PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 28040899-3 2017 Various substrates including the natural product alangiobussinine and the marinacarboline core structure were functionalized using carboline-directed delta-C(sp2)-H alkynylations. Carbolines 80-89 Sp2 transcription factor Homo sapiens 156-161 27934367-0 2016 Intramolecular Csp2-Csp2 Friedel-Crafts Arylation: Substrate- and Condition-Controlled Divergent Synthesis of Fused-beta-carbolines. Carbolines 115-131 regulator of calcineurin 2 Homo sapiens 15-19 27934367-0 2016 Intramolecular Csp2-Csp2 Friedel-Crafts Arylation: Substrate- and Condition-Controlled Divergent Synthesis of Fused-beta-carbolines. Carbolines 115-131 regulator of calcineurin 2 Homo sapiens 20-24 27934367-1 2016 A triple cooperative catalysis-mediated multicomponent reaction between 1-formyl-N-substituted-beta-carbolines, a terminal alkyne, and a secondary amine allows access to unprecedented polycyclic beta-carbolines via sequential A3-coupling and an intramolecular Csp2-Csp2 Friedel-Crafts arylation reaction. Carbolines 95-110 regulator of calcineurin 2 Homo sapiens 260-264 27934367-1 2016 A triple cooperative catalysis-mediated multicomponent reaction between 1-formyl-N-substituted-beta-carbolines, a terminal alkyne, and a secondary amine allows access to unprecedented polycyclic beta-carbolines via sequential A3-coupling and an intramolecular Csp2-Csp2 Friedel-Crafts arylation reaction. Carbolines 95-110 regulator of calcineurin 2 Homo sapiens 265-269 27230395-6 2016 The mechanisms responsible for the anti-addictive properties of ayahuasca and its alkaloids are not clarified, apparently involving both peripheral MAO-A inhibition by the beta-carbolines and central agonism of DMT at 5-HT2A receptors expressed in brain regions related to the regulation of mood and emotions. Carbolines 172-187 monoamine oxidase A Homo sapiens 148-153 27226119-0 2016 Visible Light Driven Photocascade Catalysis: Ru(bpy)3(PF6)2/TBHP-Mediated Synthesis of Fused beta-Carbolines in Batch and Flow Microreactors. Carbolines 93-108 sperm associated antigen 17 Homo sapiens 54-57 26583324-0 2015 Novel beta-carbolines inhibit Wnt/beta-catenin signaling. Carbolines 6-21 catenin beta 1 Homo sapiens 34-46 25770611-0 2015 Biosensor based on inhibition of monoamine oxidases A and B for detection of beta-carbolines. Carbolines 77-92 monoamine oxidase A Homo sapiens 33-59 27551464-0 2015 Novel beta-carbolines against colorectal cancer cell growth via inhibition of Wnt/beta-catenin signaling. Carbolines 6-21 catenin beta 1 Homo sapiens 82-94 26192590-0 2015 Selectivity Profiling and Biological Activity of Novel beta-Carbolines as Potent and Selective DYRK1 Kinase Inhibitors. Carbolines 55-70 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 95-100 25770611-7 2015 The presence of norharmane in mixtures of beta-carbolines can be identified based on the difference between the cumulative inhibition of MAO-A by all beta-carbolines and MAO-B inhibition. Carbolines 42-57 monoamine oxidase A Homo sapiens 137-142 25770611-7 2015 The presence of norharmane in mixtures of beta-carbolines can be identified based on the difference between the cumulative inhibition of MAO-A by all beta-carbolines and MAO-B inhibition. Carbolines 42-57 monoamine oxidase B Homo sapiens 170-175 25770611-1 2015 beta-Carbolines are inhibitors of monoamine oxidases (MAO-A and MAO-B) and can be found in foods, hallucinogenic plant or various drugs. Carbolines 0-15 monoamine oxidase A Homo sapiens 54-59 25770611-7 2015 The presence of norharmane in mixtures of beta-carbolines can be identified based on the difference between the cumulative inhibition of MAO-A by all beta-carbolines and MAO-B inhibition. Carbolines 150-165 monoamine oxidase A Homo sapiens 137-142 25770611-1 2015 beta-Carbolines are inhibitors of monoamine oxidases (MAO-A and MAO-B) and can be found in foods, hallucinogenic plant or various drugs. Carbolines 0-15 monoamine oxidase B Homo sapiens 64-69 25770611-6 2015 The MAO-A is inhibited by all three tested beta-carbolines (harmane, norharmane, and harmaline) while MAO-B is inhibited only by norharmane. Carbolines 43-58 monoamine oxidase A Homo sapiens 4-9 25498864-3 2015 Previous literature indicates that certain beta-carbolines including harmane modulate central monoamine levels partly through monoamine oxidase (MAO) inhibition. Carbolines 43-58 monoamine oxidase A Rattus norvegicus 126-143 25498864-3 2015 Previous literature indicates that certain beta-carbolines including harmane modulate central monoamine levels partly through monoamine oxidase (MAO) inhibition. Carbolines 43-58 monoamine oxidase A Rattus norvegicus 145-148 22425563-5 2012 The result of inhibition in human-AChE of serotonin, beta-carbolines and quinolines showed similar profile as eel-AChE with lower magnitude. Carbolines 53-68 acetylcholinesterase (Cartwright blood group) Homo sapiens 34-38 25240617-0 2014 Computational & experimental evaluation of the structure/activity relationship of beta-carbolines as DYRK1A inhibitors. Carbolines 86-101 dual specificity tyrosine phosphorylation