Results of the PolarScreen PPAR Competitor Assay for all selected compounds, except C4 and C10, which had solubility problems.

PPAR transactivation assays.

Fernanda A. H. Batista (165000)
Daniela B. B. Trivella (165003)
Amanda Bernardes (165009)
Joyce Gratieri (165011)
Paulo S. L. Oliveira (165017)
Ana Carolina M. Figueira (165022)
Paul Webb (66473)
Igor Polikarpov (89402)

May 2012

PPAR activation induced by (A) the δ-selective agonist GW0742; (B) the pan-agonist ...

Glucose depletion synergized cytotoxicity of PPARα antagonist but not agonist.

Omran Abu Aboud (442744)
Hiromi I. Wettersten (442745)
Robert H. Weiss (442746)

August 2013

A. RCC cells (Caki-1 and 786-O) were treated with DMSO (Cont), GW6471 (GW) 25 µM, and/or 2-DG (5 ...

PPARα antagonist inhibited RCC and NHK cell viability.

Omran Abu Aboud (442744)
Hiromi I. Wettersten (442745)
Robert H. Weiss (442746)

August 2013

RCC cells (Caki-1 and 786-O) were treated with DMSO, WY14,643 (WY), or GW6471 (GW) at the indicat...

Experimental IC50 values and transactivation activity of the selected compounds.

Laura Guasch (115890)
Esther Sala (115893)
Anna Castell-Auví (115896)
Lidia Cedó (115899)
Klaus R. Liedl (109013)
Gerhard Wolber (115901)
Markus Muehlbacher (115902)
Miquel Mulero (115904)
Montserrat Pinent (115906)
Anna Ardévol (115908)
Cristina Valls (115909)
Gerard Pujadas (115910)
Santiago Garcia-Vallvé (87135)

November 2012

A competitive binding assay was used to assess the ability of experimental compounds, FMOC or ros...

Carcinogenic survival assay results charting survival of PBRM1 / BAF180 knock-out cell lines with concentration intervals of the PARP inhibitor Olaparib, the POLA inhibitor Erocalciferol and the ABL inhibitor Dasatanib.

Graeme Benstead-Hume (3566114)
Xiangrong Chen (697789)
Suzanna R. Hopkins (6597443)
Karen A. Lane (6597446)
Jessica A. Downs (332831)
Frances M. G. Pearl (6597449)

April 2019

These results suggest PBRM1 mutant cells may be more sensitive to both the PARP and ABL1 inhibitors ...

Identification of PPARgamma Partial Agonists of Natural Origin (I): Development of a Virtual Screening Procedure and In Vitro Validation

Guasch Laura
Sala Esther
Castell-Auví Anna
Cedó Lidia
Liedl Klaus R.
Wolber Gerhard
Muehlbacher Markus
Mulero Miquel
Pinent Montserrat
Ardévol Anna
Valls Cristina
Pujadas Gerard
Garcia-Vallvé Santiago

November 2012

Although there are successful examples of the discovery of new PPARγ agonists, it has recently been ...

Results of 1st FCCS screening of 495 chemicals.

Shintaro Mikuni (466570)
Kota Kodama (767253)
Akira Sasaki (361986)
Naoki Kohira (767254)
Hideki Maki (316193)
Masaharu Munetomo (767255)
Katsumi Maenaka (457393)
Masataka Kinjo (30728)

July 2015

A. Bar graph of averaged binding ratios from 3 independent screenings. Error bar indicates the st...

Results of 2nd FCCS screening of 888 chemicals.

Shintaro Mikuni (466570)
Kota Kodama (767253)
Akira Sasaki (361986)
Naoki Kohira (767254)
Hideki Maki (316193)
Masaharu Munetomo (767255)
Katsumi Maenaka (457393)
Masataka Kinjo (30728)

July 2015

A. Bar graph of averaged binding ratios of 3 independent screenings. Error bar indicates the stan...

Effect of valproic acid and amiodarone on PPARα, PPAR β/δ, and PPARγ gene reporter assays.

