Page last updated: 2024-10-15

forodesine

Description

forodesine: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID135409409
CHEMBL ID218291
CHEBI ID43362
SCHEMBL ID16321929
SCHEMBL ID506383
MeSH IDM0292232

Synonyms (67)

Synonym
209799-67-7
immucillin-h
D06596
forodesine (usan/inn)
fodosine (tn)
IMH ,
1,4-dideoxy-4-aza-1-(s)-(9-deazahypoxanthin-9-yl)-d-ribitol
bcx-1777
fodosine
1NW4
2FF2
2FF1
1B8O
1G2O
nsc-717904
immucillin h
(1s)-1,4-dideoxy-4-imino-(9-deazahypoxanthin-9-yl)-d-ribitol
CHEBI:43362 ,
forodesine
7-[(2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl]-1,5-dihydro-4h-pyrrolo[3,2-d]pyrimidin-4-one
7-((2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl)-3h-pyrrolo[3,2-d]pyrimidin-4(5h)-one
bdbm50195587
7-[(2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl]-1,5-dihydropyrrolo[3,2-d]pyrimidin-4-one
CHEMBL218291 ,
1-(9-deazahypoxanthin-9-yl)-1,4-dideoxy-1,4-iminoribitol
bcx 1777
nsc 717904
forodesine [usan:inn]
immh cpd
426x066elk ,
(-)-7-((2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl)-1,5-dihydro-4h-pyrrolo(3,2-d)pyrimidin-4-one
bcx1777
unii-426x066elk
4h-pyrrolo(3,2-d)pyrimidin-4-one, 7-((2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)-2-pyrrolidinyl)-1,5-dihydro-
forodesine [inn]
(-)-7-[(2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl]-1,5-dihydro-4h-pyrrolo[3,2-d]pyrimidin-4-one
forodesine [usan]
mundesine
forodesine [mi]
forodesine [who-dd]
IWKXDMQDITUYRK-KUBHLMPHSA-N
CS-3781
SCHEMBL16321929
SCHEMBL506383
7-[(2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl]-1,5-dihydropyrrolo[2,3-e]pyrimidin-4-one
gtpl8272
fodosine (proposed trade name)
HY-16210
5(s),12(s)-dihete
(2r,3r,4s,5s)-2-(hydroxymethyl)-5-(4-hydroxy-5h-pyrrolo[3,2-d]pyrimidin-7-yl)pyrrolidine-3,4-diol
AKOS027326672
mfcd09837827
NCGC00485883-01
forodesine; immucillin h
7-[(2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl]-3,5-dihydro-4h-pyrrolo[3,2-d]pyrimidin-4-one
7-[(2s,3s,4r,5r)-3,4-dihydroxy-5-hydroxymethyl-2-pyrrolidinyl]-1,5-dihydro-4h-pyrrolo-[3,2-d]-pyrimidin-4-one
Q410040
TXFGPFIDYBMMJY-KUBHLMPHSA-N
(1s)-1,4-dideoxy-1-c-(4-hydroxypyrrolo[3,2-d]pyrimidin-7-yl)-1,4-imino-d-ribitol
DB06185
AS-35282
DTXSID50943276
7-((2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl)-3,5-dihydro-4h-pyrrolo[3,2-d]pyrimidin-4-one
7-[(2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl]-3,5-dihydropyrrolo[3,2-d]pyrimidin-4-one
4h-pyrrolo[3,2-d]pyrimidin-4-one, 7-[(2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)-2-pyrrolidinyl]-3,5-dihydro-
AKOS040741759
EX-A7842M

Research Excerpts

Overview

Forodesine is a purine nucleoside phosphorylase (PNP) inhibitor and it has shown activity in relapsed and refractory T- and B-cells leukemias as well as in cutaneous T-cell lymphoma (CTCL) Forodesine leads to intracellular accumulation of deoxyguanosine triphosphate (dGTP) resulting in apoptosis.

