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Dive into the research topics where Haixia Wang is active.

Publication


Featured researches published by Haixia Wang.


Bioorganic & Medicinal Chemistry Letters | 2013

Design, synthesis and SAR of novel glucokinase activators.

Zacharia Cheruvallath; Stephen L. Gwaltney; Mark Sabat; Mingnam Tang; Jun Feng; Haixia Wang; Joanne Miura; Prasuna Guntupalli; Andy Jennings; David J. Hosfield; Bumsup Lee; Yiqin Wu

Guided by co-crystal structures of compounds 15, 22 and 30, an SBDD approach led to the discovery of the 6-methyl pyridone series as a novel class of GKAs that potently activate GK in enzyme and cell assays. Anti-diabetic OGTT efficacy was demonstrated with 54 in a mouse model of type 2 diabetes.


ACS Medicinal Chemistry Letters | 2017

Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure.

Marion Lanier; Jason Pickens; Simone V. Bigi; Erica L. Bradshaw-Pierce; Alison Chambers; Zacharia Cheruvallath; Derek Cecil Cole; Douglas R. Dougan; Jacques Ermolieff; Tony S. Gibson; Petro Halkowycz; Aki Hirokawa; Anthony Ivetac; Joanne Miura; Evan Nunez; Mark Sabat; John Tyhonas; Haixia Wang; Xiaolun Wang; Steve Swann

Apoptosis signal-regulating kinase 1 (ASK1/MAP3K) is a mitogen-activated protein kinase family member shown to contribute to acute ischemia/reperfusion injury. Using structure-based drug design, deconstruction, and reoptimization of a known ASK1 inhibitor, a lead compound was identified. This compound displayed robust MAP3K pathway inhibition and reduction of infarct size in an isolated perfused heart model of cardiac injury.


Bioorganic & Medicinal Chemistry Letters | 2017

Design, synthesis and optimization of 7-substituted-pyrazolo[4,3- b ]pyridine ALK5 (activin receptor-like kinase 5) inhibitors

Mark Sabat; Haixia Wang; Nick Scorah; J. David Lawson; Joy Atienza; Ruhi Kamran; Mark S. Hixon; Douglas R. Dougan

A series of potent ALK5 inhibitors were designed using a SBDD approach and subsequently optimized to improve drug likeness. Starting with a 4-substituted quinoline screening hit, SAR was conducted using a ALK5 binding model to understand the binding site and optimize activity. The resulting inhibitors displayed excellent potency but were limited by high in vitro clearance in rat and human microsomes. Using a scaffold morphing strategy, these analogs were transformed into a related pyrazolo[4,3-b]pyridine series with improved ADME properties.


Bioorganic & Medicinal Chemistry Letters | 2017

Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators.

Zacharia Cheruvallath; Stephen L. Gwaltney; Mark Sabat; Mingnam Tang; Haixia Wang; Andy Jennings; David J. Hosfield; Bumsup Lee; Yiqin Wu; Petro Halkowycz; Charles E. Grimshaw

Guided by co-crystal structural information obtained from a different series we were exploring, a scaffold morphing and SBDD approach led to the discovery of the 1,4-disubstituted indazole series as a novel class of GKAs that potently activate GK in enzyme and cell assays. anti-diabetic OGTT efficacy was demonstrated with 29 in a rodent models of type 2 diabetes.


Bioorganic & Medicinal Chemistry Letters | 2016

Design, synthesis and optimization of novel Alk5 (activin-like kinase 5) inhibitors

Haixia Wang; J. David Lawson; Nick Scorah; Ruhi Kamran; Mark S. Hixon; Joy Atienza; Douglas R. Dougan; Mark Sabat

Using SBDD, a series of 4-amino-7-azaindoles were discovered as a novel class of Alk5 inhibitors that are potent in both Alk5 enzymatic and cellular assays. Subsequently a ring cyclization strategy was utilized to improve ADME properties leading to the discovery of a series of 1H-imidazo[4,5-c]pyridin-2(3H)-one drug like Alk5 inhibitors.


ACS Medicinal Chemistry Letters | 2017

Correction to “Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure”

Marion Lanier; Jason Pickens; Simone V. Bigi; Erica L. Bradshaw-Pierce; Alison Chambers; Zacharia Cheruvallath; Derek Cecil Cole; Douglas R. Dougan; Jacques Ermolieff; Tony S. Gibson; Petro Halkowycz; Aki Hirokawa; Anthony Ivetac; Christopher Mcbride; Joanne Miura; Evan Nunez; Mark Sabat; John Tyhonas; Haixia Wang; Xiaolun Wang; Steve Swann

[This corrects the article DOI: 10.1021/acsmedchemlett.6b00481.].


Archive | 2014

Pyridinyl and fused pyridinyl triazolone derivatives

John David Lawson; Mark Sabat; Nicholas Scorah; Christopher Smith; Phong H. Vu; Haixia Wang


Archive | 2013

Cinnoline derivatives as as btk inhibitors

John David Lawson; Mark Sabat; Christopher Smith; Haixia Wang; Young K. Chen; Toufike Kanouni


Archive | 2015

Heteroarylamide inhibitors of TBK1

Walter Keung; Lily Kwok; Mark Sabat; Nicholas Scorah; Haixia Wang; Steven John Woodhead; Anthony R. Gangloff


Archive | 2014

Triazolone derivatives pyridinyl and pyridinyl condensed triazolone

John David Lawson; Mark Sabat; Nicholas Scorah; Christopher Smith; Phong H. Vu; Haixia Wang

Collaboration


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Mark Sabat

Takeda Pharmaceutical Company

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Christopher Smith

Takeda Pharmaceutical Company

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Douglas R. Dougan

Takeda Pharmaceutical Company

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John David Lawson

Takeda Pharmaceutical Company

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Nicholas Scorah

Takeda Pharmaceutical Company

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Zacharia Cheruvallath

Takeda Pharmaceutical Company

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Joanne Miura

Takeda Pharmaceutical Company

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Petro Halkowycz

Takeda Pharmaceutical Company

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Phong H. Vu

Takeda Pharmaceutical Company

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Andy Jennings

Takeda Pharmaceutical Company

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