Page last updated: 2024-12-04

cystamine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cystamine is a disulfide derivative of cysteamine, a naturally occurring aminothiol. It is synthesized through the dimerization of cysteamine. Cystamine is known to act as a radioprotector, protecting against radiation-induced damage. It also exhibits antioxidant properties and has been explored as a potential therapeutic agent for conditions like Alzheimer's disease, Parkinson's disease, and amyotrophic lateral sclerosis (ALS). The protective effects of cystamine are attributed to its ability to scavenge reactive oxygen species (ROS) and modulate various signaling pathways involved in neurodegeneration. Research on cystamine focuses on understanding its mechanisms of action, exploring its therapeutic potential, and optimizing its delivery and administration.'

Cross-References

ID SourceID
PubMed CID2915
CHEMBL ID61350
CHEBI ID78757
SCHEMBL ID43866
MeSH IDM0005528

Synonyms (88)

Synonym
AKOS005431478
KBIO1_000828
DIVK1C_000828
NCI60_003711
NCI60_004921
SPECTRUM_001526
LOPAC0_000297
brn 1736027
ethylamine, 2,2'-dithiobis-
becaptan disulfure [french]
beta-mercaptoethylamine disulfide
2,2'-dithiobisethanamine
1591 l
cystinamin [german]
mercamine disulfide
einecs 200-129-4
beta,beta'-diaminodiethyl disulfide
cystineamine
bis(beta-aminoethyl)disulfide
2,2'-dithiobis(ethylamine)
cystinamin
cysteinamine disulfide
2-((2-aminoethyl)dithio)ethylamine
NCGC00013459-02
lopac-c-7255
ethanamine, 2,2'-dithiobis-
cystamine ,
2,2'-dithiobis[ethylamine]
2-(2-aminoethyldisulfanyl)ethanamine
51-85-4
decarboxycystine
NCGC00013459
BSPBIO_003434
SPECTRUM5_001336
NCI39322
KBIO2_004574
KBIOGR_001405
KBIO3_002937
KBIOSS_002006
KBIO2_002006
KBIO2_007142
SPECTRUM2_001591
NCISTRUC1_000465
SPECTRUM3_001897
NCISTRUC2_000420
SPECTRUM4_000833
SPBIO_001582
NINDS_000828
IDI1_000828
NCGC00096574-02
NCGC00096574-01
2,2'-disulfanediyldiethanamine
STK386775
0FEBEABE-F9D6-44CA-B070-61908595E698
NCGC00013459-05
chebi:78757 ,
CHEMBL61350
becaptan disulfure
4-04-00-01577 (beilstein handbook reference)
unii-r110lv8l02
r110lv8l02 ,
BBL010640
CCG-37943
NCGC00013459-04
NCGC00013459-03
2-aminoethyl disulfide
bis(.beta.-aminoethyl)disulfide
bis(.beta.-aminoethyl)disulphide
.beta.,.beta.'-diaminodiethyl disulphide
cystamine [mi]
.beta.,.beta.'-diaminodiethyl disulfide
SCHEMBL43866
2-[(2-aminoethyl)disulfanyl]ethylamine #
.beta.-mercaptoethylamine disulfide
3,4-dithiahexyl-1,6-diamine
2-(2-aminoethyldisulfanyl)ethylamine
BP-22847
aminoethyl-ss-ethylamine
DTXSID60199005
2-[(2-aminoethyl)disulfanyl]ethan-1-amine
VS-02600
Q2662688
SDCCGSBI-0050285.P004
NCGC00013459-08
AT21144
CS-0086613
HY-124476
EN300-60838

Research Excerpts

Overview

Cystamine (CysN) is a multipotent molecule with healthy effects. It is an inhibitor of transglutaminases (TGs), including the TG type 2 (TG2), an enzyme with pleiotropic functions. Cystamine is a candidate drug; however, the mechanisms by which it operates remain unclear.