ExcerptReference
"Forodesine is a transition-state analogue that inhibits purine nucleoside phosphorylase."( Forodesine in the treatment of cutaneous T-cell lymphoma.
Duvic, M; Lewis, DJ, 2017
)
"Forodesine is an orally bioavailable PNP inhibitor with picomolar potency."( Preclinical and clinical evaluation of forodesine in pediatric and adult B-cell acute lymphoblastic leukemia.
Balakrishnan, K; Bantia, S; Franklin, A; Gandhi, V; Ravandi, F, 2013
)
"Forodesine is a potent inhibitor of purine nucleoside phosphorylase (PNP) that leads to intracellular accumulation of deoxyguanosine triphosphate (dGTP) in T and B cells, resulting in apoptosis. "( Final results of a multicenter phase II study of the purine nucleoside phosphorylase (PNP) inhibitor forodesine in patients with advanced cutaneous T-cell lymphomas (CTCL) (Mycosis fungoides and Sézary syndrome).
Dummer, R; Duvic, M; Eggmann, N; Elder, J; Geskin, L; Giuliano, E; Goldinger, SM; Hutchinson, K; Illidge, TM; Kim, YH; Olsen, EA; Rozati, S; Scarisbrick, J, 2014
)
"Forodesine is a purine nucleoside phosphorylase (PNP) inhibitor and it has shown activity in relapsed and refractory T- and B-cells leukemias as well as in cutaneous T-cell lymphoma (CTCL)."( Novel purine nucleoside analogues for hematological malignancies.
Korycka, A; Lech-Marańda, E; Robak, T, 2008
)
"Forodesine is a transition-state inhibitor of the purine nucleoside phosphorylase with antileukemic activity."( Forodesine has high antitumor activity in chronic lymphocytic leukemia and activates p53-independent mitochondrial apoptosis by induction of p73 and BIM.
Alonso, R; Bantia, S; Bontemps, F; Campo, E; Colomer, D; López-Guerra, M; Manz, C; Mehrling, T; Montserrat, E; Smal, C; Upshaw, R; Villamor, N, 2009
)
"Forodesine is a new and potent purine nucleoside phosphorylase (PNP) inhibitor. "( Phase 2 and pharmacodynamic study of oral forodesine in patients with advanced, fludarabine-treated chronic lymphocytic leukemia.
Balakrishnan, K; Bantia, S; Bickel, S; Chen, Y; Gandhi, V; Kantarjian, H; Keating, MJ; Kilpatrick, JM; O'Brien, S; Ravandi, F; Tyler, BF; Verma, D, 2010
)
"Forodesine is a potent PNP inhibitor that acts by elevating plasma 2'-deoxyguanosine (dGuo) and intracellular deoxyguanosine triphosphate, which in turn affects deoxynucleotide-triphosphate pools and induces cell death by apoptosis."( Drug evaluation: forodesine - PNP inhibitor for the treatment of leukemia, lymphoma and solid tumor.
Galmarini, CM, 2006
)
"Forodesine is a highly potent, orally active, rationally designed PNP inhibitor that has shown activity in preclinical studies with malignant cells and clinical utility against T-cell acute lymphoblastic leukemia and cutaneous T-cell lymphoma."( Purine nucleoside phosphorylase inhibition as a novel therapeutic approach for B-cell lymphoid malignancies.
Furman, RR; Hoelzer, D, 2007
)

Pharmacokinetics

Forodesine has biologic activity in CLL. An alternate dosing schedule and/or higher doses to achieve greater intracellular dGTP may be beneficial in this patient population.

ExcerptReference
" This was the first clinical study in humans to demonstrate the plasma pharmacokinetics and the pharmacodynamic effectiveness of the PNP inhibitor, forodesine; however, regrowth of leukemia cells in the blood and marrow after course 1 suggested that a different therapeutic schedule should be considered for future studies."( A proof-of-principle pharmacokinetic, pharmacodynamic, and clinical study with purine nucleoside phosphorylase inhibitor immucillin-H (BCX-1777, forodesine).
Ayres, M; Bantia, S; Davisson, J; Du, M; Faderl, S; Gandhi, V; Harman, L; Kantarjian, H; Kilpatrick, JM; Plunkett, W; Thomas, D; Wierda, WG, 2005
)
" Forodesine has biologic activity in CLL; pharmacodynamic parameters suggest that an alternate dosing schedule and/or higher doses to achieve greater intracellular dGTP may be beneficial in this patient population."( Phase 2 and pharmacodynamic study of oral forodesine in patients with advanced, fludarabine-treated chronic lymphocytic leukemia.
Balakrishnan, K; Bantia, S; Bickel, S; Chen, Y; Gandhi, V; Kantarjian, H; Keating, MJ; Kilpatrick, JM; O'Brien, S; Ravandi, F; Tyler, BF; Verma, D, 2010
)