regulated kinase 1A Homo sapiens 105-111 24373881-0 2014 Inhibition of monoamine oxidase (MAO) by beta-carbolines and their interactions in live neuronal (PC12) and liver (HuH-7 and MH1C1) cells. Carbolines 41-56 monoamine oxidase A Rattus norvegicus 14-31 24373881-0 2014 Inhibition of monoamine oxidase (MAO) by beta-carbolines and their interactions in live neuronal (PC12) and liver (HuH-7 and MH1C1) cells. Carbolines 41-56 monoamine oxidase A Rattus norvegicus 33-36 24373881-4 2014 Using kynuramine assays, intracellular MAO inhibition by beta-carbolines was measured in PC12 (rat pheochromocytoma), MH1C1 (rat liver), and HuH-7 (human liver) cell lines, which were compared with human recombinant MAO and cell lysates. Carbolines 57-72 monoamine oxidase A Rattus norvegicus 39-42 24373881-4 2014 Using kynuramine assays, intracellular MAO inhibition by beta-carbolines was measured in PC12 (rat pheochromocytoma), MH1C1 (rat liver), and HuH-7 (human liver) cell lines, which were compared with human recombinant MAO and cell lysates. Carbolines 57-72 MIR7-3 host gene Homo sapiens 141-146 24373881-5 2014 beta-Carbolines (1 muM, 90 min incubations) inhibited MAO by 40-99% in live PC12 cells where MAO A was the active isoform, and <12% in HuH-7 and MH1C1 cells where MAO B was primarily active. Carbolines 0-15 latexin Homo sapiens 19-22 24373881-5 2014 beta-Carbolines (1 muM, 90 min incubations) inhibited MAO by 40-99% in live PC12 cells where MAO A was the active isoform, and <12% in HuH-7 and MH1C1 cells where MAO B was primarily active. Carbolines 0-15 monoamine oxidase A Rattus norvegicus 54-57 24373881-5 2014 beta-Carbolines (1 muM, 90 min incubations) inhibited MAO by 40-99% in live PC12 cells where MAO A was the active isoform, and <12% in HuH-7 and MH1C1 cells where MAO B was primarily active. Carbolines 0-15 monoamine oxidase A Rattus norvegicus 93-98 24373881-5 2014 beta-Carbolines (1 muM, 90 min incubations) inhibited MAO by 40-99% in live PC12 cells where MAO A was the active isoform, and <12% in HuH-7 and MH1C1 cells where MAO B was primarily active. Carbolines 0-15 MIR7-3 host gene Homo sapiens 138-143 24373881-5 2014 beta-Carbolines (1 muM, 90 min incubations) inhibited MAO by 40-99% in live PC12 cells where MAO A was the active isoform, and <12% in HuH-7 and MH1C1 cells where MAO B was primarily active. Carbolines 0-15 monoamine oxidase B Rattus norvegicus 166-171 21992679-5 2012 Clorgyline and the beta-carbolines, harman and norharman, inhibited the oxidation of MPTP by MAO-A. Carbolines 19-34 monoamine oxidase A Homo sapiens 93-98 21992679-6 2012 Cigarette smoke, as well as the naturally occurring beta-carbolines (norharman and harman) isolated from smoke and coffee inhibited the oxidation of MPTP by MAO-B and/or MAO-A, suggesting protective effects against MPTP. Carbolines 52-67 monoamine oxidase B Homo sapiens 157-162 21992679-6 2012 Cigarette smoke, as well as the naturally occurring beta-carbolines (norharman and harman) isolated from smoke and coffee inhibited the oxidation of MPTP by MAO-B and/or MAO-A, suggesting protective effects against MPTP. Carbolines 52-67 monoamine oxidase A Homo sapiens 170-175 22717507-1 2012 The natural indole alkaloids, the beta-carbolines, are often associated with cholinesterase inhibition, especially their quaternary salts, which frequently have higher activity than the free bases. Carbolines 34-49 butyrylcholinesterase Homo sapiens 77-91 22335895-2 2012 High throughput screening of approximately 140,000 compounds identified the beta-carbolines harmine and harmol as moderately potent haspin kinase inhibitors. Carbolines 76-91 histone H3 associated protein kinase Mus musculus 132-138 20641293-6 2004 HAR is a carboline analog, which is a competitive and reversible inhibitor of MAO-A with a Ki of 5 nM (6). Carbolines 9-18 monoamine oxidase A Homo sapiens 78-83 22165909-2 2012 Substitutions to the carboline cap group were well-tolerated with substitution at the 2-position of both beta- and gamma-carbolines being optimal for HDAC6 activity and selectivity. Carbolines 21-30 histone deacetylase 6 Homo sapiens 150-155 21816955-4 2011 The five beta-carbolines that we tested, which possess a pyridinium-like structure and are structurally related to the neurotoxin 1-methyl-4-phenylpyridinium, inhibited PMAT with high affinity (IC(50) values of 39.1-65.5 muM). Carbolines 9-24 solute carrier family 29 member 4 Homo sapiens 169-173 21816955-5 2011 Cytotoxicity analysis further showed that cells expressing PMAT are 14- to 15-fold more sensitive to harmalan and norharmanium, suggesting that these two beta-carbolines are also transportable substrates of PMAT. Carbolines 154-169 solute carrier family 29 member 4 Homo sapiens 59-63 21816955-5 2011 Cytotoxicity analysis further showed that cells expressing PMAT are 14- to 15-fold more sensitive to harmalan and norharmanium, suggesting that these two beta-carbolines are also transportable substrates of PMAT. Carbolines 154-169 solute carrier family 29 member 4 Homo sapiens 207-211 20036304-10 2010 The potent inhibition of MAO-A by seed and root extracts