A Highly Selective Hydantoin Inhibitor of Aggrecanase‑1 and Aggrecanase‑2 with a Low Projected Human Dose

Discovery of Highly Potent and Selective Small Molecule ADAMTS‑5 Inhibitors That Inhibit Human Cartilage Degradation via Encoded Library Technology (ELT)

Hongfeng Deng (1438666)
Heather O’Keefe (1665232)
Christopher P. Davie (1551235)
Kenneth E. Lind (1370316)
Raksha A. Acharya (2051182)
G. Joseph Franklin (1370352)
Jonathan Larkin (2051191)
Rosalie Matico (2051176)
Michael Neeb (2051161)
Monique M. Thompson (2051185)
Thomas Lohr (2051188)
Jeffrey W. Gross (2051173)
Paolo A. Centrella (1463083)
Gary K. O’Donovan (2051164)
Katie L. (Sargent) Bedard (1551253)
Kurt van Vloten (2051158)
Sibongile Mataruse (1370310)
Steven R. Skinner (2051170)
Svetlana L. Belyanskaya (1551241)
Tiffany Y. Carpenter (2051179)
Todd W. Shearer (2051167)
Matthew A. Clark (1370337)
John W. Cuozzo (1370322)
Christopher C. Arico-Muendel (1438675)
Barry A. Morgan (1551226)

August 2012

The metalloprotease ADAMTS-5 is considered a potential target for the treatment of osteoarthritis. T...

Inhibition of cartilage and bone destruction in adjuvant arthritis in the rat by a matrix metalloproteinase inhibitor

Conway, James G.
Wakefield, Jean A.
Brown, Roger H.
Marron, Brian E.
Sekut, Les
Stimpson, Stephen A.
McElroy, Andrew
Alan Menius, J.
Jeffreys, John J.
Clark, Richard L.
McGeehan, Gerard M.
Connolly, Kevin M.

January 1995

Considerable evidence has associated the expression of matrix metalloproteinases (MMPs) with the deg...

Inhibition of cartilage and bone destruction in adjuvant arthritis in the rat by a matrix metalloproteinase inhibitor

Conway, James G.
Wakefield, Jean A.
Brown, Roger H.
Marron, Brian E.
Sekut, Les
Stimpson, Stephen A.
McElroy, Andrew
Alan Menius, J.
Jeffreys, John J.
Clark, Richard L.
McGeehan, Gerard M.
Connolly, Kevin M.

January 1995

Considerable evidence has associated the expression of matrix metalloproteinases (MMPs) with the deg...

A Highly Selective Hydantoin Inhibitor of Aggrecanase‑1 and Aggrecanase‑2 with a Low Projected Human Dose

Timothy B. Durham (1698085)
Jothirajah Marimuthu (1698055)
James L. Toth (1698070)
Chin Liu (1698058)
Lisa Adams (1698061)
Daniel R. Mudra (1816981)
Craig Swearingen (1698082)
Chaohua Lin (1698079)
Mark G. Chambers (1698076)
Kannan Thirunavukkarasu (1698073)
Michael R. Wiley (189278)

June 2017

Aggrecanase-1 and -2 (ADAMTS-4 and ADAMTS-5) are zinc metalloproteases involved in the degradation o...

Identification of Potent and Selective Hydantoin Inhibitors of Aggrecanase‑1 and Aggrecanase‑2 That Are Efficacious in Both Chemical and Surgical Models of Osteoarthritis

Timothy B. Durham (1698085)
Valentine J. Klimkowski (1698067)
Christopher J. Rito (1698052)
Jothirajah Marimuthu (1698055)
James L. Toth (1698070)
Chin Liu (1698058)
Jim D. Durbin (1698088)
Stephanie L. Stout (1698064)
Lisa Adams (1698061)
Craig Swearingen (1698082)
Chaohua Lin (1698079)
Mark G. Chambers (1698076)
Kannan Thirunavukkarasu (1698073)
Michael R. Wiley (189278)

December 2014

A disintegrin and metalloproteinase with thrombospondin motifs-4 (ADAMTS-4) and ADAMTS-5 are zinc me...

Progress Towards the Identification of New Aggrecanase Inhibitors

DE RIENZO, Francesca
SAXENA, PUNEET
FILOMIA, Federico
MENZIANI, Maria Cristina
G. Caselli
F. Colace
L. Stasi
A. Giordani

January 2009

Degenerative diseases are still a challenging issue in clinical therapy; even though in several case...

Progress Towards the Identification of New Aggrecanase Inhibitors

DE RIENZO, Francesca
SAXENA, PUNEET
FILOMIA, Federico
MENZIANI, Maria Cristina
G. Caselli
F. Colace
L. Stasi
A. Giordani

January 2009

Degenerative diseases are still a challenging issue in clinical therapy; even though in several case...

Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: Synthesis and biological evaluation.

Nuti E
Santamaria S
Casalini F
Yamamoto K
Marinelli L
La Pietra V
Novellino E
Orlandini E
Nencetti S
Marini A M
Salerno S
Taliani S
Da Settimo F
Nagase H
Rossello A

January 2013

Aggrecanases, in particular aggrecanase-2 (ADAMTS-5), are considered the principal proteases respons...

Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: synthesis and biological evaluation.

Nuti, E
Santamaria, S
Casalini, F
Yamamoto, K
Marinelli, L
La Pietra, V
Novellino, E
Orlandini, E
Nencetti, S
Marini, AM
Salerno, S
Taliani, S
Da Settimo, F
Nagase, H
Rossello, A

April 2013

Aggrecanases, in particular aggrecanase-2 (ADAMTS-5), are considered the principal proteases respons...

The Effect of Protease Inhibitors on the Induction of Osteoarthritis-Related Biomarkers in Bovine Full-Depth Cartilage Explants

He Yi
Zheng Qinlong
Jiang MengMeng
Sun Shu
Christiansen Thorbjørn G.
Kassem Moustapha
Karsdal Morten A.
Bay-Jensen Anne C.

April 2015

The specific degradation of type II collagen and aggrecan by matrix metalloproteinase (MMP)-9, -13 a...

Design and Synthesis of New ADAMTS5 Inhibitors

BERTINETTO, ELISA

November 2018

ADAMTS family is made by 19 secreted zinc metalloproteinases which have important roles in connectiv...

Elevated aggrecanase activity in a rat model of joint injury is attenuated by an aggrecanase specific inhibitor

Chockalingam, P.S.
Sun, W.
Rivera-Bermudez, M.A.
Zeng, W.
Dufield, D.R.
Larsson, S.
Lohmander, L.S.
Flannery, C.R.
Glasson, S.S.
Georgiadis, K.E.
Morris, E.A.

March 2011

SummaryObjectiveTo evaluate aggrecanase activity after traumatic knee injury in a rat model by measu...

Screening, isolation and characterisation of antibodies that block aggrecanase activity of ADAMTS-5

Santamaria, Salvatore

January 2014

A Disintegrin and Metalloproteinase with ThromboSpondin Motif (ADAMTS)-5 is considered to play a key...

The effect of protease inhibitors on the induction of osteoarthritis-related biomarkers in bovine full-depth cartilage explants.

Yi He
Qinlong Zheng
MengMeng Jiang
Shu Sun
Thorbjørn G Christiansen
Moustapha Kassem
Morten A Karsdal
Anne C Bay-Jensen

The specific degradation of type II collagen and aggrecan by matrix metalloproteinase (MMP)-9, -13 a...

Aggrecanolysis in human osteoarthritis: confocal localization and biochemical characterization of ADAMTS5–hyaluronan complexes in articular cartilages

Plaas, A.
Osborn, B.
Yoshihara, Y.
Bai, Y.
Bloom, T.
Nelson, F.
Mikecz, K.
Sandy, J.D.

July 2007

SummaryObjectiveHuman osteoarthritis (OA) is characterized by aggrecanase-mediated depletion of cart...

Discovery of Highly Potent and Selective Small Molecule ADAMTS‑5 Inhibitors That Inhibit Human Cartilage Degradation via Encoded Library Technology (ELT)

Hongfeng Deng (1438666)
Heather O’Keefe (1665232)
Christopher P. Davie (1551235)
Kenneth E. Lind (1370316)
Raksha A. Acharya (2051182)
G. Joseph Franklin (1370352)
Jonathan Larkin (2051191)
Rosalie Matico (2051176)
Michael Neeb (2051161)
Monique M. Thompson (2051185)
Thomas Lohr (2051188)
Jeffrey W. Gross (2051173)
Paolo A. Centrella (1463083)
Gary K. O’Donovan (2051164)
Katie L. (Sargent) Bedard (1551253)
Kurt van Vloten (2051158)
Sibongile Mataruse (1370310)
Steven R. Skinner (2051170)
Svetlana L. Belyanskaya (1551241)
Tiffany Y. Carpenter (2051179)
Todd W. Shearer (2051167)
Matthew A. Clark (1370337)
John W. Cuozzo (1370322)
Christopher C. Arico-Muendel (1438675)
Barry A. Morgan (1551226)

August 2012

The metalloprotease ADAMTS-5 is considered a potential target for the treatment of osteoarthritis. T...