Bioavailability

ExcerptReference
" BCX-1777 has excellent oral bioavailability (63%) in mice."( Purine nucleoside phosphorylase inhibitor BCX-1777 (Immucillin-H)--a novel potent and orally active immunosuppressive agent.
Ananth, SL; Bantia, S; Horn, LL; Hutchison, TL; Kilpatrick, JM; Miller, PJ; Montgomery, JA; Morris, PE; Parker, CD; Sandhu, JS, 2001
)
" Forodesine is an orally bioavailable PNP inhibitor with picomolar potency."( Preclinical and clinical evaluation of forodesine in pediatric and adult B-cell acute lymphoblastic leukemia.
Balakrishnan, K; Bantia, S; Franklin, A; Gandhi, V; Ravandi, F, 2013
)
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)

Dosage Studied

ExcerptReference
" Forodesine has biologic activity in CLL; pharmacodynamic parameters suggest that an alternate dosing schedule and/or higher doses to achieve greater intracellular dGTP may be beneficial in this patient population."( Phase 2 and pharmacodynamic study of oral forodesine in patients with advanced, fludarabine-treated chronic lymphocytic leukemia.
Balakrishnan, K; Bantia, S; Bickel, S; Chen, Y; Gandhi, V; Kantarjian, H; Keating, MJ; Kilpatrick, JM; O'Brien, S; Ravandi, F; Tyler, BF; Verma, D, 2010
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
pyrrolopyrimidine
dihydroxypyrrolidine
[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 (14)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, PURINE NUCLEOSIDE PHOSPHORYLASEBos taurus (cattle)Ki0.00000.00000.00000.0000AID977610
Chain A, PURINE NUCLEOSIDE PHOSPHORYLASEMycobacterium tuberculosisKi0.00000.00000.00000.0000AID977610
Chain B, PURINE NUCLEOSIDE PHOSPHORYLASEMycobacterium tuberculosisKi0.00000.00000.00000.0000AID977610
Chain A, IAG-nucleoside hydrolaseTrypanosoma vivaxKi0.00620.00620.00620.0062AID977610
Chain A, IAG-nucleoside hydrolaseTrypanosoma vivaxKi0.00620.00620.00620.0062AID977610
Purine nucleoside phosphorylaseHomo sapiens (human)IC50 (µMol)0.05180.00351.49875.0000AID272823; AID424677
Purine nucleoside phosphorylaseHomo sapiens (human)Ki0.00830.00000.52897.0000AID1571176; AID1578784; AID164744; AID164928; AID164930; AID164938; AID272823; AID371442; AID409913; AID409914; AID410191
Purine nucleoside phosphorylaseMus musculus (house mouse)Ki0.00000.00000.00000.0000AID164739
Purine nucleoside phosphorylase Bos taurus (cattle)Ki0.00000.00000.53072.7000AID1571175; AID164739
Purine nucleoside phosphorylasePlasmodium falciparum (malaria parasite P. falciparum)Ki0.01020.00050.00540.0290AID1578781; AID1578782; AID536622
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, uridine phosphorylase, putativePlasmodium falciparum 3D7Kd0.00090.00090.00090.0009AID977611
Chain B, uridine phosphorylase, putativePlasmodium falciparum 3D7Kd0.00090.00090.00090.0009AID977611
Chain A, Uridine phosphorylase putativePlasmodium falciparum 3D7Kd0.00090.00090.00090.0009AID977611
Chain B, Uridine phosphorylase putativePlasmodium falciparum 3D7Kd0.00090.00090.00090.0009AID977611
Chain A, Purine nucleoside phosphorylaseHomo sapiens (human)Kd0.00090.00090.00090.0009AID977611
Purine nucleoside phosphorylaseHomo sapiens (human)Kd0.00010.00010.00010.0001AID536621
Purine nucleoside phosphorylase Bos taurus (cattle)Kd0.00000.00000.66673.3000AID694066
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Purine nucleoside phosphorylase Bos taurus (cattle)Kieq0.00000.00003.47507.4000AID694063
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (17)