of P. harmala containing beta-carbolines should contribute to the psychopharmacological and toxicological effects of this plant and could be the basis for its purported antidepressant actions. Carbolines 82-97 monoamine oxidase A Homo sapiens 25-30 21256758-0 2011 Synthesis of carbon-11-labeled bivalent beta-carbolines as new PET agents for imaging of cholinesterase in Alzheimer"s disease. Carbolines 40-55 butyrylcholinesterase Homo sapiens 89-103 20449727-6 2010 The AhR-activating property of the beta-carbolines is completely abrogated in AhR-deficient cells providing evidence that rutaecarpine, annomontine and xestomanzamine A are natural stimulators of the human AhR. Carbolines 35-50 aryl hydrocarbon receptor Homo sapiens 4-7 20449727-6 2010 The AhR-activating property of the beta-carbolines is completely abrogated in AhR-deficient cells providing evidence that rutaecarpine, annomontine and xestomanzamine A are natural stimulators of the human AhR. Carbolines 35-50 aryl hydrocarbon receptor Homo sapiens 78-81 20449727-6 2010 The AhR-activating property of the beta-carbolines is completely abrogated in AhR-deficient cells providing evidence that rutaecarpine, annomontine and xestomanzamine A are natural stimulators of the human AhR. Carbolines 35-50 aryl hydrocarbon receptor Homo sapiens 78-81 20885009-2 2010 Several beta-carbolines inhibited platelet aggregation induced by collagen, epinephrine, adenosine 5"-diphosphate, platelet-activating factor and thrombin. Carbolines 8-23 coagulation factor II, thrombin Homo sapiens 146-154 20361801-5 2010 While connecting beta-carboline units by alkylene spacers in two different series of compounds and subsequent evaluation of their AChE/BChE-inhibitory potential, we found that several of these bivalent beta-carbolines were potent NR blockers. Carbolines 202-217 acetylcholinesterase (Cartwright blood group) Homo sapiens 130-134 20361801-5 2010 While connecting beta-carboline units by alkylene spacers in two different series of compounds and subsequent evaluation of their AChE/BChE-inhibitory potential, we found that several of these bivalent beta-carbolines were potent NR blockers. Carbolines 202-217 butyrylcholinesterase Homo sapiens 135-139 20206015-4 2010 In addition, tadalafil analogues that were synthesized from l-tryptophan were more active than those derived from d-tryptophan, which is of economic value and expands the horizon for the discovery of new carbolines as PDE5 inhibitors. Carbolines 204-214 phosphodiesterase 5A Homo sapiens 218-222 19619142-2 2009 The present study screened four structurally similar beta-carbolines, 1,2,3,4-tetrahydronorharmane, norharmane, harmane and 6-methoxyharmalan, at recombinantly expressed alpha1, alpha1beta, alpha2 and alpha3 glycine receptors with the aims of identifying structural elements of both the receptor and the compounds that are important for binding and subunit specificity. Carbolines 53-68 adrenoceptor alpha 1D Homo sapiens 170-188 17692827-0 2007 Cytotoxicity of beta-carbolines in dopamine transporter expressing cells: structure-activity relationships. Carbolines 16-31 solute carrier family 6 member 3 Homo sapiens 35-55 19119997-0 2009 Structural analysis of carboline derivatives as inhibitors of MAPKAP K2 using 3D QSAR and docking studies. Carbolines 23-32 MAPK activated protein kinase 2 Homo sapiens 62-71 19119997-9 2009 The structure activity relationships elucidated here for carboline derivatives combined with their binding information will provide an integrated approach to explore the chemical space further for improving the potency of MAPKAPK2 inhibitors. Carbolines 57-66 MAPK activated protein kinase 2 Homo sapiens 222-230 18672028-14 2008 Insulin is potent in this effect; IC(50) of insulin was found to be about 4.3 x 10(-10) M. The insulin effect on the GABA dose responses looked like that of an antagonist similar to bicuculline or beta-carbolines. Carbolines 197-212 insulin Homo sapiens 0-7 18672028-14 2008 Insulin is potent in this effect; IC(50) of insulin was found to be about 4.3 x 10(-10) M. The insulin effect on the GABA dose responses looked like that of an antagonist similar to bicuculline or beta-carbolines. Carbolines 197-212 insulin Homo sapiens 44-51 18672028-14 2008 Insulin is potent in this effect; IC(50) of insulin was found to be about 4.3 x 10(-10) M. The insulin effect on the GABA dose responses looked like that of an antagonist similar to bicuculline or beta-carbolines. Carbolines 197-212 insulin Homo sapiens 95-102 18262425-4 2008 Delta-carbolines 3 and 4 showed better affinity than the corresponding beta-carbolines 1 and 2, respectively, while N-methylation (2, 4, and 6, respectively) of the pyrrole ring in 1, 3, and 5 resulted in the reduced affinity to the adenosine A(3) receptor. Carbolines 71-86 adenosine A3 receptor Homo sapiens 233-256 17883257-8 2007 beta-Carbolines were isolated from raisins and acted as good competitive inhibitors of MAO-A (harman) and MAO-B (norharman) isozymes. Carbolines 0-15 monoamine oxidase A Homo sapiens 87-92 17883257-8 2007 beta-Carbolines were isolated from raisins and