; aromatic ether; monochlorobenzenes; phenylureas; pyridinecarboxamide | angiogenesis inhibitor; anticoronaviral agent; antineoplastic agent; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; ferroptosis inducer; tyrosine kinase inhibitor | |
| l 778,123 | L-778,123 (free base) : A member of the class of imidazoles that is 1H-imidazole substituted by (4-cyanophenyl)methyl and [4-(3-chlorophenyl)-3-oxopiperazin-1-yl]methyl groups at positions 1 and 5, respectively. It is a dual inhibitor of FPTase and GGPTase-I. | imidazoles; monochlorobenzenes; nitrile; piperazinone; tertiary amino compound | antineoplastic agent; EC 2.5.1.58 (protein farnesyltransferase) inhibitor; EC 2.5.1.59 (protein geranylgeranyltransferase type I) inhibitor |
| bms 214662 | 7-cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine: a farnesyltransferase inhibitor; structure in first source BMS-214662 : A member of the class of benzodiazepines that is 2,3,4,5-tetrahydro-1H-1,4-benzodiazepine substituted by (1H-imidazol-5-yl)methyl, benzyl, (thiophen-2-yl)sulfonyl, and cyano groups at positions 1, 3R, 4 and 7, respectively. It is a potent inhibitor of farnesyltransferase (IC50 = 1.35nM) which was under clinical development for the treatment of solid tumors. | benzenes; benzodiazepine; imidazoles; nitrile; sulfonamide; thiophenes | antineoplastic agent; apoptosis inducer; EC 2.5.1.58 (protein farnesyltransferase) inhibitor |
| 7-n-butyl-6-(4'-hydroxyphenyl)-5h-pyrrolo(2,3b)pyrazine | |||
| purvalanol b | purvalanol B: protein kinase inhibitor; structure in first source | purvalanol | protein kinase inhibitor |
| h 89 | (E)-N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide : A N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide in which the double bond adopts a trans-configuration. N-(2-(4-bromocinnamylamino)ethyl)-5-isoquinolinesulfonamide: structure given in first source N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide : A member of the class of isoquinolines that is the sulfonamide obtained by formal condensation of the sulfo group of isoquinoline-5-sulfonic acid with the primary amino group of N(1)-[3-(4-bromophenyl)prop-2-en-1-yl]ethane-1,2-diamine. It is a protein kinase A inhibitor. | N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide | |
| 12-deoxyphorbol 13-acetate | phorbol ester | metabolite | |
| purvalanol a | 6-((3-chloro)anilino)-2-(isopropyl-2-hydroxyethylamino)-9-isopropylpurine: purvalanol A is the (1R)-isomer; | purvalanol | |
| s 1033 | (trifluoromethyl)benzenes; imidazoles; pyridines; pyrimidines; secondary amino compound; secondary carboxamide | anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor | |
| xl147 | aromatic amine; benzothiadiazole; quinoxaline derivative; sulfonamide | antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | |
| tamoxifen | stilbenoid; tertiary amino compound | angiogenesis inhibitor; antineoplastic agent; bone density conservation agent; EC 1.2.3.1 (aldehyde oxidase) inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; estrogen antagonist; estrogen receptor antagonist; estrogen receptor modulator | |
| sf 2370 | K-252a : A organic heterooctacyclic compound that is a potent inhibitor of protein kinase C and is isolated from Nocardiopsis sp K-252a SF 2370: indolocarbazole isolated from Actinomadura sp. SF-2370; structure given in first source | bridged compound; gamma-lactam; methyl ester; organic heterooctacyclic compound | antimicrobial agent; bacterial metabolite; EC 2.7.11.13 (protein kinase C) inhibitor; tropomyosin-related kinase B receptor antagonist |
| tandutinib | aromatic ether; N-arylpiperazine; N-carbamoylpiperazine; phenylureas; piperidines; quinazolines; tertiary amino compound | antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | |
| dasatinib | dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN). N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source | 1,3-thiazoles; aminopyrimidine; monocarboxylic acid amide; N-(2-hydroxyethyl)piperazine; N-arylpiperazine; organochlorine compound; secondary amino compound; tertiary amino compound | anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor |
| ha 1100 | HA 1100: intracellular calcium antagonist | ||
| 7-epi-hydroxystaurosporine | |||
| zd 6474 | CH 331: structure in first source | aromatic ether; organobromine compound; organofluorine compound; piperidines; quinazolines; secondary amine | antineoplastic agent; tyrosine kinase inhibitor |
| pd 407824 | |||
| harmine | harmine : A harmala alkaloid in which the harman skeleton is methoxy-substituted at C-7. Harmine: Alkaloid isolated from seeds of PEGANUM HARMALA; ZYGOPHYLLACEAE. It is identical to banisterine, or telepathine, from Banisteria caapi and is one of the active ingredients of hallucinogenic drinks made in the western Amazon region from related plants. It has no therapeutic use, but (as banisterine) was hailed as a cure for postencephalitic PARKINSON DISEASE in the 1920's. | harmala alkaloid | anti-HIV agent; EC 1.4.3.4 (monoamine oxidase) inhibitor; metabolite |
| sirolimus | sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent. Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties. | antibiotic antifungal drug; cyclic acetal; cyclic ketone; ether; macrolide lactam; organic heterotricyclic compound; secondary alcohol | antibacterial drug; anticoronaviral agent; antineoplastic agent; bacterial metabolite; geroprotector; immunosuppressive agent; mTOR inhibitor |
| ophiocordin | azepinostatin: isolated from Fusarium merismoides; structure in first source; RN assigned by CAS - 63590-19-2 (ophiocordin; azepinostatin is not the same as ophiocordin) | ||
| alvocidib | alvocidib : A synthetic dihydroxyflavone that is 5,7-dihydroxyflavone which is substituted by a 3-hydroxy-1-methylpiperidin-4-yl group at position 8 and by a chlorine at the 2' position (the (-)-3S,4R stereoisomer). A cyclin-dependent kinase 9 (CDK9) inhibitor, it has been studied for the treatment of acute myeloid leukaemia, arthritis and atherosclerotic plaque formation. alvocidib: structure given in first source | dihydroxyflavone; hydroxypiperidine; monochlorobenzenes; tertiary amino compound | antineoplastic agent; antirheumatic drug; apoptosis inducer; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor |
| arcyriaflavin a | arcyriaflavin A: from marine ascidian, Eudistoma sp.; structure given in first source | indolocarbazole | |
| pd 161570 | PD 161570: structure in first source | ||
| bosutinib | 4-((2,4-dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methyl-1-piperazinyl)propoxy)-3-quinolinecarbonitrile: a Src kinase inhibitor; structure in first source | aminoquinoline; aromatic ether; dichlorobenzene; N-methylpiperazine; nitrile; tertiary amino compound | antineoplastic agent; tyrosine kinase inhibitor |
| orantinib | orantinib : An oxindole that is 3-methyleneoxindole in which one of the hydrogens of the methylene group is substituted by a 2-(2-carboxyethyl)-3,5-dimethylpyrrol-3-yl group. It is an ATP-competitive inhibitor of the tyrosine kinase activity of fibroblast growth factor receptor 1. orantinib: an antiangiogenic agent | ||
| su 11248 | monocarboxylic acid amide; pyrroles | angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; immunomodulator; neuroprotective agent; vascular endothelial growth factor receptor antagonist | |
| urolithin d | urolithin D: has antiproliferative activity; structure in first source | hydroxycoumarin | |
| vx680 | N-arylpiperazine | ||
| cyc 116 | 4-methyl-5-(2-(4-morpholinophenylamino)pyrimidin-4-yl)thiazol-2-amine: an aurora kinase inhibitor; structure in first source | ||
