objective To compare the efficacy of platinum and non-platinum-based regimens as first-line treatment for triple-negative breast cancer is advanced (TNBC) and analyze the relationship between their success and status of the BRCA genes.
method Retrospectively analyzed clinical data from 220 patients diagnosed with advanced pathological TNBC and treated in the Department of Breast Oncology, Peking University Cancer Hospital from 2013 to 2018 and evaluate the effectiveness of chemotherapy. A total of 114 patients had BRCA1 / 2 genes were tested by next generation sequencing (NGS) using peripheral blood, and we analyzed the correlation between efficacy and BRCA1 / 2 gene status.
result non-platinum-based chemotherapy (NPCT) was given to 129 and platinum-based chemotherapy (PBCT) to 91 study patients. The level of clinical benefit (CBR) and median progression-free survival (PFS) were not statistically different between groups NPCT and PBCT. Overall average life (OS) was 30.0 and 22.5 months for PBCT and NPCT groups, respectively [P = 0.090, hazard ratio (HR) = 0.703]. BRCA status assessed 114 patients, 14 of whom have a detrimental germline BRCA1 / 2 (gBRCA) mutation (seven in each group). In PBCT group, CBR was 85.7% and 35.1% for patients with and without mutations that destroy gBRCA, respectively (P = 0.039). Median PFS was 14.9 and 5.3 months and the median OS was 26.5 and 15.5 months for patients with and without mutations that destroy gBRCA, respectively (P = 0.001, P = 0.161, respectively). Patients in group PBCT have significantly greater levels of grade 3-4 anemia (5.5% vs. 0%) and thrombocytopenia (8.8% vs 0%), while the palmar-plantar erythrodysesthesia (12.4% vs 0% ) and peripheral neuropathy (8.6% vs. 1.1%) occurred more frequently in the group NPCT.
Efficacy of platinum in advanced triple-negative breast cancer with germline BRCA mutation determined by next generation sequencing.
conclusion platinum-based regimen was more effective in patients with mutations gBRCA damage, but there was no difference in patients without BRCA gene mutation, so that the non-platinum is an option in patients without BRCA gene mutation consider the toxicity and side effects. And we suggest that patients with advanced TNBC must have a BRCA gene test.
Description: Pazopanib HCl is a receptor tyrosine kinase inhibitor that targets multiple kinases, including VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit, and c-Fms, with IC50s 10nM, 30nM, 47nM, 84nM, 74nM, 140nM, and 146nM respectively [1-3].
Description: Pazopanib HCl is a receptor tyrosine kinase inhibitor that targets multiple kinases, including VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit, and c-Fms, with IC50s 10nM, 30nM, 47nM, 84nM, 74nM, 140nM, and 146nM respectively [1-3].
Description: Pazopanib HCl is a receptor tyrosine kinase inhibitor that targets multiple kinases, including VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit, and c-Fms, with IC50s 10nM, 30nM, 47nM, 84nM, 74nM, 140nM, and 146nM respectively [1-3].
Description: Pazopanib HCl is a receptor tyrosine kinase inhibitor that targets multiple kinases, including VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit, and c-Fms, with IC50s 10nM, 30nM, 47nM, 84nM, 74nM, 140nM, and 146nM respectively [1-3].
Description: Pazopanib HCl is a receptor tyrosine kinase inhibitor that targets multiple kinases, including VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit, and c-Fms, with IC50s 10nM, 30nM, 47nM, 84nM, 74nM, 140nM, and 146nM respectively [1-3].
Description: Bestatin hydrochloride, also known as Ubenimex, is an inhibitor of aminopeptidase B and N (APN)/CD13 [1].Bestatin, an antibiotic of microbial origin, is a potent inhibitor of some aminopeptidases which can be administered to cultured cells, intact animals and humans with low toxicity.