acted as good competitive inhibitors of MAO-A (harman) and MAO-B (norharman) isozymes. Carbolines 0-15 monoamine oxidase B Homo sapiens 106-111 17583514-1 2007 beta-Carbolines stimulate insulin secretion in a glucose-dependent manner, probably by acting on I(3)-binding site. Carbolines 0-15 insulin Homo sapiens 26-33 15480838-10 2004 Various endogenous and exogenous heterocyclic molecules, which are structurally related to MPTP/MPP(+), such as isoquinolines and beta-carbolines, have been reported to exhibit similar toxic properties on DA cells, which are conferred by their uptake by the DAT. Carbolines 130-145 solute carrier family 6 member 3 Homo sapiens 258-261 16870220-8 2006 In contrast, various beta-carbolines were efficiently hydroxylated to hydroxy-beta-carbolines by CYP2D6. Carbolines 21-36 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 97-103 16870220-12 2006 Altogether, these results suggest that CYP2D6 can play an important role in the metabolic outcome of both MPTP and beta-carbolines. Carbolines 115-130 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 39-45 16061219-1 2005 This study was designed to determine the affinity and binding profile of beta-carbolines for imidazoline I2 receptors and catalytic sites of monoamine oxidase (MAO)-A/B in rat brain and liver. Carbolines 73-88 monoamine oxidase A Rattus norvegicus 141-166 16061219-5 2005 In brain and liver, competition curves for beta-carbolines against [3H]Ro41-1049 (MAO-A) and [3H]Ro19-6327 (MAO-B) were monophasic and resulted in different drug potencies for the two MAO isozymes (higher affinities for MAO-A) and in similar pharmacological profiles in both tissues. Carbolines 43-58 monoamine oxidase A Rattus norvegicus 82-87 16061219-5 2005 In brain and liver, competition curves for beta-carbolines against [3H]Ro41-1049 (MAO-A) and [3H]Ro19-6327 (MAO-B) were monophasic and resulted in different drug potencies for the two MAO isozymes (higher affinities for MAO-A) and in similar pharmacological profiles in both tissues. Carbolines 43-58 monoamine oxidase B Rattus norvegicus 108-113 16061219-5 2005 In brain and liver, competition curves for beta-carbolines against [3H]Ro41-1049 (MAO-A) and [3H]Ro19-6327 (MAO-B) were monophasic and resulted in different drug potencies for the two MAO isozymes (higher affinities for MAO-A) and in similar pharmacological profiles in both tissues. Carbolines 43-58 monoamine oxidase A Rattus norvegicus 82-85 16061219-5 2005 In brain and liver, competition curves for beta-carbolines against [3H]Ro41-1049 (MAO-A) and [3H]Ro19-6327 (MAO-B) were monophasic and resulted in different drug potencies for the two MAO isozymes (higher affinities for MAO-A) and in similar pharmacological profiles in both tissues. Carbolines 43-58 monoamine oxidase A Rattus norvegicus 220-225 16356849-1 2005 Mana-Hox, an analog of beta-carbolines with anticancer activity, induces aberrant mitosis and delays mitotic exit. Carbolines 23-38 mannosidase alpha class 2C member 1 Homo sapiens 0-4 14660022-7 2003 The results reveal that beta-carbolines can potentiate the rate of insulin secretion from human islets and suggest that these agents may be useful prototypes for the development of novel insulin secretagogues. Carbolines 24-39 insulin Homo sapiens 67-74 15262334-0 2004 The strong inhibition of triosephosphate isomerase by the natural beta-carbolines may explain their neurotoxic actions. Carbolines 66-81 triosephosphate isomerase 1 Homo sapiens 25-50 15262334-3 2004 Utilizing [3H]BC, we have identified several proteins to which BC binds with high affinity (e.g. the chaperone member glucose regulated protein 78, the enzyme carboxylesterase, the cytochrome P450 2E1, the enzyme monoamine oxidase B and a small G-protein of the Rho subfamily). Carbolines 14-16 monoamine oxidase B Homo sapiens 213-232 15262334-4 2004 In the present study we isolated a protein from bovine brain to which [3H]BC binds with high affinity and identified it being the enzyme triosephosphate isomerase (TPI; EC 5.3.1.1.). Carbolines 74-76 triosephosphate isomerase 1 Bos taurus 137-162 15262334-4 2004 In the present study we isolated a protein from bovine brain to which [3H]BC binds with high affinity and identified it being the enzyme triosephosphate isomerase (TPI; EC 5.3.1.1.). Carbolines 74-76 triosephosphate isomerase 1 Bos taurus 164-167 14660022-0 2003 Effects of the beta-carbolines, harmane and pinoline, on insulin secretion from isolated human islets of Langerhans. Carbolines 15-30 insulin Homo sapiens 57-64 14660022-2 2003 Recently, it has been proposed that beta-carbolines may be endogenous ligands having activity at imidazoline sites and we have, therefore, studied the effects of beta-carbolines on insulin secretion. Carbolines 162-177 insulin Homo sapiens 181-188 14660022-7 2003 The results reveal that beta-carbolines can potentiate the rate of insulin secretion from human islets and suggest that these agents may be useful prototypes for the development of novel insulin secretagogues. Carbolines 24-39 insulin Homo sapiens 187-194 14660022-3 2003 The beta-carbolines harmane, norharmane