Processvia Protein(s)Taxonomy
inosine catabolic processPurine nucleoside phosphorylaseHomo sapiens (human)
urate biosynthetic processPurine nucleoside phosphorylaseHomo sapiens (human)
positive regulation of T cell proliferationPurine nucleoside phosphorylaseHomo sapiens (human)
positive regulation of alpha-beta T cell differentiationPurine nucleoside phosphorylaseHomo sapiens (human)
allantoin metabolic processPurine nucleoside phosphorylaseHomo sapiens (human)
nucleobase-containing compound metabolic processPurine nucleoside phosphorylaseHomo sapiens (human)
inosine catabolic processPurine nucleoside phosphorylaseHomo sapiens (human)
deoxyinosine catabolic processPurine nucleoside phosphorylaseHomo sapiens (human)
deoxyadenosine catabolic processPurine nucleoside phosphorylaseHomo sapiens (human)
purine ribonucleoside salvagePurine nucleoside phosphorylaseHomo sapiens (human)
IMP catabolic processPurine nucleoside phosphorylaseHomo sapiens (human)
nicotinamide riboside catabolic processPurine nucleoside phosphorylaseHomo sapiens (human)
immune responsePurine nucleoside phosphorylaseHomo sapiens (human)
nucleotide biosynthetic processPurine nucleoside phosphorylaseHomo sapiens (human)
response to xenobiotic stimulusPurine nucleoside phosphorylaseHomo sapiens (human)
positive regulation of interleukin-2 productionPurine nucleoside phosphorylaseHomo sapiens (human)
purine-containing compound salvagePurine nucleoside phosphorylaseHomo sapiens (human)
dAMP catabolic processPurine nucleoside phosphorylaseHomo sapiens (human)
purine ribonucleoside salvagePurine nucleoside phosphorylase Bos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
nucleoside bindingPurine nucleoside phosphorylaseHomo sapiens (human)
purine nucleobase bindingPurine nucleoside phosphorylaseHomo sapiens (human)
purine-nucleoside phosphorylase activityPurine nucleoside phosphorylaseHomo sapiens (human)
protein bindingPurine nucleoside phosphorylaseHomo sapiens (human)
phosphate ion bindingPurine nucleoside phosphorylaseHomo sapiens (human)
identical protein bindingPurine nucleoside phosphorylaseHomo sapiens (human)
guanosine phosphorylase activityPurine nucleoside phosphorylaseHomo sapiens (human)
purine-nucleoside phosphorylase activityPurine nucleoside phosphorylase Bos taurus (cattle)
guanosine phosphorylase activityPurine nucleoside phosphorylase Bos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
extracellular regionPurine nucleoside phosphorylaseHomo sapiens (human)
cytoplasmPurine nucleoside phosphorylaseHomo sapiens (human)
cytosolPurine nucleoside phosphorylaseHomo sapiens (human)
secretory granule lumenPurine nucleoside phosphorylaseHomo sapiens (human)
extracellular exosomePurine nucleoside phosphorylaseHomo sapiens (human)
ficolin-1-rich granule lumenPurine nucleoside phosphorylaseHomo sapiens (human)
cytoplasmPurine nucleoside phosphorylaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (61)