Description: Bestatin hydrochloride, also known as Ubenimex, is an inhibitor of aminopeptidase B and N (APN)/CD13 [1].Bestatin, an antibiotic of microbial origin, is a potent inhibitor of some aminopeptidases which can be administered to cultured cells, intact animals and humans with low toxicity.
Description: Bestatin hydrochloride, also known as Ubenimex, is an inhibitor of aminopeptidase B and N (APN)/CD13 [1].Bestatin, an antibiotic of microbial origin, is a potent inhibitor of some aminopeptidases which can be administered to cultured cells, intact animals and humans with low toxicity.
Description: Bestatin hydrochloride, also known as Ubenimex, is an inhibitor of aminopeptidase B and N (APN)/CD13 [1].Bestatin, an antibiotic of microbial origin, is a potent inhibitor of some aminopeptidases which can be administered to cultured cells, intact animals and humans with low toxicity.
Description: Flavopiridol hydrochloride is a selective inhibitor of CDK1, CDK2, CDK4 and CDK6 with IC50 value all ~41 nM as well as CDK7 with 300nM [1] [2] [3].CDKs are protein kinase families which involve in the process of regulating transcription, mRNA processing, cell differentiation and cell cycle.
Description: Flavopiridol hydrochloride is a selective inhibitor of CDK1, CDK2, CDK4 and CDK6 with IC50 value all ~41 nM as well as CDK7 with 300nM [1] [2] [3].CDKs are protein kinase families which involve in the process of regulating transcription, mRNA processing, cell differentiation and cell cycle.
Description: Flavopiridol hydrochloride is a selective inhibitor of CDK1, CDK2, CDK4 and CDK6 with IC50 value all ~41 nM as well as CDK7 with 300nM [1] [2] [3].CDKs are protein kinase families which involve in the process of regulating transcription, mRNA processing, cell differentiation and cell cycle.
Description: Flavopiridol hydrochloride is a selective inhibitor of CDK1, CDK2, CDK4 and CDK6 with IC50 value all ~41 nM as well as CDK7 with 300nM [1] [2] [3].CDKs are protein kinase families which involve in the process of regulating transcription, mRNA processing, cell differentiation and cell cycle.
Description: Flavopiridol hydrochloride is a selective inhibitor of CDK1, CDK2, CDK4 and CDK6 with IC50 value all ~41 nM as well as CDK7 with 300nM [1] [2] [3].CDKs are protein kinase families which involve in the process of regulating transcription, mRNA processing, cell differentiation and cell cycle.
Description: Resminostat is an inhibitor of histone deacetylase (HDAC) with IC50 values of 42.5nM, 50.1nM and 71.8nM, respectively against HDAC1, 3 and 6 [1].
Description: Resminostat is an inhibitor of histone deacetylase (HDAC) with IC50 values of 42.5nM, 50.1nM and 71.8nM, respectively against HDAC1, 3 and 6 [1].
Description: Resminostat is an inhibitor of histone deacetylase (HDAC) with IC50 values of 42.5nM, 50.1nM and 71.8nM, respectively against HDAC1, 3 and 6 [1].
Description: Resminostat is an inhibitor of histone deacetylase (HDAC) with IC50 values of 42.5nM, 50.1nM and 71.8nM, respectively against HDAC1, 3 and 6 [1].
Description: Rimonabant, also known as SR141716, was the first selective central cannabinoid (CB1) receptor inverse agonist (Ki = 1.8 nM) to be developed as an appetite suppressant, anti-obesity drug.
Description: Rimonabant, also known as SR141716, was the first selective central cannabinoid (CB1) receptor inverse agonist (Ki = 1.8 nM) to be developed as an appetite suppressant, anti-obesity drug.
Description: Rimonabant, also known as SR141716, was the first selective central cannabinoid (CB1) receptor inverse agonist (Ki = 1.8 nM) to be developed as an appetite suppressant, anti-obesity drug.
Description: Rimonabant, also known as SR141716, was the first selective central cannabinoid (CB1) receptor inverse agonist (Ki = 1.8 nM) to be developed as an appetite suppressant, anti-obesity drug.