and pinoline increased insulin secretion two- to threefold from isolated human islets of Langerhans. Carbolines 4-19 insulin Homo sapiens 63-70 11909733-3 2002 While most beta-carbolines inhibited CDK2 and CDK5 to the same extent, selective inhibition against CDK2 was observed in 1-(2-chlorophenyl)- (12), 1-(2-fluorophenyl)- (15), and 1-(2-chloro-5-nitrophenyl)- (28) beta-carbolines. Carbolines 11-26 cyclin dependent kinase 2 Homo sapiens 37-41 15028583-9 2003 Thus, beta-carbolines represent a new class of insulin secretagogues, although it remains unclear whether their action is mediated solely by I(3) sites in the beta cell. Carbolines 6-21 insulin Homo sapiens 47-54 14568301-1 2003 This study investigated the inhibitory effect of 9H-pyrido[3,4-b]indole (norharman), one of the naturally occurring beta-carbolines, on cytochrome P450 (CYP)-related activities and the relationship between its inhibitory effect, its intercalation to DNA, and its comutagenic effect. Carbolines 116-131 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 136-151 14568301-1 2003 This study investigated the inhibitory effect of 9H-pyrido[3,4-b]indole (norharman), one of the naturally occurring beta-carbolines, on cytochrome P450 (CYP)-related activities and the relationship between its inhibitory effect, its intercalation to DNA, and its comutagenic effect. Carbolines 116-131 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 153-156 14568301-8 2003 Norharman"s inhibition of CYP and its enhancement of the N-OH-Glu-P-1 mutagenicity suggest that beta-carbolines modulate chemical carcinogenesis by controlling the xenobiotic metabolism and by intercalating to DNA. Carbolines 96-111 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 26-29 12804796-3 2003 beta-Carbolines and antioxidants (superoxide dismutase, catalase, ascorbate or rutin) prevented the loss of cell viability in PC12 cells treated with 250 microM MPP(+), while the effects of N-acetylcysteine and dithiothreitol were not observed. Carbolines 0-15 catalase Rattus norvegicus 56-64 12804796-6 2003 beta-Carbolines (50 microM) inhibited the decrease in mitochondrial transmembrane potential, cytochrome c release, activation of caspase-3, formation of reactive oxygen species (ROS) and depletion of GSH caused by MPP(+) in PC12 cells. Carbolines 0-15 caspase 3 Rattus norvegicus 129-138 12727306-1 2003 We have previously speculated that elevated levels of nicotinamide N-methyltransferase (NNMT), the primary catabolic enzyme of nicotinamide, may result in reduced Complex I activity in idiopathic Parkinson"s disease (IPD) in two ways: (1) reduction in the levels of nicotinamide available for nicotinamide adenine dinucleotide synthesis; and (2) increased methylation of compounds such as tetrahydroisoquinolines and beta-carbolines, which are potent Complex I inhibitors. Carbolines 417-432 nicotinamide N-methyltransferase Homo sapiens 54-86 12727306-1 2003 We have previously speculated that elevated levels of nicotinamide N-methyltransferase (NNMT), the primary catabolic enzyme of nicotinamide, may result in reduced Complex I activity in idiopathic Parkinson"s disease (IPD) in two ways: (1) reduction in the levels of nicotinamide available for nicotinamide adenine dinucleotide synthesis; and (2) increased methylation of compounds such as tetrahydroisoquinolines and beta-carbolines, which are potent Complex I inhibitors. Carbolines 417-432 nicotinamide N-methyltransferase Homo sapiens 88-92 12639576-0 2003 Synthesis and biological activities of novel beta-carbolines as PDE5 inhibitors. Carbolines 45-60 phosphodiesterase 5A Canis lupus familiaris 64-68 11909733-3 2002 While most beta-carbolines inhibited CDK2 and CDK5 to the same extent, selective inhibition against CDK2 was observed in 1-(2-chlorophenyl)- (12), 1-(2-fluorophenyl)- (15), and 1-(2-chloro-5-nitrophenyl)- (28) beta-carbolines. Carbolines 11-26 cyclin dependent kinase 5 Homo sapiens 46-50 11909733-3 2002 While most beta-carbolines inhibited CDK2 and CDK5 to the same extent, selective inhibition against CDK2 was observed in 1-(2-chlorophenyl)- (12), 1-(2-fluorophenyl)- (15), and 1-(2-chloro-5-nitrophenyl)- (28) beta-carbolines. Carbolines 11-26 cyclin dependent kinase 2 Homo sapiens 100-104 11909733-3 2002 While most beta-carbolines inhibited CDK2 and CDK5 to the same extent, selective inhibition against CDK2 was observed in 1-(2-chlorophenyl)- (12), 1-(2-fluorophenyl)- (15), and 1-(2-chloro-5-nitrophenyl)- (28) beta-carbolines. Carbolines 210-225 cyclin dependent kinase 2 Homo sapiens 100-104 12831203-5 2002 For aminoimidazoazaarenes, the most abundant ions were derived from the loss of a methyl group and the breaking of the aminoimidazole moiety, while for carbolines the major product ions arose from the loss of ammonia and HCN. Carbolines 152-162 metastasis associated lung adenocarcinoma transcript 1 Homo sapiens 221-224 10940539-0 2000 Binding of beta-carbolines and related agents at serotonin (5-HT(2) and 5-HT(1A)), dopamine (D(2)) and benzodiazepine receptors. Carbolines 11-26 5-hydroxytryptamine receptor 1A Homo sapiens 72-79 