| axitinib | aryl sulfide; benzamides; indazoles; pyridines | antineoplastic agent; tyrosine kinase inhibitor; vascular endothelial growth factor receptor antagonist | |
| a 419259 | |||
| b 43 | RK-24466 : A member of the class of pyrrolopyrimidines that is 7H-pyrrolo[2,3-d]pyrimidine substituted by amino, 4-phenoxyphenyl, and cyclopentyl groups at positions 4, 5 and 7, respectively. It is a potent inhibitor of Lck that inhibits Lck (64-509) and LckCD isoforms (IC50 of less than 1 and 2 nM, respectively). | aromatic amine; aromatic ether; cyclopentanes; primary amino compound; pyrrolopyrimidine | EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor; geroprotector |
| cgp 53353 | 4,5-bis(4-fluoroanilino)phthalimide: structure in first source | phthalimides | |
| temsirolimus | macrolide lactam | ||
| hexarelin | hexarelin: a synthetic growth hormone releasing peptide; structurally similar to GHRP-6, with the substitution of D-Trp with its 2-methyl derivative; more potent & stable and less toxic than GHRP-6 | ||
| pep005 | 3-ingenyl angelate: protein kinase C agonist and antineoplastic; structure in first source | ||
| on 01910 | N-[2-methoxy-5-({[2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl}methyl)phenyl]glycine : A glycine derivative that is glycine in which one of the hydrogens of the amino group is substituted by a 2-methoxy-5-({[2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl}methyl)phenyl group. ON 01910: a Plk1 inhibitor with antineoplastic activity; structure in first source rigosertib : An N-[2-methoxy-5-({[2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl}methyl)phenyl]glycine in which the double bond has E-configuration. It is a non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM and exhibits anti-cancer properties. | N-[2-methoxy-5-({[2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl}methyl)phenyl]glycine | antineoplastic agent; apoptosis inducer; EC 2.7.11.21 (polo kinase) inhibitor; microtubule-destabilising agent |
| a 770041 | aromatic amide | ||
| [4-[[4-(1-benzothiophen-2-yl)-2-pyrimidinyl]amino]phenyl]-[4-(1-pyrrolidinyl)-1-piperidinyl]methanone | benzamides; N-acylpiperidine | ||
| sm 130686 | SM 130686: a growth hormone secretagogue; structure in first source | ||
| macimorelin | |||
| av 412 | |||
| edotecarin | |||
| tabimorelin | tabimorelin: a growth hormone secretagogue; structure in first source | ||
| cp 547632 | 3-(4-bromo-2,6-difluorobenzyloxy)-5-(3-(4-pyrrolidin-1-ylbutyl)ureido)isothiazole-4-carboxylic acid amide: inhibits vascular endothelial growth factor receptor-2 tyrosine kinase; structure in first source | ||
| ripasudil | isoquinolines | ||
| osi 930 | OSI 930: inhibits both receptor tyrosine kinase Kit and kinase insert domain receptor; structure in first source | aromatic amide | |
| scio-469 | SCIO-469: a small-molecule p38 mitogen-activated protein (MAP) kinase inhibitor for potential oral therapy for inflammatory disorders; in phase lib clinical trials for rheumatoid arthritis 4/2004 talmapimod : An indolecarboxamide obtained by formal condensation of the carboxy group of 6-chloro-3-[(dimethylamino)(oxo)acetyl]-1-methylindole-5-carboxylic acid with the secondary amino group of (2S,5R)-1-[(4-fluorophenyl)methyl]-2,5-dimethylpiperazine. It is a potent inhibitor of MAPK and exhibits anti-cancer properties. | aromatic amide; aromatic ketone; chloroindole; dicarboxylic acid diamide; indolecarboxamide; monofluorobenzenes; N-acylpiperazine; N-alkylpiperazine | antineoplastic agent; apoptosis inducer; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor |
| cp 724714 | 2-methoxy-N-(3-(4-((3-methyl-4-((6-methyl-3-pyridinyl)oxy)phenyl)amino)-6-quinazolinyl)-2-propenyl)acetamide: CP-724714 is the ((2E)-isomer, 1:1.5 succinate); structure in first source | 2-methoxy-N-[3-[4-[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]anilino]-6-quinazolinyl]prop-2-enyl]acetamide | antineoplastic agent; apoptosis inducer; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; hepatotoxic agent |