ExcerptReferenceRelevance
"Cystamine is a small disulfide that gives rise to sulfane sulfur when it undergoes oxidation catalyzed by diamine oxidase (a ubiquitous enzyme in animals)."( Sulfur metabolism in AIDS: cystamine as an anti-HIV agent.
Toohey, JI, 2009
)
1.37
"Cystamine (CysN) is a multipotent molecule with healthy effects and, moreover, it is an inhibitor of transglutaminases (TGs), including the TG type 2 (TG2), an enzyme with pleiotropic functions, involved in different pathways of inflammation and central in the pathogenesis of some human disorders as the IBD."( Beneficial effects of treatment with transglutaminase inhibitor cystamine on the severity of inflammation in a rat model of inflammatory bowel disease.
Bardella, MT; Bonura, A; Braidotti, P; Busca, G; Ciulla, MM; Elli, L; Ferrero, S; Maioli, C; Paliotti, R; Roncoroni, L; Terrani, C, 2011
)
1.33
"Cystamine is a more potent inhibitor for TGase than cysteamine with different kinetics pattern in a non-reducing condition."( Different inhibition characteristics of intracellular transglutaminase activity by cystamine and cysteamine.
Cho, SY; Jang, GY; Jeon, JH; Kim, CW; Kim, IG; Lee, HJ; Park, SC; Shim, DM; Yeo, EJ, 2004
)
1.27
"Cystamine is a byproduct of pantetheinase-catalyzed pantothenic acid recycling from pantetheine for biosynthesis of Coenzyme A (CoA), a ubiquitous and metabolically indispensable cofactor."( Post-translational disulfide modifications in cell signaling--role of inter-protein, intra-protein, S-glutathionyl, and S-cysteaminyl disulfide modifications in signal transmission.
Chu, F; O'Brian, CA, 2005
)
1.05
"Cystamine is a candidate drug; however, the mechanisms by which it operates remain unclear."( Cystamine and cysteamine increase brain levels of BDNF in Huntington disease via HSJ1b and transglutaminase.
Alberch, J; Borrell-Pagès, M; Brouillet, E; Bryson, EA; Canals, JM; Cheetham, ME; Cordelières, FP; Grange, G; Guillermier, M; Hantraye, P; Hirsch, E; Humbert, S; Néri, C; Parker, JA; Pineda, JR; Saudou, F, 2006
)
2.5

Effects

Cystamine has been shown to cause marked suppression of HIV replication in cultured lymphocytes and macrophages. Cystamine is currently being evaluated in a human clinical trial in Huntington's disease (HD)

ExcerptReferenceRelevance
"Cystamine has been shown to cause marked suppression of HIV replication in cultured lymphocytes and macrophages; the inference is that the cystamine/diamine oxidase system may replace the cystine/cystathionase system as a source of sulfane sulfur."( Sulfur metabolism in AIDS: cystamine as an anti-HIV agent.
Toohey, JI, 2009
)
1.37
"Cystamine has shown significant neuroprotective properties in preclinical studies of Parkinson's disease (PD) and Huntington's disease (HD). "( Cystamine metabolism and brain transport properties: clinical implications for neurodegenerative diseases.
Bousquet, M; Calon, F; Cicchetti, F; Gibrat, C; Ouellet, M; Rouillard, C, 2010
)
3.25
"Cystamine has demonstrated neuroprotective activity in a variety of studies, and is currently being evaluated in a human clinical trial in Huntington's disease (HD). "( Cystamine and ethyl-eicosapentaenoic acid treatment fail to prevent malonate-induced striatal toxicity in mice.
Leavitt, BR; Sivananthan, SN, 2011
)
3.25
"Cystamine has been reported to be taken up and metabolized to taurine by the rat lung slices. "( The uptake and metabolism of cystamine and taurine by isolated perfused rat and rabbit lungs.
Kodavanti, UP; Mehendale, HM; Sharma, R; Smith, LL, 1995
)
2.03
"Both cystamine and taurine have been implicated as antioxidants, and we suggest that cystamine is actively accumulated by the lung as part of the process to protect pulmonary tissue against oxidative stress."( The accumulation of cystamine and its metabolism to taurine in rat lung slices.
Cohen, GM; Haschek, WM; Lewis, CP; Smith, LL; Wyatt, I, 1989
)
1.06

Actions

ExcerptReferenceRelevance
"Cystamine caused an increase in the concentration of mainly nonprotein thiols, whereas the mexamine administration increased the protein SH-groups (mainly between the 20th and 30th min after treatment)."( The concentrations of SH-groups in some radiosensitive tissues after the administration of radioprotectors in rats.
Krízala, J; Ledvina, M; Stoklasová, A, 1980
)
0.98

Treatment

Cystamine treatment of various genetic models of HD demonstrated protection against neurodegeneration and/or improvement in behavior. Cystamine pretreatment significantly decreased TG2 activity and gene expression in the Cyst+VILI group (P < 0.05)