10940539-1 2000 A large series of beta-carbolines was examined for their ability to bind at [3H]agonist-labeled 5-HT(2A) serotonin receptors. Carbolines 18-33 5-hydroxytryptamine receptor 2A Homo sapiens 96-103 10940539-4 2000 The beta-carbolines were found to bind with modest affinity at 5-HT(2A) receptors, and affinity was highly dependent upon the presence of ring substituents and ring saturation. Carbolines 4-19 5-hydroxytryptamine receptor 2A Homo sapiens 63-70 10940539-7 2000 Although the only common receptor population that might account for this action is 5-HT(2A), on the basis of a lack of enhanced affinity for agonist-labeled 5-HT(2A) receptors, as well as on their lack of agonist action in the PI hydrolysis assay, it is difficult to conclude that the beta-carbolines behave in a manner consistent with that of other classical hallucinogens. Carbolines 285-300 5-hydroxytryptamine receptor 2A Homo sapiens 83-90 7699568-9 1994 In contrast, all the beta-carbolines investigated in this study had low potencies as inhibitors of monoamine oxidase B. Carbolines 21-36 monoamine oxidase B Bos taurus 99-118 10788565-5 2000 In vitro GRAB analysis has identified several imidazoline receptor ligands and beta-carbolines as AhR agonists and also revealed the presence of AhR agonist activity in crude DMSO extracts of commercial newspapers. Carbolines 79-94 aryl hydrocarbon receptor Homo sapiens 98-101 9534250-4 1998 A comparison with conventional matrices for carbohydrates (DHB and DHB/HIC) indicates that beta-carbolines provide the same level of sensitivity and resolution in the positive mode, but offer the advantage of high levels of sensitivity and resolution in the negative mode. Carbolines 91-106 MyoD family inhibitor domain containing Homo sapiens 71-74 8959985-11 1996 MAO-B is essential for the activation of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine to 1-methyl-4-phenylpyridinium ion, for a component of the enzymatic conversion of dopamine to hydrogen peroxide (H2O2), and for the activation of other potential toxins such as isoquinolines and beta-carbolines. Carbolines 282-297 monoamine oxidase B Homo sapiens 0-5 7491124-5 1995 The alterations, by beta-carbolines, of some important enzymatic systems, e.g. cytochrome P-450, have been clearly demonstrated, yet many discrepancies and contradictions exist so that an interpretation of the results and the definition of some common mechanism appears premature. Carbolines 20-35 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 79-95 1530666-3 1992 Harmaline and a number of other beta-carbolines inhibited HNMT with IC50 values in the range of 1-10 microM. Carbolines 32-47 histamine N-methyltransferase Rattus norvegicus 58-62 2167977-6 1990 In addition to H1 and A2, there appears to be a relatively narrow hydrophobic pocket in the binding cleft that can accommodate substituents at the 3-position of the beta-carbolines which have chain lengths less than or equal to C5. Carbolines 165-180 H1.5 linker histone, cluster member Homo sapiens 15-24 1530666-0 1992 Inhibition of histamine-N-methyltransferase (HNMT) by fragments of 9-amino-1,2,3,4-tetrahydroacridine (tacrine) and by beta-carbolines. Carbolines 119-134 histamine N-methyltransferase Rattus norvegicus 14-43 1530666-0 1992 Inhibition of histamine-N-methyltransferase (HNMT) by fragments of 9-amino-1,2,3,4-tetrahydroacridine (tacrine) and by beta-carbolines. Carbolines 119-134 histamine N-methyltransferase Rattus norvegicus 45-49 1652145-1 1991 Previous research has demonstrated that low doses of anxiogenic central benzodiazepine receptor (CBR) ligands, the beta-carbolines, improve performance in various learning and memory tests in animals if administered prior to training. Carbolines 115-130 cannabinoid receptor 1 Rattus norvegicus 64-95 1652145-1 1991 Previous research has demonstrated that low doses of anxiogenic central benzodiazepine receptor (CBR) ligands, the beta-carbolines, improve performance in various learning and memory tests in animals if administered prior to training. Carbolines 115-130 cannabinoid receptor 1 Rattus norvegicus 97-100 2137718-4 1990 The partially competitive nature of inhibition by one of the more effective pairs, 2-methyl-harmine and harmine, was consistent with uptake of the beta-carbolines by the synaptosomal dopamine uptake system, as was the fact that the accumulation of 2-[14C]methyl-harmine was significantly reduced by low Na+ media and by nomifensine, a potent inhibitor of the dopamine transporter. Carbolines 147-162 solute carrier family 6 member 3 Homo sapiens 359-379 35312174-0 2022 A green synthesis of Carbene-metal-amido (CMAs) Complexes and Carboline -derived CMAs with potent in vitro and ex vivo anti cancer activity. Carbolines 62-71 cytidine monophosphate N-acetylneuraminic acid synthetase Homo sapiens 81-85 34560263-0 2021 Development of BET inhibitors as potential treatments for cancer: A new carboline chemotype. Carbolines 72-81 delta/notch-like EGF repeat containing Mus musculus 15-18 2159126-2 1990 In rat brain DBI coexists with at least three different processing products and