Inhibition of cartilage and bone destruction in adjuvant arthritis in the rat by a matrix metalloproteinase inhibitor

Conway, James G.
Wakefield, Jean A.
Brown, Roger H.
Marron, Brian E.
Sekut, Les
Stimpson, Stephen A.
McElroy, Andrew
Alan Menius, J.
Jeffreys, John J.
Clark, Richard L.
McGeehan, Gerard M.
Connolly, Kevin M.

January 1995

Considerable evidence has associated the expression of matrix metalloproteinases (MMPs) with the deg...

Inhibition of cartilage and bone destruction in adjuvant arthritis in the rat by a matrix metalloproteinase inhibitor

Conway, James G.
Wakefield, Jean A.
Brown, Roger H.
Marron, Brian E.
Sekut, Les
Stimpson, Stephen A.
McElroy, Andrew
Alan Menius, J.
Jeffreys, John J.
Clark, Richard L.
McGeehan, Gerard M.
Connolly, Kevin M.

January 1995

Considerable evidence has associated the expression of matrix metalloproteinases (MMPs) with the deg...

A Highly Selective Hydantoin Inhibitor of Aggrecanase‑1 and Aggrecanase‑2 with a Low Projected Human Dose

Timothy B. Durham (1698085)
Jothirajah Marimuthu (1698055)
James L. Toth (1698070)
Chin Liu (1698058)
Lisa Adams (1698061)
Daniel R. Mudra (1816981)
Craig Swearingen (1698082)
Chaohua Lin (1698079)
Mark G. Chambers (1698076)
Kannan Thirunavukkarasu (1698073)
Michael R. Wiley (189278)

June 2017

Aggrecanase-1 and -2 (ADAMTS-4 and ADAMTS-5) are zinc metalloproteases involved in the degradation o...

Identification of Potent and Selective Hydantoin Inhibitors of Aggrecanase‑1 and Aggrecanase‑2 That Are Efficacious in Both Chemical and Surgical Models of Osteoarthritis

Timothy B. Durham (1698085)
Valentine J. Klimkowski (1698067)
Christopher J. Rito (1698052)
Jothirajah Marimuthu (1698055)
James L. Toth (1698070)
Chin Liu (1698058)
Jim D. Durbin (1698088)
Stephanie L. Stout (1698064)
Lisa Adams (1698061)
Craig Swearingen (1698082)
Chaohua Lin (1698079)
Mark G. Chambers (1698076)
Kannan Thirunavukkarasu (1698073)
Michael R. Wiley (189278)

December 2014

A disintegrin and metalloproteinase with thrombospondin motifs-4 (ADAMTS-4) and ADAMTS-5 are zinc me...

Progress Towards the Identification of New Aggrecanase Inhibitors

DE RIENZO, Francesca
SAXENA, PUNEET
FILOMIA, Federico
MENZIANI, Maria Cristina
G. Caselli
F. Colace
L. Stasi
A. Giordani

January 2009

Degenerative diseases are still a challenging issue in clinical therapy; even though in several case...

Progress Towards the Identification of New Aggrecanase Inhibitors

DE RIENZO, Francesca
SAXENA, PUNEET
FILOMIA, Federico
MENZIANI, Maria Cristina
G. Caselli
F. Colace
L. Stasi
A. Giordani

January 2009

Degenerative diseases are still a challenging issue in clinical therapy; even though in several case...

Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: Synthesis and biological evaluation.

Nuti E
Santamaria S
Casalini F
Yamamoto K
Marinelli L
La Pietra V
Novellino E
Orlandini E
Nencetti S
Marini A M
Salerno S
Taliani S
Da Settimo F
Nagase H
Rossello A

January 2013

Aggrecanases, in particular aggrecanase-2 (ADAMTS-5), are considered the principal proteases respons...

Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: synthesis and biological evaluation.

Nuti, E
Santamaria, S
Casalini, F
Yamamoto, K
Marinelli, L
La Pietra, V
Novellino, E
Orlandini, E
Nencetti, S
Marini, AM
Salerno, S
Taliani, S
Da Settimo, F
Nagase, H
Rossello, A

April 2013

Aggrecanases, in particular aggrecanase-2 (ADAMTS-5), are considered the principal proteases respons...

The Effect of Protease Inhibitors on the Induction of Osteoarthritis-Related Biomarkers in Bovine Full-Depth Cartilage Explants

He Yi
Zheng Qinlong
Jiang MengMeng
Sun Shu
Christiansen Thorbjørn G.
Kassem Moustapha
Karsdal Morten A.
Bay-Jensen Anne C.