Description: Rotigotine is dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively. Rotigotine also has significant affinity for 5-HT1A and adrenergic ?2B receptors. Rotigotine exhibits antiparkinsonian acitivity.
Description: Rotigotine is dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively. Rotigotine also has significant affinity for 5-HT1A and adrenergic ?2B receptors. Rotigotine exhibits antiparkinsonian acitivity.
Description: Rotigotine is dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively. Rotigotine also has significant affinity for 5-HT1A and adrenergic ?2B receptors. Rotigotine exhibits antiparkinsonian acitivity.
Description: Rotigotine is dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively. Rotigotine also has significant affinity for 5-HT1A and adrenergic ?2B receptors. Rotigotine exhibits antiparkinsonian acitivity.
Description: Rotigotine is dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively. Rotigotine also has significant affinity for 5-HT1A and adrenergic ?2B receptors. Rotigotine exhibits antiparkinsonian acitivity.
Description: Tipiracil is an inhibitor of Thymidine phosphorylase (TP). Thymidine phosphorylase (TP)is a key enzyme in the pyrimidine nucleoside salvage pathway.
Description: Tipiracil is an inhibitor of Thymidine phosphorylase (TP). Thymidine phosphorylase (TP)is a key enzyme in the pyrimidine nucleoside salvage pathway.
Description: Tipiracil is an inhibitor of Thymidine phosphorylase (TP). Thymidine phosphorylase (TP)is a key enzyme in the pyrimidine nucleoside salvage pathway.
Description: Tipiracil is an inhibitor of Thymidine phosphorylase (TP). Thymidine phosphorylase (TP)is a key enzyme in the pyrimidine nucleoside salvage pathway.
Description: Tipiracil is an inhibitor of Thymidine phosphorylase (TP). Thymidine phosphorylase (TP)is a key enzyme in the pyrimidine nucleoside salvage pathway.
Description: Description: IC50 Value: 40 nM (VEGFR2) [1]; 500 nM (EGFR) [2] Vandetanib is an anti-cancer drug that is used for the treatment of certain tumours of thethyroid gland.
Description: Description: IC50 Value: 40 nM (VEGFR2) [1]; 500 nM (EGFR) [2] Vandetanib is an anti-cancer drug that is used for the treatment of certain tumours of thethyroid gland.
Description: IC50: Vernakalant inhibits two specific potassium currents, IKur (IC50 = 9 ??) and IKACh (IC50=10 ?M) which are only present in atrial myocardium [1].Vernakalant blocks atrial potassium channels, thereby prolonging repolarization.
Description: IC50: Vernakalant inhibits two specific potassium currents, IKur (IC50 = 9 ??) and IKACh (IC50=10 ?M) which are only present in atrial myocardium [1].Vernakalant blocks atrial potassium channels, thereby prolonging repolarization.
Description: IC50: Vernakalant inhibits two specific potassium currents, IKur (IC50 = 9 ??) and IKACh (IC50=10 ?M) which are only present in atrial myocardium [1].Vernakalant blocks atrial potassium channels, thereby prolonging repolarization.
Description: Vilazodone (EMD 68843; SB 659746A; 5-{4-[4-(5-cyano-3-indolyl)-butyl]-1-piperazinyl}-benzofuran-2-carboxamide hydrochloride) is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist currently under clinical evaluation for the treatment of major depression.
Description: Vilazodone (EMD 68843; SB 659746A; 5-{4-[4-(5-cyano-3-indolyl)-butyl]-1-piperazinyl}-benzofuran-2-carboxamide hydrochloride) is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist currently under clinical evaluation for the treatment of major depression.
Description: Vilazodone (EMD 68843; SB 659746A; 5-{4-[4-(5-cyano-3-indolyl)-butyl]-1-piperazinyl}-benzofuran-2-carboxamide hydrochloride) is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist currently under clinical evaluation for the treatment of major depression.