the members of this peptide family have been shown to displace benzodiazepines and beta carbolines from recognition sites located on the allosteric modulatory centers of GABAA receptors. Carbolines 163-178 diazepam binding inhibitor Rattus norvegicus 13-16 35180487-0 2022 Facile synthesis of C1-substituted beta-carbolines as CDK4 inhibitors for the treatment of cancer. Carbolines 35-50 cyclin dependent kinase 4 Homo sapiens 54-58 2450203-1 1988 Effects of benzodiazepines (BDZs) and beta carbolines (beta CCs) on sustained repetitive firing at high frequency (SRF) of action potentials of mouse spinal cord neurons in cell culture were examined using intracellular recording techniques. Carbolines 38-53 serum response factor Mus musculus 115-118 3882420-6 1985 This protease and the factor altering ER-DNA binding were eluted together from chromatography on DEAE-cellulose, AcA 44, and carboline-agarose and were sensitive to the same inhibitors. Carbolines 125-134 estrogen receptor 1 Bos taurus 38-40 3807051-1 1986 Two beta-carbolines, methyl beta-carboline-3-carboxylate (beta-CCM) and ethyl beta-carboline-3-carboxylate (beta-CCE), caused the parallel shift of the dose-response curve for cholecystokinin (CCK) in isolated guinea-pig gallbladder muscle. Carbolines 4-19 cholecystokinin Cavia porcellus 193-196 3819722-1 1987 Diazepam binding inhibitor (DBI), a peptide located in CNS neurons, blocks the binding of benzodiazepines and beta-carbolines to the allosteric modulatory sites of gamma-aminobutyric acid (GABAA) receptors. Carbolines 110-125 diazepam binding inhibitor Rattus norvegicus 0-32 3088605-5 1986 The concentration of 5 different beta-carbolines in platelet rich plasma (PRP) was measured using an HPLC-fluorometric method. Carbolines 33-48 proline rich protein 2-like 1 Rattus norvegicus 74-77 6864229-0 1983 In vitro studies on the effect of beta-carbolines on the activities of acetylcholinesterase and choline acetyltransferase and on the muscarinic receptor binding of the rat brain. Carbolines 34-49 acetylcholinesterase Rattus norvegicus 71-91 6431906-5 1984 Pseudomonad tryptophan 2,3-dioxygenase was inhibited by a different spectrum of beta-carbolines. Carbolines 80-95 tryptophan 2,3-dioxygenase Homo sapiens 12-38 6864229-0 1983 In vitro studies on the effect of beta-carbolines on the activities of acetylcholinesterase and choline acetyltransferase and on the muscarinic receptor binding of the rat brain. Carbolines 34-49 choline O-acetyltransferase Rattus norvegicus 96-121 6864229-1 1983 Acetylcholinesterase (acetylcholine acetylhydrolase, EC 3.1.1.7) activity and muscarinic receptor binding of homogenates from several brain structures were inhibited by beta-carbolines. Carbolines 169-184 acetylcholinesterase Rattus norvegicus 0-20 7130973-1 1982 The inhibitory action of a range of beta-carbolines on human and rat monoamine oxidase (MAO) A and B has been studied. Carbolines 36-51 monoamine oxidase A Rattus norvegicus 69-100 6142598-10 1983 Beta-carbolines such as PCC also discriminate receptor subtypes, yet they act as antagonists at the BZ receptor. Carbolines 0-15 crystallin gamma D Homo sapiens 24-27 7130973-4 1982 Of the carbolines which have been found endogenously, tetrahydro-beta-carboline, 6-methoxytetrahydro-beta-carboline and harmane are all sufficiently potent inhibitors of human MAO A, with I50 values of 5 X 10(-6), 10(-6), 5 X 10(-7) M respectively, for this property to be of possible physiological significance. Carbolines 7-17 monoamine oxidase A Homo sapiens 176-181 6121956-3 1981 Biochemical studies have revealed beta-carbolines" several actions, including inhibition of MAO-A, competitive inhibition of 5-HT uptake, general inhibition of Na+ dependent transports, binding to benzodiazepine and opiate receptors and probable action on dopamine receptors, which may all participate to a variable degree in the actions of different beta-carbolines. Carbolines 34-49 monoamine oxidase A Homo sapiens 92-97 6121956-10 1981 It has been suggested that some beta-carbolines act as the physiological ligands (agonists) of the benzodiazepine receptors, but the physiological beta-carbolines so far known seem to have other effects, such as the inhibition of MAO-A or 5-HT uptake in low concentrations. Carbolines 32-47 monoamine oxidase A Homo sapiens 230-235 6121956-10 1981 It has been suggested that some beta-carbolines act as the physiological ligands (agonists) of the benzodiazepine receptors, but the physiological beta-carbolines so far known seem to have other effects, such as the inhibition of MAO-A or 5-HT uptake in low concentrations. Carbolines 147-162 monoamine oxidase A Homo sapiens 230-235 5035798-0 1972 Naturally occurring and synthetic -carbolines as cholinesterase inhibitors. Carbolines 36-46 butyrylcholinesterase Homo sapiens 50-64 6255316-0 1980 [Study of binding of spin probes of the carboline and benzocarboline series to bovine serum albumin]. Carbolines 40-49 albumin Homo sapiens 86-100 32761352-1 2020 CYP2D6 metabolically inactivates several neurotoxins, including beta-carbolines, which are implicated in neurodegenerative