| hmn-214 | (E)-4-(2-(2-(N-acetyl-N-(4-methoxybenzenesulfonyl)amino)stilbazole)) 1-oxide: an antineoplastic agent; structure in first source | ||
| l 162752 | |||
| ct52923 | CT52923: structure in first source | ||
| tivozanib | N-(2-chloro-4-((6,7-dimethoxy-4-quinolyl)oxy)phenyl)-N'-(5-methyl-3-isoxazolyl)urea: KNR-951 is the HCl, monohydrate salt; an antineoplastic agent; structure in first source | aromatic ether | |
| hki 272 | nitrile; quinolines | antineoplastic agent; tyrosine kinase inhibitor | |
| sk&f 110679 | |||
| cediranib | aromatic ether | ||
| ps1145 | PS1145: IkappaB kinase inhibitor; structure in first source | beta-carbolines | |
| chir 99021 | CHIR 99021 : A member of the class of aminopyrimidines that is 2-aminopyrimidine substituted at positions N2, 5 and 6 by (5-cyanopyridin-2-yl)ethyl, 4-methylimidazol-2-yl and 2,4-dichlorophenyl groups respectively. Chir 99021: structure in first source | aminopyridine; aminopyrimidine; cyanopyridine; diamine; dichlorobenzene; imidazoles; secondary amino compound | EC 2.7.11.26 (tau-protein kinase) inhibitor |
| masitinib | 1,3-thiazoles; benzamides; N-alkylpiperazine; pyridines | antineoplastic agent; antirheumatic drug; tyrosine kinase inhibitor | |
| azd 6244 | AZD 6244: a MEK inhibitor | benzimidazoles; bromobenzenes; hydroxamic acid ester; monochlorobenzenes; organofluorine compound; secondary amino compound | anticoronaviral agent; antineoplastic agent; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor |
| su 14813 | 5-((5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl)-N-(2-hydroxy-3-morpholin-4-ylpropyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide: has both antineoplastic and antiangiogenic activities; structure in first source | ||
| bibw 2992 | aromatic ether; enamide; furans; monochlorobenzenes; organofluorine compound; quinazolines; secondary carboxamide; tertiary amino compound | antineoplastic agent; tyrosine kinase inhibitor | |
| sotrastaurin | sotrastaurin : A member of the class of maleimides that is maleimide which is substituted at position 3 by an indol-3-yl group and at position 4 by a quinazolin-4-yl group, which in turn is substituted at position 2 by a 4-methylpiperazin-1-yl group. It is a potent and selective inhibitor of protein kinase C and has been investigated as an immunosuppresant in renal transplant patients. sotrastaurin: a potent protein kinase C-selective inhibitor; structure in first source | indoles; maleimides; N-alkylpiperazine; N-arylpiperazine; quinazolines | anticoronaviral agent; EC 2.7.11.13 (protein kinase C) inhibitor; immunosuppressive agent |
| saracatinib | aromatic ether; benzodioxoles; diether; N-methylpiperazine; organochlorine compound; oxanes; quinazolines; secondary amino compound | anticoronaviral agent; antineoplastic agent; apoptosis inducer; autophagy inducer; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor; radiosensitizing agent | |
| vx 702 | VX 702: a p38 MAP kinase inhibitor | phenylpyridine | |
| crenolanib | aminopiperidine; aromatic ether; benzimidazoles; oxetanes; quinolines; tertiary amino compound | angiogenesis inhibitor; antineoplastic agent; apoptosis inducer; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | |
| tg100-115 | 3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol: for treatment of ischemia reperfusion injury; structure in first source | pteridines | |
| ly 338522 | LY 338522: des-methyl metabolite of LY333531; structure in first source | ||
