Capillary bioreactors based on human purine nucleoside phosphorylase: A new approach for ligands identification and characterization

Moraes, Marcela Cristina de; Ducati, Rodrigo G.; Donato, Augusto José; Basso, Luiz Augusto; Santos, Daniel Silas Veras dos; Cardoso, Carmen L.; Cass, Quézia B.

doi:10.1016/j.chroma.2011.10.056

Cited by 23 publications

(12 citation statements)

References 39 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Because XO inhibitors can affect the purine pathway, and because selectivity plays a crucial role in selecting enzyme inhibitors, the three most XO-ICER-active ruthenium complexes were also evaluated with the HsPNP-ICER. 12 With the HsPNP-ICER, compound BCX-762 was used as a reference inhibitor. 14 The results demonstrated a high selectivity index of the tested complexes towards XO ( Figure 6).…”

Section: Screening Assaymentioning

confidence: 99%

Characterization and screening of tight binding inhibitors of xanthine oxidase: an on-flow assay

et al. 2015

View full text Add to dashboard Cite

show abstract

Section: Screening Assaymentioning

confidence: 99%

Characterization and screening of tight binding inhibitors of xanthine oxidase: an on-flow assay

et al. 2015

View full text Add to dashboard Cite

show abstract

“…The fourth-generation immucillin derivative DI4G ( Figure 1 ) is a potent transition-state analog inhibitor of human PNP (HsPNP). This compound has been described as competitive inhibitor of HsPNP with K i of 11.8 ± 1.47 nM regarding inosine substrate [ 22 ]. In addition, DI4G showed an IC 50 value of 40.6 ± 0.36 nM when evaluated at substrate concentrations near to the K M values for HsPNP [ 22 ].…”

Section: Introductionmentioning

confidence: 99%

In VitroImmunomodulatory Activity of a Transition-State Analog Inhibitor of Human Purine Nucleoside Phosphorylase in Cutaneous Leishmaniasis

Carvalho

Prates

Silva

et al. 2017

Journal of Immunology Research

Self Cite

View full text Add to dashboard Cite

Cutaneous leishmaniasis (CL) is the most common clinical form of American tegumentary leishmaniasis caused by Leishmania (Viannia) braziliensis. CL is associated with a strong Th1 immune response. This exacerbated inflammatory response is correlated with severity of disease and delays the healing time of the ulcer. The fourth-generation immucillin derivative (DI4G), a potent inhibitor of purine nucleoside phosphorylase, has been proposed as a promising agent in the treatment of diseases associated with T cell activation. Herein, we evaluated the in vitro immunomodulatory activity of DI4G in cells of patients presenting with CL. Peripheral blood mononuclear cells (PBMC) from CL patients were stimulated with soluble leishmania antigen (SLA), in the presence or absence of DI4G, and IFN-γ, TNF, CXCL9, and CXCL10 levels were determined by ELISA. Lymphocyte proliferation in the presence or absence of DI4G was also evaluated, using flow cytometry. DI4G was able to decrease (p < 0 05) IFN-γ production but did not change the TNF, CXCL9, and CXCL10 levels. DI4G decreased (p < 0 05) the lymphoproliferative response mediated by CD8 + T cells, but not that by CD4 + T cells. DI4G is able to attenuate the exaggerated immune response in CL, exhibiting immunomodulatory activity in IFN-γ production and in CD8 + T cell proliferation.

show abstract

“…As a result, the chromatography-based bioassays have been exploited as a promising approach for the identification of novel active compounds [4–7]. Once a compound is identified with this approach, the compound can be fully characterized including its affinity for the targeted protein [8, 9]. Several recent reviews [2, 4, 9] have discussed in great detail the variety of supports and method of immobilization.…”

Section: Introductionmentioning

confidence: 99%

“…The bioaffinity columns for these assays are usually prepared by in-situ immobilization in capillary columns (100 µm × 0.5 mm) packed with porous spherical silica [12, 13]. Zonal chromatography has also been used in screening inhibitors for immobilized enzyme reactors (IMERs) [4, 8, 14–17]. In these studies, inhibition of enzymatic activity can be studied by measuring changes in product formation.…”

Section: Introductionmentioning

confidence: 99%

Targeting Anti-Cancer Active Compounds: Affinity-Based Chromatographic Assays

Moraes¹,

Cardoso²,

Seidl³

et al. 2016

CPD

View full text Add to dashboard Cite

Affinity-based chromatography assays encompass the use of solid supports containing immobilized biological targets to monitor binding events in the isolation , identification and/or characterization of bioactive compounds. This powerful bioanalytical technique allows the screening of potential binders through fast analyses that can be directly performed using isolated substances or complex matrices. An overview of the recent researches in frontal and zonal affinity-based chromatography screening assays, which has been used as a tool in the identification and characterization of new anti-cancer agents, is discussed. In addition, a critical evaluation of the recently emerged ligands fishing assays in complex mixtures is also discussed.

show abstract

Capillary bioreactors based on human purine nucleoside phosphorylase: A new approach for ligands identification and characterization

Cited by 23 publications

References 39 publications

Characterization and screening of tight binding inhibitors of xanthine oxidase: an on-flow assay

Characterization and screening of tight binding inhibitors of xanthine oxidase: an on-flow assay

In VitroImmunomodulatory Activity of a Transition-State Analog Inhibitor of Human Purine Nucleoside Phosphorylase in Cutaneous Leishmaniasis

Targeting Anti-Cancer Active Compounds: Affinity-Based Chromatographic Assays

Contact Info

Product

Resources

About