ExcerptReferenceRelevance
"Cystamine pretreatment significantly decreased TG2 activity and gene expression in the Cyst+VILI group (P < 0.05)."( Effects of transglutaminase 2 inhibition on ventilator-induced lung injury.
Hur, GY; In, KH; Kang, KH; Kim, JH; Lee, EJ; Lee, SH; Lee, SY; Min, KH; Oh, WO; Shim, JJ; Shin, C; Suh, IB; Yoon, DW, 2014
)
1.12
"Cystamine treatment significantly increased brain-derived neurotrophic factor (BDNF) levels and phosphorylation of TrkB in brain after stroke."( Cystamine improves functional recovery via axon remodeling and neuroprotection after stroke in mice.
Chen, YC; Cui, Y; Ding, J; Jiao, Y; Ju, SH; Li, PC; Qian, C; Teng, GJ; Yang, XY; Yao, HH, 2015
)
2.58
"Cystamine treatment attenuated ICH-induced brain swelling (day 3: 14.4+/-3.2 vs."( Tissue-type transglutaminase and the effects of cystamine on intracerebral hemorrhage-induced brain edema and neurological deficits.
Hua, Y; Keep, RF; Okauchi, M; Xi, G, 2009
)
1.33
"Cystamine treatment of various genetic models of HD demonstrated protection against neurodegeneration and/or improvement in behavior."( Cystamine and ethyl-eicosapentaenoic acid treatment fail to prevent malonate-induced striatal toxicity in mice.
Leavitt, BR; Sivananthan, SN, 2011
)
2.53
"Cystamine treatment was performed by daily intraperitoneal administration."( Cystamine attenuates lupus-associated apoptosis of ventricular tissue by suppressing both intrinsic and extrinsic pathways.
Chen, TY; Chiang, SY; Hsu, TC; Kao, SH; Kuo, CY; Li, SL; Tzang, BS, 2012
)
2.54
"Cystamine pre-treatment restored ΔF508-CFTR response to the CFTR potentiators genistein, Vrx-532 or Vrx-770 in freshly isolated brushed nasal epithelial cells from ΔF508-CFTR homozygous patients."( Targeting autophagy as a novel strategy for facilitating the therapeutic action of potentiators on ΔF508 cystic fibrosis transmembrane conductance regulator.
Carnuccio, R; De Matteis, A; Esposito, S; Gavina, M; Guido, S; Kroemer, G; Luciani, A; Luini, A; Maiuri, L; Maiuri, MC; Pettoello-Mantovani, M; Raia, V; Russo, I; Scholte, B; Silano, M; Villella, VR, 2012
)
1.1
"Cystamine treatment normalized transglutaminase and GGEL levels in R6/2 mice."( Therapeutic effects of cystamine in a murine model of Huntington's disease.
Beal, MF; Bogdanov, M; Cooper, AJ; Dedeoglu, A; Ferrante, RJ; Hersch, SM; Jeitner, TM; Kowall, NW; Kubilus, JK; Matson, SA; Matson, WR; Ratan, RR, 2002
)
1.35
"Cystamine treatment also ameliorated the striatal volume loss and striatal neuronal atrophy observed in these animals, but was unable to prevent motor dysfunction or the down-regulation of dopamine and cyclic adenosine monophsophate-regulated phosphoprotein (DARPP-32) expression in the striatum."( Cystamine treatment is neuroprotective in the YAC128 mouse model of Huntington disease.
Bailey, CD; Hayden, MR; Johnson, GV; Leavitt, BR; Pearson, J; Rogers, DA; Van Raamsdonk, JM, 2005
)
2.49
"Cystamine treatment lowered the degree of cross-linking of the pigmentation antigen gp75/TRP-1 in MM418c5 cells."( Inhibition of melanin synthesis by cystamine in human melanoma cells.
Gardiner, B; Kay, G; Parsons, PG; Qiu, L; Sturm, RA; Tonks, I; Zhang, M, 2000
)
1.31
"The cystamine-treated cells demonstrated a marked inhibition of sickling under hypoxic conditions, a decrease in their mean corpuscular hemoglobin concentration, and a significant increase in their oxygen affinity."( Inhibition of erythrocyte sickling by cystamine, a thiol reagent.
Beuzard, Y; Hassan, W; Rosa, J, 1976
)
1.01
"Cystamine post-treatment, therefore, does not appear to inhibit toxicant-induced influx of extracellular calcium into toxicant-damaged cells."( Amelioration of carbon tetrachloride-induced hepatic necrosis by post-toxicant treatment with cystamine.
Gandolfi, AJ; MacDonald, JR; Sipes, IG, 1986
)
1.21
"Treatment with cystamine resulted in amelioration of impaired function with concomitant enhancement of axonal remodeling. "( Cystamine improves functional recovery via axon remodeling and neuroprotection after stroke in mice.
Chen, YC; Cui, Y; Ding, J; Jiao, Y; Ju, SH; Li, PC; Qian, C; Teng, GJ; Yang, XY; Yao, HH, 2015
)
2.21
"Treatment with cystamine and garlic extract reduced the liver fibrosis and collagen deposition, particularly in the garlic extract group (p<0.01)."( Garlic extract prevents CCl(4)-induced liver fibrosis in rats: The role of tissue transglutaminase.
Amoruso, DC; Caporaso, N; D'Argenio, G; D'Armiento, MR; Fogliano, V; Mazzone, G; Mezza, E; Morisco, F; Ribecco, MT; Romano, A; Vitaglione, P, 2010
)
0.7
"The treatment of cystamine, a transglutaminase(TGase) inhibitor, has beneficial effects in several diseases including CAG-expansion disorders and cataract. "( Different inhibition characteristics of intracellular transglutaminase activity by cystamine and cysteamine.
Cho, SY; Jang, GY; Jeon, JH; Kim, CW; Kim, IG; Lee, HJ; Park, SC; Shim, DM; Yeo, EJ, 2004
)
0.89
"Pretreatment with cystamine, but not Methylene Blue, significantly reduced the maximum Isc and the cGMP release induced by L-arginine methyl ester and the nitric oxide donor sodium nitroprusside, implicating the involvement of particulate guanylate cyclase."( Nitric oxide stimulates cyclic guanosine monophosphate production and electrogenic secretion in Caco-2 colonocytes.
Milla, PJ; Rolfe, VE, 1999
)
0.63
"Treatment with cystamine, phlorrhizin or nicotinic acid, which induced liver glycogenolysis, resulted in the increase of liver lactate dehydrogenase activity. "( Changes in the liver lactate dehydrogenase isozyme profile after induced glycogenolysis.
Benito, M; García-Bueno, M; Medina, JM; Moreno, FJ, 1978
)
0.61
"Treatment with cystamine prior to DMN administration completely abolished the depression of protein synthesis and reduced by more than 90% the methylation by [14C]DMN of purine bases in liver DNA."( Dimethylnitrosamine-induced inhibition of hepatic protein synthesis in vitro and the effect of pretreatment with cystamine or pregnenolone-16alpha-carbonitrile.
Kleihues, P; Margison, GP; Margison, JM, 1975
)
0.8
"The treatment with cystamine, cysteamine and riboxine prior to irradiation (< 2 Gy) did not influence the postirradiation values of the parameters under study."( [An experimental approach to determining the protective properties of drugs against ionizing radiation in low and sublethal doses].
Chertkov, KS; Chotiĭ, VG; Glushkov, VA; Maliutina, TS; Sbitneva, MF; Vernigorova, LA,
)
0.45