Description: Voreloxin is a small molecule and a naphthyridine analogue with antineoplastic activity. Vosaroxin intercalates into DNA in a site-specific manner and blocks the re-ligation process carried out by topoisomerase II during DNA replication.
Description: Voreloxin is a small molecule and a naphthyridine analogue with antineoplastic activity. Vosaroxin intercalates into DNA in a site-specific manner and blocks the re-ligation process carried out by topoisomerase II during DNA replication.
Description: Voreloxin is a small molecule and a naphthyridine analogue with antineoplastic activity. Vosaroxin intercalates into DNA in a site-specific manner and blocks the re-ligation process carried out by topoisomerase II during DNA replication.
Description: PJ34 is a novel and potent inhibitor of poly(ADP-ribose) polymerase (PARP), an enzyme involved in DNA repair and cell proliferation, that dose-dependently inhibits purified PARP enzyme in a cell-free assay with half maximal effective concentration EC50 value of 20 nM.
Description: PJ34 is a novel and potent inhibitor of poly(ADP-ribose) polymerase (PARP), an enzyme involved in DNA repair and cell proliferation, that dose-dependently inhibits purified PARP enzyme in a cell-free assay with half maximal effective concentration EC50 value of 20 nM.
Description: PJ34 is a novel and potent inhibitor of poly(ADP-ribose) polymerase (PARP), an enzyme involved in DNA repair and cell proliferation, that dose-dependently inhibits purified PARP enzyme in a cell-free assay with half maximal effective concentration EC50 value of 20 nM.
Description: PJ34 is a novel and potent inhibitor of poly(ADP-ribose) polymerase (PARP), an enzyme involved in DNA repair and cell proliferation, that dose-dependently inhibits purified PARP enzyme in a cell-free assay with half maximal effective concentration EC50 value of 20 nM.
Description: PJ34 is a novel and potent inhibitor of poly(ADP-ribose) polymerase (PARP), an enzyme involved in DNA repair and cell proliferation, that dose-dependently inhibits purified PARP enzyme in a cell-free assay with half maximal effective concentration EC50 value of 20 nM.
Description: IC50: 2 nM: blocks the receptor tyrosine kinase RET in Drosophila.AD57, as a polypharmacological cancer therapeutic, is designed to regulate multiple targets related to cancer.
Description: IC50: 2 nM: blocks the receptor tyrosine kinase RET in Drosophila.AD57, as a polypharmacological cancer therapeutic, is designed to regulate multiple targets related to cancer.
Description: IC50: 2 nM: blocks the receptor tyrosine kinase RET in Drosophila.AD57, as a polypharmacological cancer therapeutic, is designed to regulate multiple targets related to cancer.
Description: IC50: 11.52 nM: inhibits monoamine oxidase (MAO) type A (MAO-A).IC50: 8.2 nM: blocks MAO type B (MAO-B).Pargyline, an irreversible and non-selective inhibitor of MAO, is used to treat moderate hypertension and cancer cells.
Description: IC50: 11.52 nM: inhibits monoamine oxidase (MAO) type A (MAO-A).IC50: 8.2 nM: blocks MAO type B (MAO-B).Pargyline, an irreversible and non-selective inhibitor of MAO, is used to treat moderate hypertension and cancer cells.
Description: Clenbuterol is a sympathomimetic ?2-adrenoceptor agonist. ?2-adrenoceptor agonists, mainly long-acting ?2-adrenoceptor agonists, are an important pharmacological approach to induce bronchodilation in patients with chronic obstructive pulmonary disease.
Description: Clenbuterol is a sympathomimetic ?2-adrenoceptor agonist. ?2-adrenoceptor agonists, mainly long-acting ?2-adrenoceptor agonists, are an important pharmacological approach to induce bronchodilation in patients with chronic obstructive pulmonary disease.
Description: Clenbuterol is a sympathomimetic ?2-adrenoceptor agonist. ?2-adrenoceptor agonists, mainly long-acting ?2-adrenoceptor agonists, are an important pharmacological approach to induce bronchodilation in patients with chronic obstructive pulmonary disease.