April 2015

The specific degradation of type II collagen and aggrecan by matrix metalloproteinase (MMP)-9, -13 a...

Design and Synthesis of New ADAMTS5 Inhibitors

BERTINETTO, ELISA

November 2018

ADAMTS family is made by 19 secreted zinc metalloproteinases which have important roles in connectiv...

Elevated aggrecanase activity in a rat model of joint injury is attenuated by an aggrecanase specific inhibitor

Chockalingam, P.S.
Sun, W.
Rivera-Bermudez, M.A.
Zeng, W.
Dufield, D.R.
Larsson, S.
Lohmander, L.S.
Flannery, C.R.
Glasson, S.S.
Georgiadis, K.E.
Morris, E.A.

March 2011

SummaryObjectiveTo evaluate aggrecanase activity after traumatic knee injury in a rat model by measu...

Screening, isolation and characterisation of antibodies that block aggrecanase activity of ADAMTS-5

Santamaria, Salvatore

January 2014

A Disintegrin and Metalloproteinase with ThromboSpondin Motif (ADAMTS)-5 is considered to play a key...

The effect of protease inhibitors on the induction of osteoarthritis-related biomarkers in bovine full-depth cartilage explants.

Yi He
Qinlong Zheng
MengMeng Jiang
Shu Sun
Thorbjørn G Christiansen
Moustapha Kassem
Morten A Karsdal
Anne C Bay-Jensen

The specific degradation of type II collagen and aggrecan by matrix metalloproteinase (MMP)-9, -13 a...

Aggrecanolysis in human osteoarthritis: confocal localization and biochemical characterization of ADAMTS5–hyaluronan complexes in articular cartilages

Plaas, A.
Osborn, B.
Yoshihara, Y.
Bai, Y.
Bloom, T.
Nelson, F.
Mikecz, K.
Sandy, J.D.

July 2007

SummaryObjectiveHuman osteoarthritis (OA) is characterized by aggrecanase-mediated depletion of cart...

Discovery of Highly Potent and Selective Small Molecule ADAMTS‑5 Inhibitors That Inhibit Human Cartilage Degradation via Encoded Library Technology (ELT)

Hongfeng Deng (1438666)
Heather O’Keefe (1665232)
Christopher P. Davie (1551235)
Kenneth E. Lind (1370316)
Raksha A. Acharya (2051182)
G. Joseph Franklin (1370352)
Jonathan Larkin (2051191)
Rosalie Matico (2051176)
Michael Neeb (2051161)
Monique M. Thompson (2051185)
Thomas Lohr (2051188)
Jeffrey W. Gross (2051173)
Paolo A. Centrella (1463083)
Gary K. O’Donovan (2051164)
Katie L. (Sargent) Bedard (1551253)
Kurt van Vloten (2051158)
Sibongile Mataruse (1370310)
Steven R. Skinner (2051170)
Svetlana L. Belyanskaya (1551241)
Tiffany Y. Carpenter (2051179)
Todd W. Shearer (2051167)
Matthew A. Clark (1370337)
John W. Cuozzo (1370322)
Christopher C. Arico-Muendel (1438675)
Barry A. Morgan (1551226)

August 2012

The metalloprotease ADAMTS-5 is considered a potential target for the treatment of osteoarthritis. T...

Inhibition of cartilage and bone destruction in adjuvant arthritis in the rat by a matrix metalloproteinase inhibitor

Conway, James G.
Wakefield, Jean A.
Brown, Roger H.
Marron, Brian E.
Sekut, Les
Stimpson, Stephen A.
McElroy, Andrew
Alan Menius, J.
Jeffreys, John J.
Clark, Richard L.
McGeehan, Gerard M.
Connolly, Kevin M.

January 1995

Considerable evidence has associated the expression of matrix metalloproteinases (MMPs) with the deg...

Inhibition of cartilage and bone destruction in adjuvant arthritis in the rat by a matrix metalloproteinase inhibitor

Conway, James G.
Wakefield, Jean A.
Brown, Roger H.
Marron, Brian E.
Sekut, Les
Stimpson, Stephen A.
McElroy, Andrew
Alan Menius, J.
Jeffreys, John J.
Clark, Richard L.
McGeehan, Gerard M.
Connolly, Kevin M.

January 1995

Considerable evidence has associated the expression of matrix metalloproteinases (MMPs) with the deg...

A Highly Selective Hydantoin Inhibitor of Aggrecanase‑1 and Aggrecanase‑2 with a Low Projected Human Dose

Abstract

Extracted data

A Highly Selective Hydantoin Inhibitor of Aggrecanase‑1 and Aggrecanase‑2 with a Low Projected Human Dose

Abstract

Extracted data

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