The Determination of Enzyme Dissociation Constants

Lineweaver, Hans; Burk, Dean

doi:10.1021/ja01318a036

Cited by 11,875 publications

(4,013 citation statements)

References 1 publication

Supporting

Mentioning

3,886

Contrasting

Unclassified

Order By: Relevance

“…The kinetics of hNIS-mediated iodide uptake were examined in UVW ± hNIS cells, with V max and K m values obtained using the Lineweaver-Burk double reciprocal plot. 10 The K m value obtained in our system (35 M) is comparable to those values previously obtained for the rat thyroid FRTL -5 cell line, and other NIS -transfected nonthyroid cell lines. 5,8 The rates of both I À influx and efflux were established in UVW ± hNIS cells.…”

Section: Discussionsupporting

confidence: 87%

“…The initial velocity of iodide uptake was measured after 5 minutes incubation with 10 ±500 M NaI containing trace Na 125 I ( specific activity = 0.32± 16 cpm /pmol ) . K m and V max values were calculated using a LineweaverBurk plot 10 (Fig 3 ). The values obtained are similar to Ci / mL Na 125 I ( specific activity = 100 Ci / mol ) for 1 hour.…”

Section: Kinetics Of Iodide Uptake and Efflux In Uvw ± Hnis Cellsmentioning

confidence: 99%

See 1 more Smart Citation

Experimental targeted radioiodide therapy following transfection of the sodium iodide symporter gene: Effect on clonogenicity in both two-and three-dimensional models

et al. 2000

View full text Add to dashboard Cite

To evaluate the potential of the expression of the sodium / iodide symporter ( NIS ) as a means of targeting radioiodine to tumor cells, we have employed plasmid -mediated transfection of the NIS gene into a range of mammalian cell hosts. We observed perchlorate -inhibitable iodide uptake up to 41 -fold over control in all NIS -transfected cells. We assessed the effect of NIS expression followed by exposure to 131 I À on the clonogenic survival of UVW glioma cells. After exposure of two -dimensional monolayer cultures of UVW ± NIS cells to 131 I À at a radioactive concentration of 4 MBq / mL, clonogenic survival was reduced to 21%. Similar treatment of UVW ± NIS cells in three -dimensional spheroid cultures resulted in a reduction of clonogenic survival to 2.5%. This increase in sensitivity to 131 I À exposure is likely to be due to a radiological bystander effect. These results are very encouraging for the development of a novel cytotoxic gene -therapy strategy in which a radiological bystander effect plays a significant role in tumor cell sterilization. Cancer Gene Therapy ( 2000 ) 7, 1529 ± 1536

show abstract

Section: Discussionsupporting

confidence: 87%

Section: Kinetics Of Iodide Uptake and Efflux In Uvw ± Hnis Cellsmentioning

confidence: 99%

Experimental targeted radioiodide therapy following transfection of the sodium iodide symporter gene: Effect on clonogenicity in both two-and three-dimensional models

et al. 2000

View full text Add to dashboard Cite

show abstract

“…This suggests that 2 is functioning as a noncompetitive inhibitor LIMK2, rather than an uncompetitive (lines never intersect), competitive (lines intersect on the Y-axis), or mixed inhibitor (lines intersect somewhere in between the X-and Yaxes). 23,24 The excitement over this chemical series of selective, allosteric inhibitors prompted a rapid expansion of the SARs to increase the potency at LIMK2. The synthetic strategy, outlined in Scheme 1, was straightforward.…”

mentioning

confidence: 99%

Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation

Goodwin

Cianchetta

Burgoon

et al. 2014

ACS Med. Chem. Lett.

View full text Add to dashboard Cite

The first allosteric, type III inhibitor of LIM-kinase 2 (LIMK2) is reported. A series of molecules that feature both an N-phenylsulfonamide and tertiary amide were not only very potent at LIMK2 but also were extremely selective against a panel of other kinases. Enzymatic kinetic studies showed these molecules to be noncompetitive with ATP, suggesting allosteric inhibition. X-ray crystallography confirmed that these sulfonamides are a rare example of a type III kinase inhibitor that binds away from the highly conserved hinge region and instead resides in the hydrophobic pocket formed in the DFG-out conformation of the kinase, thus accounting for the high level of selectivity observed.

show abstract

“…The results are listed in table 1. The kinetic parameters of the exchange reactions for fluorotryptophans acting as substrates were evaluated from Lineweaver-Burk plots [16] (fig. 1).…”

Section: Resultsmentioning

confidence: 99%

Fluorinated tryptophans as substrates and inhibitors of the ATP‐[³²P] PP_i exchange reaction catalysed by tryptophanyl tRNA synthetase

Nevinsky¹,

Фаворова²,

Lavrik³

et al. 1974

FEBS Letters

View full text Add to dashboard Cite

The Determination of Enzyme Dissociation Constants

Cited by 11,875 publications

References 1 publication

Experimental targeted radioiodide therapy following transfection of the sodium iodide symporter gene: Effect on clonogenicity in both two-and three-dimensional models

Experimental targeted radioiodide therapy following transfection of the sodium iodide symporter gene: Effect on clonogenicity in both two-and three-dimensional models

Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation

Fluorinated tryptophans as substrates and inhibitors of the ATP‐[³²P] PP_i exchange reaction catalysed by tryptophanyl tRNA synthetase

Contact Info

Product

Resources

About

The Determination of Enzyme Dissociation Constants

Cited by 11,875 publications

References 1 publication

Experimental targeted radioiodide therapy following transfection of the sodium iodide symporter gene: Effect on clonogenicity in both two-and three-dimensional models

Experimental targeted radioiodide therapy following transfection of the sodium iodide symporter gene: Effect on clonogenicity in both two-and three-dimensional models

Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation

Fluorinated tryptophans as substrates and inhibitors of the ATP‐[32P] PPi exchange reaction catalysed by tryptophanyl tRNA synthetase

Contact Info

Product

Resources

About

Fluorinated tryptophans as substrates and inhibitors of the ATP‐[³²P] PP_i exchange reaction catalysed by tryptophanyl tRNA synthetase