Toxicity

ExcerptReferenceRelevance
"The disulfide metabolites of thiono-sulfur drugs were found to be about 50 to 100 times more toxic to isolated rat hepatocytes than the corresponding parent drugs."( The toxicity of disulphides to isolated hepatocytes and mitochondria.
Jatoe, SD; Lauriault, V; McGirr, LG; O'Brien, PJ, 1988
)
0.27
"It has been shown that unithiol diminishes toxic action of cysteamine, AET, and disulfide of WR-1065 on mice."( [Decrease of toxic effects of aminothiol radiation-protective agents and increase of chemical protection action against ionizing radiation by the use of unithiol].
Bol'shakova, OI; Grachev, SA; Korolva, IK; Nikanorova, NG; Sverdlov, AG,
)
0.13
"In experiments with dogs it was shown that administration of unithiol before administration of cystamine decreases toxic effect of the last: period of excitation induced by cystamine is shortened, the time of emetic reaction decreases and expression of the emetic reaction to this preparation is diminished, the recorded EKG changes of conditions of heart decrease."( [Effect of unithiol on cystamine toxicity in dogs].
Grachev, SA; Nikanorova, NG; Sverdlov, AG; Timoshenko, SI,
)
0.66
" Our findings suggest that this toxic model is not reflective or predictive of findings in genetic mouse models, and may not be useful as a preclinical screen for HD therapeutics."( Cystamine and ethyl-eicosapentaenoic acid treatment fail to prevent malonate-induced striatal toxicity in mice.
Leavitt, BR; Sivananthan, SN, 2011
)
1.81