Assay IDTitleYearJournalArticle
AID1578787Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes assessed as reduction in [3H]ethanolamine incorporation incubated for 18 hrs followed by addition of [3H]ethanolamine and measured after 48 hrs by scintillation countin2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues.
AID409913Initial binding affinity to wild type human PNP2008Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
Immucillins in custom catalytic-site cavities.
AID272825Inhibition of DNA synthesis in CCRF-CEM cells assessed as inhibition of [3H]Thymidine incorporation upto 100 nM2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Simplified analogues of immucillin-G retain potent human purine nucleoside phosphorylase inhibitory activity.
AID536621Inhibition of human PNP2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Exploring new inhibitors of Plasmodium falciparum purine nucleoside phosphorylase.
AID409921Ratio of relative binding Km/Ki for wild type human PNP to relative binding affinity Km/Ki for human PNP His257Gly mutant2008Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
Immucillins in custom catalytic-site cavities.
AID272833Antiproliferative activity against CCRF-CEM cells2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Simplified analogues of immucillin-G retain potent human purine nucleoside phosphorylase inhibitory activity.
AID462377Inhibition of calf spleen PNP assessed as inhibition of 7-methylguanosine phosphorolysis after 50 mins by spectrophotometry in presence of 50 mM inorganic phosphate2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Structural-based design and synthesis of novel 9-deazaguanine derivatives having a phosphate mimic as multi-substrate analogue inhibitors for mammalian PNPs.
AID409920Ratio of Km for human PNP His257Gly mutant to Ki for human PNP His257Gly mutant relative to inosine2008Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
Immucillins in custom catalytic-site cavities.
AID523342Antiparasitic activity against chloroquine-sensitive Plasmodium falciparum Ghana assessed as reduction in parasite growth after 3 days by fluorimetry2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis.
AID523341Antileishmanial activity against Leishmania infantum MHOM/MA/67/ITMAP263 intracellular amastigotes assessed as reduction in parasite growth after 3 days by fluorometrically2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis.
AID523340Antitrypanosomal activity against Trypanosoma cruzi Tulahuen CL2 s-galactosidase strain assessed as reduction in parasite growth after 3 days by fluorometrically2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis.
AID164739Inhibitory activity of compound against bovine purine nucleoside phosphorylase (PNP)2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases.
AID164742Dissociation constant against Human Purine Nucleoside Phosphorylase was reported2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Synthesis of second-generation transition state analogues of human purine nucleoside phosphorylase.
AID1571176Inhibition of human PNP using inosine as substrate by xanthine oxidase coupled assay2018MedChemComm, Dec-01, Volume: 9, Issue:12
The transition to magic bullets - transition state analogue drug design.
AID164938Inhibitory activity of compound against human purine nucleoside phosphorylase (PNP)2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Targeting the polyamine pathway with transition-state analogue inhibitors of 5'-methylthioadenosine phosphorylase.
AID1571177Inhibition of bovine spleen PNP assessed as dissociation half life using inosine as substrate by xanthine oxidase coupled assay2018MedChemComm, Dec-01, Volume: 9, Issue:12
The transition to magic bullets - transition state analogue drug design.
AID409914Equilibrium binding affinity to wild type human PNP2008Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
Immucillins in custom catalytic-site cavities.
AID409916Ratio of Km for wild type human PNP to Ki for wild type human PNP relative to inosine2008Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
Immucillins in custom catalytic-site cavities.
AID272824Inhibition of human dCK activity2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Simplified analogues of immucillin-G retain potent human purine nucleoside phosphorylase inhibitory activity.
AID523326Inhibition of Trypanosoma brucei brucei Inosine guanosine nucleoside hydrolase2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis.
AID523324Inhibition of Trypanosoma vivax Inosine-adenosine-guanosine-nucleoside hydrolase2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis.
AID694066Binding affinity to calf recombinant PNP expressed in Escherichia coli BL21 (DE3) by isothermal titration calorimetry2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Trimeric purine nucleoside phosphorylase: exploring postulated one-third-of-the-sites binding in the transition state.
AID1578784Inhibition of human PNP assessed as inhibitor constant for enzyme-inhibitor-substrate complex formation2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues.
AID1578782Inhibition of Plasmodium falciparum His-tagged PNP assessed as inhibitor constant for enzyme-inhibitor-substrate complex formation2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues.
AID523328Antitrypanosomal activity against suramin sensitive Trypanosoma brucei brucei Lister 427 assessed as reduction in parasite growth after 3 days by fluorometrically2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis.
AID410191Initial binding affinity to human PNP His257Gly mutant2008Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
Immucillins in custom catalytic-site cavities.
AID1578783Inhibition of human PNP assessed as inhibitor constant for enzyme-inhibitor complex formation2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues.
AID1571178Oral bioavailability in mouse2018MedChemComm, Dec-01, Volume: 9, Issue:12
The transition to magic bullets - transition state analogue drug design.
AID164744Inhibitory activity of compound against human purine nucleoside phosphorylase (PNP)2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases.
AID272823Inhibition of human PNP activity2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Simplified analogues of immucillin-G retain potent human purine nucleoside phosphorylase inhibitory activity.