Description: Clenbuterol is a sympathomimetic ?2-adrenoceptor agonist. ?2-adrenoceptor agonists, mainly long-acting ?2-adrenoceptor agonists, are an important pharmacological approach to induce bronchodilation in patients with chronic obstructive pulmonary disease.
Description: EC50: 0.37 ?M for activating p53; 0.47 ?M for inhibiting NF-?B CBL0137 (hydrochloride) is a curaxin that activates p53 and inhibits NF-?B.
Description: EC50: 0.37 ?M for activating p53; 0.47 ?M for inhibiting NF-?B CBL0137 (hydrochloride) is a curaxin that activates p53 and inhibits NF-?B.
Description: EC50: 0.37 ?M for activating p53; 0.47 ?M for inhibiting NF-?B CBL0137 (hydrochloride) is a curaxin that activates p53 and inhibits NF-?B.
Description: EC50: 0.37 ?M for activating p53; 0.47 ?M for inhibiting NF-?B CBL0137 (hydrochloride) is a curaxin that activates p53 and inhibits NF-?B.
Description: EC50: 0.37 ?M for activating p53; 0.47 ?M for inhibiting NF-?B CBL0137 (hydrochloride) is a curaxin that activates p53 and inhibits NF-?B.
Description: Clinafloxacin is a broad-spectrum antibiotic of the quinolone carboxylic acid category that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumonia. Clinafloxacin, a fluoroquinolone, is currently in development for oral and intravenous therapy of serious infections.
Description: Clinafloxacin is a broad-spectrum antibiotic of the quinolone carboxylic acid category that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumonia. Clinafloxacin, a fluoroquinolone, is currently in development for oral and intravenous therapy of serious infections.
Description: Clinafloxacin is a broad-spectrum antibiotic of the quinolone carboxylic acid category that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumonia. Clinafloxacin, a fluoroquinolone, is currently in development for oral and intravenous therapy of serious infections.
Description: Clinafloxacin is a broad-spectrum antibiotic of the quinolone carboxylic acid category that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumonia. Clinafloxacin, a fluoroquinolone, is currently in development for oral and intravenous therapy of serious infections.
Description: Isoxsuprine is a modulator of ?2 adrenoreceptor and has agonist or antagonist effects.The ?2 adrenoceptors are a class of G protein-coupled receptors that are targets for epinephrine.
Description: Isoxsuprine is a modulator of ?2 adrenoreceptor and has agonist or antagonist effects.The ?2 adrenoceptors are a class of G protein-coupled receptors that are targets for epinephrine.
Description: Kanosamine is the antibiotic produced by Bacillus cereus UW85. Kanosamine showed highly inhibitory effects to the growth of plant-pathogenic oomycetes and moderately inhibitory effects to certain fungi and inhibited few bacterial species tested.
Description: Kanosamine is the antibiotic produced by Bacillus cereus UW85. Kanosamine showed highly inhibitory effects to the growth of plant-pathogenic oomycetes and moderately inhibitory effects to certain fungi and inhibited few bacterial species tested.
Description: Kanosamine is the antibiotic produced by Bacillus cereus UW85. Kanosamine showed highly inhibitory effects to the growth of plant-pathogenic oomycetes and moderately inhibitory effects to certain fungi and inhibited few bacterial species tested.
Description: Zoniporide (hydrochloride) is a novel, potent, and selective sodium-hydrogen exchanger isoform-1 (NHE-1) inhibitor [1]. The Na+/H+ exchanger (NHE) has been involved in intracellular pH homeostasis of many mammalian cell types.
Description: Zoniporide (hydrochloride) is a novel, potent, and selective sodium-hydrogen exchanger isoform-1 (NHE-1) inhibitor [1]. The Na+/H+ exchanger (NHE) has been involved in intracellular pH homeostasis of many mammalian cell types.