| PDGF receptor tyrosine kinase inhibitor III | PDGF receptor tyrosine kinase inhibitor III : An N-arylpiperazine that is piperazine in which the hydrogen attached to the nitrogen at position 1 is replaced by a (4-phenoxyphenyl)aminocarbonyl group, while the hydrogen attached to the nitrogen at position 4 is replaced by a 6,7-dimethoxyquinazolin-4-yl group. It is an inhibitor of tyrosine kinases FLT3, PDGFR and KIT. | aromatic ether; N-arylpiperazine; N-carbamoylpiperazine; phenylureas; quinazolines; tertiary amino compound | EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor |
| brivanib | aromatic ether; diether; fluoroindole; pyrrolotriazine; secondary alcohol | angiogenesis inhibitor; antineoplastic agent; apoptosis inducer; drug metabolite; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; fibroblast growth factor receptor antagonist | |
| rgb 286638 | |||
| bms-566394 | BMS-566394: structure in first source | ||
| at 7519 | 4-(2,6-dichlorobenzamido)-N-(piperidin-4-yl)-pyrazole-3-carboxamide : A member of the class of pryrazoles that is 4-amino-1H-pyrazole-3-carboxylic acid in which the primary amino group has been acylated by a 2,6-dichlorobenzoyl group and in which the carboxylic acid has been converted into a carboxamide by formal condensation with the primary amino group of 4-aminopiperidine. | dichlorobenzene; piperidines; pyrazoles; secondary carboxamide | antineoplastic agent; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor |
| bms-690514 | |||
| inno-406 | biaryl | ||
| N-[5-[[5-[(4-acetyl-1-piperazinyl)-oxomethyl]-4-methoxy-2-methylphenyl]thio]-2-thiazolyl]-4-[(3,3-dimethylbutan-2-ylamino)methyl]benzamide | benzamides | ||
| abt 869 | aromatic amine; indazoles; phenylureas | angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | |
| azd 8931 | sapitinib : A member of the class of quinazolines that is 4-amino-7-methoxyquinazoline in which the amino group has been substituted by a 3-chloro-2-fluorophenyl group and in which position 6 of the quinoline ring has been substituted by a {1-[2-(methylamino)-2-oxoethyl]piperidin-4-yl}oxy group. Sapitinib is a dual tyrosine kinase inhibitor (TKI) of epithelial growth factor receptors (EGFR) HER2 and HER3. | aromatic ether; monochlorobenzenes; monofluorobenzenes; piperidines; quinazolines; secondary amino compound; tertiary amino compound | EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; epidermal growth factor receptor antagonist |
| arq 197 | indoles | ||
| ridaforolimus | macrolide lactam | ||
| ulimorelin | ulimorelin: ghrelin agonist; an 18-membered macrocycle containing 3 amide bonds and a secondary amine as well as 4 stereogenic centers; belongs to macrocyclic peptidomimetics | oligopeptide | |
| ch 4987655 | |||
| cc-930 | |||
| gw 2580 | 5-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)pyrimidine-2,4-diamine: a cFMS kinase inhibitor; structure in first source | ||
| incb3619 | INCB3619: ADAM inhibitor; structure in first source | ||
| chir-265 | aromatic ether | ||
| motesanib | pyridinecarboxamide | ||
| fostamatinib | fostamatinib: a spleen tyrosine kinase (Syk) inhibitor, metabolized to R406 | ||
| trametinib | acetamides; aromatic amine; cyclopropanes; organofluorine compound; organoiodine compound; pyridopyrimidine; ring assembly | anticoronaviral agent; antineoplastic agent; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; geroprotector | |
| mln8054 | benzazepine | ||
| pf-562,271 | indoles | ||
| ly2603618 | ureas | ||
| tg100801 | |||
| dactolisib | dactolisib : An imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment. dactolisib: antineoplastic agent that inhibits both phosphatidylinositol 3-kinase and mTOR | imidazoquinoline; nitrile; quinolines; ring assembly; ureas | antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; mTOR inhibitor |
| gsk 461364 | GSK 461364: an antineoplastic agent that inhibits polo-like kinase 1 | (trifluoromethyl)benzenes | |
| n-(3-fluorophenyl)-1-((4-(((3s)-3-methyl-1-piperazinyl)methyl)phenyl)acetyl)-4-piperidinamine | N-(3-fluorophenyl)-1-((4-(((3S)-3-methyl-1-piperazinyl)methyl)phenyl)acetyl)-4-piperidinamine: a small molecule motilin receptor agonist; structure in first source | acetamides | |