AID92759Inhibitory activity of compound against inosine-uridine nucleoside hydrolase (IU-NH) from crithidia fasciculata2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases.
AID92758Inhibitory activity of compound against perine-specific inosine-adenosine-guanosine nucleoside hydrolase (IAG-NH) from Trypanosoma brucei2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases.
AID164604Rate constant of compound was determined for interaction with bovine purine nucleoside phosphorylase (PNP)2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases.
AID1571175Inhibition of bovine spleen PNP using inosine as substrate by xanthine oxidase coupled assay2018MedChemComm, Dec-01, Volume: 9, Issue:12
The transition to magic bullets - transition state analogue drug design.
AID164930Equilibrium dissociation constant determined against human purine nucleoside phosphorylase (PNP) after slow-onset inhibition2003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
Exploring structure-activity relationships of transition state analogues of human purine nucleoside phosphorylase.
AID409918Equilibrium binding affinity to human PNP His257Gly mutant2008Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
Immucillins in custom catalytic-site cavities.
AID694063Inhibition of bovine PNP using 7-methylguanosine as substrate by spectrophotometric based coupled assay2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Trimeric purine nucleoside phosphorylase: exploring postulated one-third-of-the-sites binding in the transition state.
AID523327Inhibition of human purine nucleoside phosphorylase2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis.
AID523329Cytotoxicity against human MRC5 SV2 cells after 48 hrs2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis.
AID523325Inhibition of Trypanosoma brucei brucei inosine-adenosine-guanosine nucleoside hydrolase (IAG-NH)2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis.
AID1578781Inhibition of Plasmodium falciparum His-tagged PNP assessed as inhibitor constant for enzyme-inhibitor complex formation2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues.
AID164928Inhibition of human purine nucleoside phosphorylase; Initial rate.2003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
Exploring structure-activity relationships of transition state analogues of human purine nucleoside phosphorylase.
AID536622Inhibition of Plasmodium falciparum PNP expressed in Escherichia coli BL21(DE3) cells by spectrophotometry2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Exploring new inhibitors of Plasmodium falciparum purine nucleoside phosphorylase.
AID164740Rate constant of compound was determined for interaction with human purine nucleoside phosphorylase (PNP)2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases.
AID164741Binding affinity towards Human Purine Nucleoside Phosphorylase was reported2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Synthesis of second-generation transition state analogues of human purine nucleoside phosphorylase.
AID371442Inhibition of human PNP by xanthine-oxidase coupled assay2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Third-generation immucillins: syntheses and bioactivities of acyclic immucillin inhibitors of human purine nucleoside phosphorylase.
AID424677Inhibition of human purine nucleoside phosphorylase2009Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10
Synthesis of analogs of forodesine HCl, a human purine nucleoside phosphorylase inhibitor-Part II.
AID1811Experimentally measured binding affinity data derived from PDB2006Journal of molecular biology, Jun-02, Volume: 359, Issue:2
Transition-state complex of the purine-specific nucleoside hydrolase of T. vivax: enzyme conformational changes and implications for catalysis.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2006Journal of molecular biology, Jun-02, Volume: 359, Issue:2
Transition-state complex of the purine-specific nucleoside hydrolase of T. vivax: enzyme conformational changes and implications for catalysis.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings 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.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine 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.
AID1346173Human purine nucleoside phosphorylase (Nucleoside synthesis and metabolism)1998Biochemistry, Jun-16, Volume: 37, Issue:24
One-third-the-sites transition-state inhibitors for purine nucleoside phosphorylase.
AID1811Experimentally measured binding affinity data derived from PDB2001Biochemistry, Jul-27, Volume: 40, Issue:28
Structures of purine nucleoside phosphorylase from Mycobacterium tuberculosis in complexes with immucillin-H and its pieces.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2001Biochemistry, Jul-27, Volume: 40, Issue:28
Structures of purine nucleoside phosphorylase from Mycobacterium tuberculosis in complexes with immucillin-H and its pieces.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2001Biochemistry, Jan-30, Volume: 40, Issue:4
Transition state structure of purine nucleoside phosphorylase and principles of atomic motion in enzymatic catalysis.
AID1811Experimentally measured binding affinity data derived from PDB2001Biochemistry, Jan-30, Volume: 40, Issue:4
Transition state structure of purine nucleoside phosphorylase and principles of atomic motion in enzymatic catalysis.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2004The Journal of biological chemistry, Apr-30, Volume: 279, Issue:18
Plasmodium falciparum purine nucleoside phosphorylase: crystal structures, immucillin inhibitors, and dual catalytic function.
AID1811Experimentally measured binding affinity data derived from PDB2004The Journal of biological chemistry, Apr-30, Volume: 279, Issue:18
Plasmodium falciparum purine nucleoside phosphorylase: crystal structures, immucillin inhibitors, and dual catalytic function.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (108)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (2.78)18.2507
2000's65 (60.19)29.6817
2010's33 (30.56)24.3611
2020's7 (6.48)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (6.42%)5.53%
Reviews25 (22.94%)6.00%
Case Studies2 (1.83%)4.05%
Observational1 (0.92%)0.25%
Other74 (67.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]