Description: Zoniporide (hydrochloride) is a novel, potent, and selective sodium-hydrogen exchanger isoform-1 (NHE-1) inhibitor [1]. The Na+/H+ exchanger (NHE) has been involved in intracellular pH homeostasis of many mammalian cell types.
Description: IC50: 20, 119, 83, 8, and 8 nM for PRMT1, 3, 4, 6, and 8, respectivelyMS023 is a type I PRMT inhibitor. Protein arginine methyltransferases (PRMTs) play a critical role in various biological processes.
Description: IC50: 20, 119, 83, 8, and 8 nM for PRMT1, 3, 4, 6, and 8, respectivelyMS023 is a type I PRMT inhibitor. Protein arginine methyltransferases (PRMTs) play a critical role in various biological processes.
Description: IC50: 20, 119, 83, 8, and 8 nM for PRMT1, 3, 4, 6, and 8, respectivelyMS023 is a type I PRMT inhibitor. Protein arginine methyltransferases (PRMTs) play a critical role in various biological processes.
Description: IC50: 20, 119, 83, 8, and 8 nM for PRMT1, 3, 4, 6, and 8, respectivelyMS023 is a type I PRMT inhibitor. Protein arginine methyltransferases (PRMTs) play a critical role in various biological processes.
Description: Chlorprothixene (hydrochloride) is an antagonist of dopamine receptor and histamine receptors [1]. Chlorprothixene is also an inhibitor of GABAA receptor [2]. All of these three receptors are implicated in many neurological processes, including motivation, pleasure, cognition, memory and learning.
Description: Chlorprothixene (hydrochloride) is an antagonist of dopamine receptor and histamine receptors [1]. Chlorprothixene is also an inhibitor of GABAA receptor [2]. All of these three receptors are implicated in many neurological processes, including motivation, pleasure, cognition, memory and learning.
Description: Chlorprothixene (hydrochloride) is an antagonist of dopamine receptor and histamine receptors [1]. Chlorprothixene is also an inhibitor of GABAA receptor [2]. All of these three receptors are implicated in many neurological processes, including motivation, pleasure, cognition, memory and learning.
Description: Chlorprothixene (hydrochloride) is an antagonist of dopamine receptor and histamine receptors [1]. Chlorprothixene is also an inhibitor of GABAA receptor [2]. All of these three receptors are implicated in many neurological processes, including motivation, pleasure, cognition, memory and learning.
Description: Chlorprothixene (hydrochloride) is an antagonist of dopamine receptor and histamine receptors [1]. Chlorprothixene is also an inhibitor of GABAA receptor [2]. All of these three receptors are implicated in many neurological processes, including motivation, pleasure, cognition, memory and learning.
Description: Cycloguanil is an inhibitor of dihydrofolate reductase (DHFR)[1].Dihydrofolate reductase (DHFR) is an enzyme that involved in reducing dihydrofolic acid to tetrahydrofolic acid.
Description: Cycloguanil is an inhibitor of dihydrofolate reductase (DHFR)[1].Dihydrofolate reductase (DHFR) is an enzyme that involved in reducing dihydrofolic acid to tetrahydrofolic acid.
Description: Cycloguanil is an inhibitor of dihydrofolate reductase (DHFR)[1].Dihydrofolate reductase (DHFR) is an enzyme that involved in reducing dihydrofolic acid to tetrahydrofolic acid.
Description: Bufuralol is a non-specific ?-adrenergic blocker. Beta adrenergic agonists are medications relaxing muscles of the airways, which widens the airways and leads to easier breathing.
Description: Bufuralol is a non-specific ?-adrenergic blocker. Beta adrenergic agonists are medications relaxing muscles of the airways, which widens the airways and leads to easier breathing.
Description: Bufuralol is a non-specific ?-adrenergic blocker. Beta adrenergic agonists are medications relaxing muscles of the airways, which widens the airways and leads to easier breathing.