| e 7050 | aromatic ether | ||
| 2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)-7-pyrido[2,3-d]pyrimidinone | pyrazolopyridine | ||
| tak-901 | |||
| buparlisib | NVP-BKM120: a pan class I PI3 kinase inhibitor with antineoplastic activity; structure in first source | aminopyridine; aminopyrimidine; morpholines; organofluorine compound | antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor |
| azd 1480 | |||
| pha 848125 | N,1,4,4-tetramethyl-8-((4-(4-methylpiperazin-1-yl)phenyl)amino)-4,5-dihydro-1H-pyrazolo(4,3-h)quinazoline-3-carboxamide: a cyclin dependent kinase inhibitor | ||
| gsk690693 | 1,2,5-oxadiazole; acetylenic compound; aromatic amine; aromatic ether; imidazopyridine; piperidines; primary amino compound; tertiary alcohol | antineoplastic agent; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | |
| 14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene | 14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene: has antineoplastic activity; also inhibits Fms-like tyrosine kinase-3; structure in first source | ||
| pf 04217903 | quinolines | ||
| gdc 0941 | pictrelisib : A sulfonamide composed of indazole, morpholine, and methylsulfonyl-substituted piperazine rings bound to a thienopyrimidine ring. | indazoles; morpholines; piperazines; sulfonamide; thienopyrimidine | EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor |
| icotinib | |||
| yil 781 | YIL 781: an appetite suppressant and weight loss promoter; structure in first source | ||
| kx-01 | |||
| mk 5108 | aromatic ether | ||
| cudc 101 | 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide: a histone deacetylase inhibitor; structure in first source | ||
| mln 8237 | MLN 8237: an aurora kinase A inhibitor | benzazepine | |
| bms 754807 | BMS 754807: an IGR-1R kinase inhibitor; structure in first source | pyrazoles; pyridines; pyrrolidines; pyrrolotriazine | antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor |
| sgi 1776 | SGI 1776: a Pim kinase inhibitor; structure in first source | imidazoles | |
| mk-1775 | adavosertib: a Wee1 kinase inhibitor; structure in first source | piperazines | |
| dcc-2036 | rebastinib: an inhibitor of Tie2 tyrosine kinase receptor and antineoplastic agent | organofluorine compound; phenylureas; pyrazoles; pyridinecarboxamide; quinolines | tyrosine kinase inhibitor |
| cabozantinib | cabozantinib : A dicarboxylic acid diamide that is N-phenyl-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide in which the hydrogen at position 4 on the phenyl ring is substituted by a (6,7-dimethoxyquinolin-4-yl)oxy group. A multi-tyrosine kinase inhibitor, used (as its malate salt) for the treatment of progressive, metastatic, medullary thyroid cancer. cabozantinib: a multikinase inhibitor | aromatic ether; dicarboxylic acid diamide; organofluorine compound; quinolines | antineoplastic agent; tyrosine kinase inhibitor |
| poziotinib | HM781-36B: antitumor irreversible Pan-HER inhibitor for treatment of gastric cancer | acrylamides; aromatic ether; dichlorobenzene; diether; monofluorobenzenes; N-acylpiperidine; quinazolines; secondary amino compound; substituted aniline | antineoplastic agent; apoptosis inducer; epidermal growth factor receptor antagonist |
| TAK-580 | MLN 2480: brain-penetrant RAF dimer antagonist TAK-580 : A 1,3-thiazolecarboxamide that is 2-[(1R)-1-aminoethyl]-1,3-thiazole-5-carboxylic acid in which the carboxy group undergoes formal condensation with the amino group of 5-chloro-4-(trifluoromethyl)pyridin-2-amine and in which the amino group undergoes formal condensation with the carboxy group of 6-amino-5-chloropyrimidine-4-carboxylic acid. It is a pan-RAF kinase inhibitor which is currently in clinical development for the treatment of radiographically recurrent or progressive low-grade glioma in children and young adults. | 1,3-thiazolecarboxamide; aminopyrimidine; chloropyridine; organofluorine compound; pyrimidinecarboxamide; secondary carboxamide | antineoplastic agent; apoptosis inducer; B-Raf inhibitor |