Ewa Szalowska (516453)
Bart van der Burg (516454)
Hai-Yen Man (516455)
Peter J. M. Hendriksen (516456)
Ad A. C. M. Peijnenburg (516457)

January 2014

Luciferase activity of PPARα CALUX cells upon exposure to PPARα agonists: GW7647 (A) and valproic...

Identification of novel multitargeted PPARα/γ/δ pan agonists by core hopping of rosiglitazone

Wang XJ
Zhang J
Wang SQ
Xu WR
Cheng XC
Wang RL

November 2014

Xue-Jiao Wang,1 Jun Zhang,1 Shu-Qing Wang,1 Wei-Ren Xu,2 Xian-Chao Cheng,1 Run-Ling Wang1 1Tianjin ...

PPARγ binds three MCFAs.

Marcelo Vizoná Liberato (162662)
Alessandro S. Nascimento (162666)
Steven D. Ayers (162670)
Jean Z. Lin (105176)
Aleksandra Cvoro (105194)
Rodrigo L. Silveira (162673)
Leandro Martínez (79928)
Paulo C. T. Souza (162677)
Daniel Saidemberg (162681)
Tuo Deng (162685)
Angela Angelica Amato (162690)
Marie Togashi (162694)
Willa A. Hsueh (162700)
Kevin Phillips (162705)
Mário Sérgio Palma (162711)
Francisco A. R. Neves (162716)
Munir S. Skaf (162722)
Paul Webb (66473)
Igor Polikarpov (89402)

May 2012

(A) Structure of the PPARγ LBD chain A subunit showing positions of MCFA electron densitie...

Validation of each method used in the virtual screening workflow.

Laura Guasch (115890)
Esther Sala (115893)
Anna Castell-Auví (115896)
Lidia Cedó (115899)
Klaus R. Liedl (109013)
Gerhard Wolber (115901)
Markus Muehlbacher (115902)
Miquel Mulero (115904)
Montserrat Pinent (115906)
Anna Ardévol (115908)
Cristina Valls (115909)
Gerard Pujadas (115910)
Santiago Garcia-Vallvé (87135)

November 2012

A dataset of 19 known PPARγ partial agonists, 135 known PPARγ full agonists and 3122 decoys extra...

rCR2 binding to C3d as measured by ELISA.

Adam Badar (353606)
Sarah DeFreitas (353608)
James M. McDonnell (353610)
Norhakim Yahya (353612)
David Thakor (353613)
Reza Razavi (90384)
Richard Smith (45265)
Steven Sacks (353615)
Gregory E. D. Mullen (67161)

February 2013

To determine the binding of rCR2 to C3d, the antigen C3d was coated on ELISA plates at increasing...

Identification of PPARgamma partial agonists of natural origin (I): development of a virtual screening procedure and in vitro validation.

Laura Guasch
Esther Sala
Anna Castell-Auví
Lidia Cedó
Klaus R Liedl
Gerhard Wolber
Markus Muehlbacher
Miquel Mulero
Montserrat Pinent
Anna Ardévol
Cristina Valls
Gerard Pujadas
Santiago Garcia-Vallvé

BACKGROUND: Although there are successful examples of the discovery of new PPARγ agonists, it has re...

Single Point Hit Confirmation and Control Screens.

C. Aaron Monroy (406183)
Duncan I. Mackie (406184)
David L. Roman (406185)

April 2013

(A) Single point hit confirmation assay was an analysis of each of the initial hits in a 384-well...

PPAR transactivation assays.

Fernanda A. H. Batista (165000)
Daniela B. B. Trivella (165003)
Amanda Bernardes (165009)
Joyce Gratieri (165011)
Paulo S. L. Oliveira (165017)
Ana Carolina M. Figueira (165022)
Paul Webb (66473)
Igor Polikarpov (89402)

May 2012

PPAR activation induced by (A) the δ-selective agonist GW0742; (B) the pan-agonist ...

Glucose depletion synergized cytotoxicity of PPARα antagonist but not agonist.