Description: AN3365 is a potent and selective leucyl-tRNA synthetase inhibitor [1].The leucyl-tRNA synthetase belongs to a member of the class I aminoacyl-tRNA synthetase family.
Description: AN3365 is a potent and selective leucyl-tRNA synthetase inhibitor [1].The leucyl-tRNA synthetase belongs to a member of the class I aminoacyl-tRNA synthetase family.
Description: AN3365 is a potent and selective leucyl-tRNA synthetase inhibitor [1].The leucyl-tRNA synthetase belongs to a member of the class I aminoacyl-tRNA synthetase family.
Description: Calindol is an activator of the calcium-sensing receptor (CaSR).The extracellular calciumsensing receptor (CaSR), a G protein-coupled receptor (GPCR), senses extracellular calcium[Ca2+]e and regulates calciumion homeostasis.
Description: Calindol is an activator of the calcium-sensing receptor (CaSR).The extracellular calciumsensing receptor (CaSR), a G protein-coupled receptor (GPCR), senses extracellular calcium[Ca2+]e and regulates calciumion homeostasis.
Description: Calindol is an activator of the calcium-sensing receptor (CaSR).The extracellular calciumsensing receptor (CaSR), a G protein-coupled receptor (GPCR), senses extracellular calcium[Ca2+]e and regulates calciumion homeostasis.
Description: Kasugamycin is an aminoglycosidic antibiotic. Aminoglycoside, a medicinal and bacteriologic category of traditional Gram-negative antibacterial therapeutic agent, inhibits protein synthesis and contains as a portion of the molecule an amino-modified glycoside.
Description: Kasugamycin is an aminoglycosidic antibiotic. Aminoglycoside, a medicinal and bacteriologic category of traditional Gram-negative antibacterial therapeutic agent, inhibits protein synthesis and contains as a portion of the molecule an amino-modified glycoside.
Description: Fendiline is an ?2-adrenergic receptor antagonist and L-type calcium channel blocker [1,2].The ?2 adrenergic receptor is a G protein-coupled receptor (GPCR). Until now, three different ?2-receptor subtypes have been identified: ?2A, ?2B, and ?2C.
Description: (±)-Salsolinol targets depolarize dopamineric neurons. Dopaminergic neurons produce dopamine, a neurotransmitter with various roles in neurological functions.
Description: Ki: 2, 6.9, and 1.7 ?M for ?1A, ?1B, ?1D, respectivelyMidodrine is the prodrug of the ?1-adrenergic receptor agonist, 1-(2?,5?-dimethoxyphenyl)-2-aminoethanol.
Description: Ki: 2, 6.9, and 1.7 ?M for ?1A, ?1B, ?1D, respectivelyMidodrine is the prodrug of the ?1-adrenergic receptor agonist, 1-(2?,5?-dimethoxyphenyl)-2-aminoethanol.
Description: Celiprolol is a ?1 adrenergic receptor antagonist and ?2 adrenergic receptor partial agonist.?2 adrenergic receptor agonists, also known as adrenergic ?2 receptor agonists, are a class of drugs acting on the ?2 adrenergic receptor.
Description: Celiprolol is a ?1 adrenergic receptor antagonist and ?2 adrenergic receptor partial agonist.?2 adrenergic receptor agonists, also known as adrenergic ?2 receptor agonists, are a class of drugs acting on the ?2 adrenergic receptor.
Description: Celiprolol is a ?1 adrenergic receptor antagonist and ?2 adrenergic receptor partial agonist.?2 adrenergic receptor agonists, also known as adrenergic ?2 receptor agonists, are a class of drugs acting on the ?2 adrenergic receptor.
Description: Trimidox (hydrochloride) is a specific ribonucleotide reductase inhibitor [1][2][3]. Ribonucleotide reductase is the rate-limiting enzyme for de novo DNA synthesis.
Description: Trimidox (hydrochloride) is a specific ribonucleotide reductase inhibitor [1][2][3]. Ribonucleotide reductase is the rate-limiting enzyme for de novo DNA synthesis.