| gsk 2126458 | omipalisib : A member of the class of quinolines that is quinoline which is substituted by pyridazin-4-yl and 5-[(2,4-difluorobenzene-1-sulfonyl)amino]-6-methoxypyridin-3-yl groups at positions 4 and 6, respectively. It is a highly potent inhibitor of PI3K and mTOR developed by GlaxoSmithKline and was previously in human phase 1 clinical trials for the treatment of idiopathic pulmonary fibrosis and solid tumors. omipalisib: inhibitor of mTOR protein | aromatic ether; difluorobenzene; pyridazines; pyridines; quinolines; sulfonamide | anticoronaviral agent; antineoplastic agent; autophagy inducer; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; mTOR inhibitor; radiosensitizing agent |
| emd1214063 | tepotinib: MET inhibitor | ||
| pf 3758309 | PF 3758309: a PAK4 p21-activated kinase inhibitor; structure in first source | organic heterobicyclic compound; organonitrogen heterocyclic compound; organosulfur heterocyclic compound | |
| (5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol | (5-(2,4-bis((3S)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol: a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity; structure in first source | benzyl alcohols; morpholines; pyridopyrimidine; tertiary amino compound | antineoplastic agent; apoptosis inducer; mTOR inhibitor |
| gsk 1363089 | GSK 1363089: a multikinase inhibitor that acts on Met, RON, Axl, and VEGFR; structure in first source | aromatic ether | |
| kin-193 | pyridopyrimidine | ||
| bay 869766 | |||
| as 703026 | pyridinecarboxamide | ||
| grassystatin a | grassystatin A: isolated from a cyanobacterium, identified as Lyngbya cf.; structure in first source | ||
| dabrafenib | 1,3-thiazoles; aminopyrimidine; organofluorine compound; sulfonamide | anticoronaviral agent; antineoplastic agent; B-Raf inhibitor | |
| nitd 609 | NITD 609: an antimalarial and coccidiostat; structure in first source | ||
| pki 587 | gedatolisib: inhibits both phosphatidylinositol 3-kinase and mTOR; structure in first source | ||
| gsk 2334470 | GSK 2334470: a PDK1 inhibitor; structure in first source | indazoles | |
| abemaciclib | |||
| mk-8776 | |||
| jnj38877605 | quinolines | ||
| dinaciclib | pyrazolopyrimidine | ||
| alectinib | aromatic ketone; morpholines; nitrile; organic heterotetracyclic compound; piperidines | antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | |
| gsk2141795 | GSK2141795: an Akt inhibitor with antineoplastic activity; structure in first source | ||
| cep-32496 | agerafenib: inhibitor of RAF family kinases; structure in first source | ||
| ceritinib | ceritinib : A member of the class of aminopyrimidines that is 2,6-diamino-5-chloropyrimidine in which the amino groups at positions 2 and 6 are respectively carrying 2-methoxy-4-(piperidin-4-yl)-5-methylphenyl and 2-(isopropylsulfonyl)phenyl substituents. Used for the treatment of ALK-positive metastatic non-small cell lung cancer. ceritinib: an anaplastic lymphoma kinase inhibitor | aminopyrimidine; aromatic ether; organochlorine compound; piperidines; secondary amino compound; sulfone | antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor |
| tetrahydroamentoflavone | tetrahydroamentoflavone: isolated from Semecarpus anacardium; structure in first source | ||
| chir 258 | |||
| osi 027 | OSI 027: inhibits both mTORC1 and mTORC2; structure in first source | ||
| nintedanib | nintedanib : A member of the class of oxindoles that is a kinase inhibitor used (in the form of its ethylsulfonate salt) for the treatment of idiopathic pulmonary fibrosis and cancer. |