Omran Abu Aboud (442744)
Hiromi I. Wettersten (442745)
Robert H. Weiss (442746)

August 2013

A. RCC cells (Caki-1 and 786-O) were treated with DMSO (Cont), GW6471 (GW) 25 µM, and/or 2-DG (5 ...

PPARα antagonist inhibited RCC and NHK cell viability.

Omran Abu Aboud (442744)
Hiromi I. Wettersten (442745)
Robert H. Weiss (442746)

August 2013

RCC cells (Caki-1 and 786-O) were treated with DMSO, WY14,643 (WY), or GW6471 (GW) at the indicat...

Experimental IC50 values and transactivation activity of the selected compounds.

Laura Guasch (115890)
Esther Sala (115893)
Anna Castell-Auví (115896)
Lidia Cedó (115899)
Klaus R. Liedl (109013)
Gerhard Wolber (115901)
Markus Muehlbacher (115902)
Miquel Mulero (115904)
Montserrat Pinent (115906)
Anna Ardévol (115908)
Cristina Valls (115909)
Gerard Pujadas (115910)
Santiago Garcia-Vallvé (87135)

November 2012

A competitive binding assay was used to assess the ability of experimental compounds, FMOC or ros...

Carcinogenic survival assay results charting survival of PBRM1 / BAF180 knock-out cell lines with concentration intervals of the PARP inhibitor Olaparib, the POLA inhibitor Erocalciferol and the ABL inhibitor Dasatanib.

Graeme Benstead-Hume (3566114)
Xiangrong Chen (697789)
Suzanna R. Hopkins (6597443)
Karen A. Lane (6597446)
Jessica A. Downs (332831)
Frances M. G. Pearl (6597449)

April 2019

These results suggest PBRM1 mutant cells may be more sensitive to both the PARP and ABL1 inhibitors ...

Identification of PPARgamma Partial Agonists of Natural Origin (I): Development of a Virtual Screening Procedure and In Vitro Validation

Guasch Laura
Sala Esther
Castell-Auví Anna
Cedó Lidia
Liedl Klaus R.
Wolber Gerhard
Muehlbacher Markus
Mulero Miquel
Pinent Montserrat
Ardévol Anna
Valls Cristina
Pujadas Gerard
Garcia-Vallvé Santiago

November 2012

Although there are successful examples of the discovery of new PPARγ agonists, it has recently been ...

Results of 1st FCCS screening of 495 chemicals.

Shintaro Mikuni (466570)
Kota Kodama (767253)
Akira Sasaki (361986)
Naoki Kohira (767254)
Hideki Maki (316193)
Masaharu Munetomo (767255)
Katsumi Maenaka (457393)
Masataka Kinjo (30728)

July 2015

A. Bar graph of averaged binding ratios from 3 independent screenings. Error bar indicates the st...

Results of 2nd FCCS screening of 888 chemicals.

Shintaro Mikuni (466570)
Kota Kodama (767253)
Akira Sasaki (361986)
Naoki Kohira (767254)
Hideki Maki (316193)
Masaharu Munetomo (767255)
Katsumi Maenaka (457393)
Masataka Kinjo (30728)

July 2015

A. Bar graph of averaged binding ratios of 3 independent screenings. Error bar indicates the stan...

Effect of valproic acid and amiodarone on PPARα, PPAR β/δ, and PPARγ gene reporter assays.

Ewa Szalowska (516453)
Bart van der Burg (516454)
Hai-Yen Man (516455)
Peter J. M. Hendriksen (516456)
Ad A. C. M. Peijnenburg (516457)

January 2014

Luciferase activity of PPARα CALUX cells upon exposure to PPARα agonists: GW7647 (A) and valproic...

Identification of novel multitargeted PPARα/γ/δ pan agonists by core hopping of rosiglitazone

Wang XJ
Zhang J
Wang SQ
Xu WR
Cheng XC
Wang RL

November 2014

Xue-Jiao Wang,1 Jun Zhang,1 Shu-Qing Wang,1 Wei-Ren Xu,2 Xian-Chao Cheng,1 Run-Ling Wang1 1Tianjin ...

PPARγ binds three MCFAs.

