Discovery of PF-06835919: A Potent Inhibitor of Ketohexokinase (KHK) for the Treatment of Metabolic Disorders Driven by the Overconsumption of Fructose-Reference-Cited by-同舟云学术

Discovery of PF-06835919: A Potent Inhibitor of Ketohexokinase (KHK) for the Treatment of Metabolic Disorders Driven by the Overconsumption of Fructose

Published:2020-09-10 Issue:22 Volume:63 Page:13546-13560
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Futatsugi Kentaro¹^ORCID,Smith Aaron C.²^ORCID,Tu Meihua¹,Raymer Brian¹,Ahn Kay³^ORCID,Coffey Steven B.²,Dowling Matthew S.²^ORCID,Fernando Dilinie P.²,Gutierrez Jemy A.³,Huard Kim¹,Jasti Jayasankar²,Kalgutkar Amit S.¹^ORCID,Knafels John D.²,Pandit Jayvardhan²,Parris Kevin D.²,Perez Sylvie³,Pfefferkorn Jeffrey A.³,Price David A.¹,Ryder Tim²,Shavnya Andre²,Stock Ingrid A.²,Tsai Andy S.²,Tesz Gregory J.³,Thuma Benjamin A.²,Weng Yan¹,Wisniewska Hanna M.²,Xing Gang³,Zhou Jun⁴,Magee Thomas V.¹

Affiliation:

1. Pfizer Inc. Medicine Design, 1 Portland Street, Cambridge, Massachusetts 02139, United States

2. Pfizer Inc. Medicine Design, Eastern Point Road, Groton, Connecticut 06340, United States

3. Pfizer Inc. Internal Medicine Research Unit, 1 Portland Street, Cambridge, Massachusetts 02139, United States

4. Pfizer Inc. Drug Safety R&D, Eastern Point Road, Groton, Connecticut 06340, United States

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.0c00944

Reference32 articles.

1. Consuming fructose-sweetened, not glucose-sweetened, beverages increases visceral adiposity and lipids and decreases insulin sensitivity in overweight/obese humans

2. Consumption of fructose-sweetened beverages for 10 weeks increases postprandial triacylglycerol and apolipoprotein-B concentrations in overweight and obese women

3. Increased fructose consumption is associated with fibrosis severity in patients with nonalcoholic fatty liver disease

4. Soft drink consumption is associated with fatty liver disease independent of metabolic syndrome

5. Sugar-Sweetened Beverages, Weight Gain, and Incidence of Type 2 Diabetes in Young and Middle-Aged Women

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