Pharmacokinetics

ExcerptReferenceRelevance
" Half-life period of thioridazine was found to be reduced and its level in the brain tissue was diminished in the irradiated, cystamine-pretreated animals in comparison with the irradiated, untreated ones."( Changes in pharmacodynamics and pharmacokinetics of psycholeptic drugs in the course of radiation disease. Effects of premedication with cystamine on dynamics and kinetics of thioridazine.
Cenajek, D; Chodera, A; Kozaryn, I; Szczawińska, K; Wójciak, Z,
)
0.54
" Pharmacokinetic parameters were calculated by using a two-compartment model."( Pharmacokinetics and tissue retention of (Gd-DTPA)-cystamine copolymers, a biodegradable macromolecular magnetic resonance imaging contrast agent.
Feng, Y; Ke, T; Lu, ZR; Schabel, M; Wang, X, 2005
)
0.58

Dosage Studied

ExcerptRelevanceReference
" The second approach was a detailed comparison between alpha 2-receptor occupancy by [3H] UK 14304 and the cyclic AMP inhibitory dose-response curve to this agonist in cells incubated also under conditions avoiding cyclic AMP breakdown."( Evidence against the "spare" receptor nature of alpha 2-adrenoceptors in hamster white fat cells.
Dieudonne, MN; Giudicelli, Y; Pecquery, R, 1990
)
0.28
" Benextramine (3, 6 and 12 mg/Kg) displaced the dose-response curve to methoxamine to the right."( Benextramine and nifedipine distinguish between sub-classes of alpha 1-adrenoceptors.
Tabrizchi, R; Triggle, CR, 1989
)
0.28
" In the presence of Ang II, the NE dose-response curve shifted to the left twofold and the maximal response was not changed."( Angiotensin II amplification of alpha-adrenergic vasoconstriction: role of receptor reserve.
Purdy, RE; Weber, MA, 1988
)
0.27
" Isolated aortic rings were mounted in tissue baths for the measurement of isometric contraction and 5-HT dose-response curves were obtained in the presence and absence of receptor antagonists."( Receptors for 5-hydroxytryptamine in rabbit blood vessels: activation of alpha adrenoceptors in rabbit thoracic aorta.
Murray, DL; Purdy, RE; Stupecky, GL, 1987
)
0.27
" The dose-response curve to intra-arterial noradrenaline (after beta-adrenoceptor blockade) was shifted rightwards about ten fold by benextramine (10 mg kg-1) and by phenoxybenzamine (5 mg kg-1)."( Lack of involvement of alpha-adrenoceptors in sympathetic neural vasoconstriction in the hindquarters of the rabbit.
Hirst, GD; Lew, MJ, 1987
)
0.27
" In rabbit isolated saphenous vein, cumulative dose-response curves to various NPY agonists were obtained."( Discrimination by benextramine between the NPY-Y1 receptor subtypes present in rabbit isolated vas deferens and saphenous vein.
Corsi, M; Palea, S; Rimland, JM; Trist, DG, 1995
)
0.29
" Next, we determined norepinephrine dose-response relations before and after prazosin, yohimbine, and benextramine."( Effects of maturation on alpha-adrenergic receptor affinity and occupancy in small cerebral arteries.
Elliott, SR; Pearce, WJ, 1994
)
0.29
" Furthermore, NPY was without effect on the dose-response curve to ATP in resting conditions."( Failure of the putative neuropeptide Y antagonists, benextramine and PYX-2, to inhibit Y2 receptors in rat isolated prostatic vas deferens.
Corsi, M; Palea, S; Ratti, E; Rimland, JM; Trist, DG, 1995
)
0.29
" The competitive alpha1-adrenoceptor antagonists produced dextral shifts of the dose-response curves to NA in longitudinal and circular muscle."( Discrimination by SZL49 between contractions evoked by noradrenaline in longitudinal and circular muscle of human vas deferens.
Amobi, NI; Guillebaud, J; Kaisary, AV; Smith, IC; Turner, E, 2002
)
0.31
" However, cysteamine is associated with an offending odor and taste and this, coupled to a rapid first pass metabolism and a 6h dosing regimen, suggest a clear need to improve the therapy."( PEGylated derivatives of cystamine as enhanced treatments for nephropathic cystinosis.
Cairns, D; Di Salvo, A; Kay, G; Knott, RM; Omran, Z, 2011
)
0.67
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
EC 2.3.2.13 (protein-glutamine gamma-glutamyltransferase) inhibitorAn EC 2.3.2.* (aminoacyltransferase) inhibitor that interferes with the action of protein-glutamine gamma-glutamyltransferase (EC 2.3.2.13).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
organic disulfideCompounds of structure RSSR in which R and R' are organic groups.
primary amino compoundA compound formally derived from ammonia by replacing one hydrogen atom by an organyl group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency11.38940.100020.879379.4328AID488772; AID488773; AID588453; AID588456
GLS proteinHomo sapiens (human)Potency5.62340.35487.935539.8107AID624146
ThrombopoietinHomo sapiens (human)Potency31.62280.02517.304831.6228AID917; AID918
thyroid stimulating hormone receptorHomo sapiens (human)Potency6.30960.001318.074339.8107AID926; AID938
regulator of G-protein signaling 4Homo sapiens (human)Potency5.97280.531815.435837.6858AID504845
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency22.38720.035520.977089.1251AID504332
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency25.11890.354828.065989.1251AID504847
chromobox protein homolog 1Homo sapiens (human)Potency50.11870.006026.168889.1251AID488953
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.03550.00106.000935.4813AID943
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (30)