Marcelo Vizoná Liberato (162662)
Alessandro S. Nascimento (162666)
Steven D. Ayers (162670)
Jean Z. Lin (105176)
Aleksandra Cvoro (105194)
Rodrigo L. Silveira (162673)
Leandro Martínez (79928)
Paulo C. T. Souza (162677)
Daniel Saidemberg (162681)
Tuo Deng (162685)
Angela Angelica Amato (162690)
Marie Togashi (162694)
Willa A. Hsueh (162700)
Kevin Phillips (162705)
Mário Sérgio Palma (162711)
Francisco A. R. Neves (162716)
Munir S. Skaf (162722)
Paul Webb (66473)
Igor Polikarpov (89402)

May 2012

(A) Structure of the PPARγ LBD chain A subunit showing positions of MCFA electron densitie...

Validation of each method used in the virtual screening workflow.

Laura Guasch (115890)
Esther Sala (115893)
Anna Castell-Auví (115896)
Lidia Cedó (115899)
Klaus R. Liedl (109013)
Gerhard Wolber (115901)
Markus Muehlbacher (115902)
Miquel Mulero (115904)
Montserrat Pinent (115906)
Anna Ardévol (115908)
Cristina Valls (115909)
Gerard Pujadas (115910)
Santiago Garcia-Vallvé (87135)

November 2012

A dataset of 19 known PPARγ partial agonists, 135 known PPARγ full agonists and 3122 decoys extra...

rCR2 binding to C3d as measured by ELISA.

Adam Badar (353606)
Sarah DeFreitas (353608)
James M. McDonnell (353610)
Norhakim Yahya (353612)
David Thakor (353613)
Reza Razavi (90384)
Richard Smith (45265)
Steven Sacks (353615)
Gregory E. D. Mullen (67161)

February 2013

To determine the binding of rCR2 to C3d, the antigen C3d was coated on ELISA plates at increasing...

Identification of PPARgamma partial agonists of natural origin (I): development of a virtual screening procedure and in vitro validation.

Laura Guasch
Esther Sala
Anna Castell-Auví
Lidia Cedó
Klaus R Liedl
Gerhard Wolber
Markus Muehlbacher
Miquel Mulero
Montserrat Pinent
Anna Ardévol
Cristina Valls
Gerard Pujadas
Santiago Garcia-Vallvé

BACKGROUND: Although there are successful examples of the discovery of new PPARγ agonists, it has re...

Single Point Hit Confirmation and Control Screens.

C. Aaron Monroy (406183)
Duncan I. Mackie (406184)
David L. Roman (406185)

April 2013

(A) Single point hit confirmation assay was an analysis of each of the initial hits in a 384-well...

PPAR transactivation assays.

Fernanda A. H. Batista (165000)
Daniela B. B. Trivella (165003)
Amanda Bernardes (165009)
Joyce Gratieri (165011)
Paulo S. L. Oliveira (165017)
Ana Carolina M. Figueira (165022)
Paul Webb (66473)
Igor Polikarpov (89402)

May 2012

PPAR activation induced by (A) the δ-selective agonist GW0742; (B) the pan-agonist ...

Glucose depletion synergized cytotoxicity of PPARα antagonist but not agonist.

Omran Abu Aboud (442744)
Hiromi I. Wettersten (442745)
Robert H. Weiss (442746)

August 2013

A. RCC cells (Caki-1 and 786-O) were treated with DMSO (Cont), GW6471 (GW) 25 µM, and/or 2-DG (5 ...

PPARα antagonist inhibited RCC and NHK cell viability.

Omran Abu Aboud (442744)
Hiromi I. Wettersten (442745)
Robert H. Weiss (442746)

August 2013

RCC cells (Caki-1 and 786-O) were treated with DMSO, WY14,643 (WY), or GW6471 (GW) at the indicat...

Results of the PolarScreen PPAR Competitor Assay for all selected compounds, except C4 and C10, which had solubility problems.

Abstract

Extracted data

Results of the PolarScreen PPAR Competitor Assay for all selected compounds, except C4 and C10, which had solubility problems.

Abstract

Extracted data

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