Description: Trimidox (hydrochloride) is a specific ribonucleotide reductase inhibitor [1][2][3]. Ribonucleotide reductase is the rate-limiting enzyme for de novo DNA synthesis.
Description: Trimidox (hydrochloride) is a specific ribonucleotide reductase inhibitor [1][2][3]. Ribonucleotide reductase is the rate-limiting enzyme for de novo DNA synthesis.
Description: Stachydrine is an anti-metastatic agent.Stachydrine, a pyrrolidine betaine, was first isolated from seed husk and the pulp of the fruit of C. Leonurus, and many other Asian plants and fruits.
Description: Stachydrine is an anti-metastatic agent.Stachydrine, a pyrrolidine betaine, was first isolated from seed husk and the pulp of the fruit of C. Leonurus, and many other Asian plants and fruits.
Description: Stachydrine is an anti-metastatic agent.Stachydrine, a pyrrolidine betaine, was first isolated from seed husk and the pulp of the fruit of C. Leonurus, and many other Asian plants and fruits.
Description: Stachydrine is an anti-metastatic agent.Stachydrine, a pyrrolidine betaine, was first isolated from seed husk and the pulp of the fruit of C. Leonurus, and many other Asian plants and fruits.
Description: Barnidipine is a calcium-channel blocker.A calcium channel, an ion channel which displays selective permeability to calcium ions, is sometimes synonymous as voltage-dependent calcium channel, although there are also ligand-gated calcium channels.
Description: Barnidipine is a calcium-channel blocker.A calcium channel, an ion channel which displays selective permeability to calcium ions, is sometimes synonymous as voltage-dependent calcium channel, although there are also ligand-gated calcium channels.
Description: Guanabenz is an orally active ?2-adrenoceptor agonist with hypotensive effects [1]. The ?2 adrenergic receptors belong to a family of G protein-coupled receptor (GPCR), mediate many physiological actions of the endogenous catecholamines adrenaline and noradrenaline.
Description: Guanabenz is an orally active ?2-adrenoceptor agonist with hypotensive effects [1]. The ?2 adrenergic receptors belong to a family of G protein-coupled receptor (GPCR), mediate many physiological actions of the endogenous catecholamines adrenaline and noradrenaline.
Description: Ulixertinib, also named as BVD-523, is a novel and reversible inhibitor of ERK1/2. Ulixertinib potently and selectively inhibits the activity of ERK1 and ERK2 kinases in a reversible, ATP-competitive fashion [1].
Description: Ulixertinib, also named as BVD-523, is a novel and reversible inhibitor of ERK1/2. Ulixertinib potently and selectively inhibits the activity of ERK1 and ERK2 kinases in a reversible, ATP-competitive fashion [1].
Description: Ulixertinib, also named as BVD-523, is a novel and reversible inhibitor of ERK1/2. Ulixertinib potently and selectively inhibits the activity of ERK1 and ERK2 kinases in a reversible, ATP-competitive fashion [1].
Description: Chlorcyclizine is a phenylpiperazine antagonist for histamine H1 receptor [1]. The histamine has been involved in modulating many physiological functions of the hypothalamus, such as arousal state, feeding, locomotor activity, and drinking.
Description: Chlorcyclizine is a phenylpiperazine antagonist for histamine H1 receptor [1]. The histamine has been involved in modulating many physiological functions of the hypothalamus, such as arousal state, feeding, locomotor activity, and drinking.
Description: Chlorcyclizine is a phenylpiperazine antagonist for histamine H1 receptor [1]. The histamine has been involved in modulating many physiological functions of the hypothalamus, such as arousal state, feeding, locomotor activity, and drinking.
Description: Chlorcyclizine is a phenylpiperazine antagonist for histamine H1 receptor [1]. The histamine has been involved in modulating many physiological functions of the hypothalamus, such as arousal state, feeding, locomotor activity, and drinking.