Assay IDTitleYearJournalArticle
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID45884Antiviral activity against HIV-1 in CEM-SS cells using XXT assay1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Zinc ejection as a new rationale for the use of cystamine and related disulfide-containing antiviral agents in the treatment of AIDS.
AID161899Compound was tested for effects on HIV-1 protease; NI = No inhibition1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Zinc ejection as a new rationale for the use of cystamine and related disulfide-containing antiviral agents in the treatment of AIDS.
AID695877Cytotoxicity against human KB-3-1 cells incubated for 72 hrs by MTT assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Collateral sensitivity of multidrug-resistant cells to the orphan drug tiopronin.
AID695851Resistance index, ratio of IC50 for human KB-3-1 cells to IC50 for drug-resistant human KBV1 cells expressing P-gp2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Collateral sensitivity of multidrug-resistant cells to the orphan drug tiopronin.
AID317096Inhibition of mouse neuroblast cell migration from subventricular zone tissue explants at 223 uM after 48 hrs relative to control2008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Discovery of new small molecules that influence neuroblast cell migration from the subventricular zone.
AID89002Compound was tested for binding of HIV-1 to CEM-ss cells; NI = No inhibition1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Zinc ejection as a new rationale for the use of cystamine and related disulfide-containing antiviral agents in the treatment of AIDS.
AID200145Compound was tested for the effect on HIV-1 Reverse Transcriptase; NI = No inhibition1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Zinc ejection as a new rationale for the use of cystamine and related disulfide-containing antiviral agents in the treatment of AIDS.
AID695876Cytotoxicity against drug-resistant human KBV1 cells expressing P-gp incubated for 72 hrs by MTT assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Collateral sensitivity of multidrug-resistant cells to the orphan drug tiopronin.
AID45374Antiviral activity against HIV-1 in CEM-SS cells using XXT assay1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Zinc ejection as a new rationale for the use of cystamine and related disulfide-containing antiviral agents in the treatment of AIDS.
AID45885Antiviral activity against HIV-1ADA in CEM-SS cells using monocyte/macrophage cultures1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Zinc ejection as a new rationale for the use of cystamine and related disulfide-containing antiviral agents in the treatment of AIDS.
AID45376Antiviral activity against HIV-1ADA in CEM-SS cells using monocyte/macrophage cultures1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Zinc ejection as a new rationale for the use of cystamine and related disulfide-containing antiviral agents in the treatment of AIDS.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,046)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990574 (54.88)18.7374
1990's138 (13.19)18.2507
2000's137 (13.10)29.6817
2010's163 (15.58)24.3611
2020's34 (3.25)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 51.10

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index51.10 (24.57)
Research Supply Index7.17 (2.92)
Research Growth Index4.43 (4.65)
Search Engine Demand Index85.78 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (51.10)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (0.31%)5.53%
Reviews30 (2.32%)6.00%
Case Studies5 (0.39%)4.05%
Observational0 (0.00%)0.25%
Other1,255 (96.99%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]