diseases. Carbolines 64-79 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 0-6 31787028-2 2020 Previously we isolated a dimeric beta-carboline-type alkaloid Picrasidine C from the root of Picrasma quassioides as subtype-selective peroxisome proliferator-activated receptor alpha (PPARalpha) agonist. Carbolines 33-47 peroxisome proliferator activated receptor alpha Homo sapiens 185-194 32761352-2 2020 Variation in CYP2D6 within the brain may alter local inactivation of neurotoxic beta-carbolines, thereby influencing neurotoxicity. Carbolines 80-95 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 13-19 32926882-3 2020 The primary goal of this study was to evaluate the abuse potential of the beta-carbolines harmane, norharmane, and harmine - MAO inhibitors that are found in cigarette smoke - in an intracranial self-simulation (ICSS) model in rats. Carbolines 74-89 monoamine oxidase A Rattus norvegicus 125-128 32410501-1 2021 Pictet-Spengler cyclization method has been adopted for the synthesis of three carboline derived compounds: two compounds with tetrahydro gama- and beta- having CF3 group and amino alkyl chain at delta and alpha position, respectively, and another with guanidine alkyl chain at alpha-position.Structure-activity relationship of the analogues with human serum albumin was studied by fluorescence and Fourier-transform infrared spectroscopic analysis followed by molecular docking. Carbolines 79-88 albumin Homo sapiens 353-366 32766642-2 2020 In this work, two dinuclear phosphorescent rhenium(i) tricarbonyl complexes (DRe1 and DRe2) containing carboline derivatives have been synthesized, characterized and explored as potential chemotherapeutic and photodynamic therapy agents. Carbolines 103-112 kelch like family member 24 Homo sapiens 77-81 32766642-2 2020 In this work, two dinuclear phosphorescent rhenium(i) tricarbonyl complexes (DRe1 and DRe2) containing carboline derivatives have been synthesized, characterized and explored as potential chemotherapeutic and photodynamic therapy agents. Carbolines 103-112 cytokine induced apoptosis inhibitor 1 Homo sapiens 86-90 29268246-7 2018 As determined by HPLC-DAD, beta-carbolines, methylene blue, kaempferol and clorgyline inhibited MAO-A and methylene blue, 5-nitroindazole, norharman and deprenyl inhibited MAO-B, and all of them inhibited the oxidation of TMB in the same extent. Carbolines 27-42 monoamine oxidase A Homo sapiens 96-101 29268246-7 2018 As determined by HPLC-DAD, beta-carbolines, methylene blue, kaempferol and clorgyline inhibited MAO-A and methylene blue, 5-nitroindazole, norharman and deprenyl inhibited MAO-B, and all of them inhibited the oxidation of TMB in the same extent. Carbolines 27-42 monoamine oxidase B Homo sapiens 172-177 27977936-4 2017 The goal of this study is to determine the interaction of beta-carbolines with human OCT1, 2, and 3 (SLC22A1-3). Carbolines 58-73 solute carrier family 22 member 1 Homo sapiens 85-99 27977936-4 2017 The goal of this study is to determine the interaction of beta-carbolines with human OCT1, 2, and 3 (SLC22A1-3). Carbolines 58-73 solute carrier family 22 member 1 Homo sapiens 101-108 27977936-9 2017 All tested beta-carbolines potently inhibited hOCT2 with IC50 values in the sub- or low micromolar range. Carbolines 11-26 solute carrier family 22 member 2 Homo sapiens 46-51 27977936-15 2017 Our data support a significant role of hOCT1-3 in tissue uptake and disposition of beta-carbolines. Carbolines 83-98 solute carrier family 22 member 1 Homo sapiens 39-44 27977936-16 2017 Importantly, the potent inhibition of hOCT2 by beta-carbolines also raises the concern of potential drug interactions between naturally occurring bioactive alkaloids and drugs eliminated by hOCT2. Carbolines 47-62 solute carrier family 22 member 2 Homo sapiens 38-43 27977936-16 2017 Importantly, the potent inhibition of hOCT2 by beta-carbolines also raises the concern of potential drug interactions between naturally occurring bioactive alkaloids and drugs eliminated by hOCT2. Carbolines 47-62 solute carrier family 22 member 2 Homo sapiens 190-195 30326662-5 2018 Moreover, the levels of cytochrome C in mitochondria, and the expressions of bcl-2 protein, decreased after treatment with beta-carbolines, which indicated that 6i and 6u could induce mitochondria-mediated apoptosis. Carbolines 123-138 cytochrome c, somatic Homo sapiens 24-36 30326662-5 2018 Moreover, the levels of cytochrome C in mitochondria, and the expressions of bcl-2 protein, decreased after treatment with beta-carbolines, which indicated that 6i and 6u could induce mitochondria-mediated apoptosis. Carbolines 123-138 BCL2 apoptosis regulator Homo sapiens 77-82 29367595-7 2018 Molecular docking studies showed that the compounds could combine with the active site of AChE by the pi-pi or cation-pi action between the carboline ring and the phenyl rings of the residues, and the beta-carboline moiety is embedded in a cavity surrounded by four aromatic residues of Trp86, Tyr337, Trp439 and Tyr449. Carbolines 140-149 acetylcholinesterase (Cartwright blood group) Homo sapiens 90-94