A. Rendina

发表

Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases.

Michelle C. Schaeffer, Carol A. Capriotti, P. A. Harris, 2017, Journal of medicinal chemistry.

Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties.

Chong-Hwan Chang, P. Lam, D. Cheney, 2008, Bioorganic & medicinal chemistry letters.

Discovery of novel P1 groups for coagulation factor VIIa inhibition using fragment-based screening.

L. Mueller, D. Cheney, W. Metzler, 2015, Journal of medicinal chemistry.

Inhibition of acetyl-coenzyme a carboxylase by coenzyme a conjugates of grass-selective herbicides

M. Hixon, A. Rendina, W. Taylor, 1995 .

A highly selective, cell-permeable furin inhibitor BOS-318 rescues key features of cystic fibrosis airway disease.

K. Wilcoxen, N. Campobasso, J. Axten, 2022, Cell chemical biology.

Design and synthesis of bicyclic pyrazinone and pyrimidinone amides as potent TF-FVIIa inhibitors.

Wen Jiang, R. Knabb, A. Rendina, 2013, Bioorganic & medicinal chemistry letters.

Pyridine and pyridinone-based factor XIa inhibitors.

P. Morin, D. Seiffert, A. Rendina, 2015, Bioorganic & medicinal chemistry letters.

Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.

P. Morin, D. Seiffert, A. Rendina, 2014, Journal of medicinal chemistry.

New IDH1 mutant inhibitors for treatment of acute myeloid leukemia.

Nicholas D. Adams, G. Drewes, M. Bantscheff, 2015, Nature chemical biology.

1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.

P. Lam, K. He, R. Knabb, 2006, Bioorganic & medicinal chemistry letters.

Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.

P. Lam, K. He, R. Knabb, 2006, Bioorganic & medicinal chemistry letters.

Nonbenzamidine acylsulfonamide tissue factor-factor VIIa inhibitors.

D. Cheney, C. Weigelt, Yan Zou, 2013, Bioorganic & medicinal chemistry letters.

A human fatty acid synthase inhibitor binds β-ketoacyl reductase in the keto-substrate site.

Ramona N Plant, K. Brown, J. Briand, 2014, Nature chemical biology.

Mechanistic MALDI-TOF Cell-Based Assay for the Discovery of Potent and Specific Fatty Acid Synthase Inhibitors.

C. Hopf, A. Rendina, J. A. Krueger, 2019, Cell chemical biology.

Differential activation of recombinant human acetyl-CoA carboxylases 1 and 2 by citrate.

M. Witmer, J. Marcinkeviciene, A. Rendina, 2008, Archives of biochemistry and biophysics.

Neutral macrocyclic factor VIIa inhibitors.

Brandon L. Parkhurst, Wen Jiang, D. Cheney, 2017, Bioorganic & medicinal chemistry letters.

Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors.

Brandon L. Parkhurst, Wen Jiang, D. Cheney, 2016, ACS medicinal chemistry letters.

In vitro, antithrombotic and bleeding time studies of BMS-654457, a small-molecule, reversible and direct inhibitor of factor XIa

D. Seiffert, A. Rendina, M. Harpel, 2015, Journal of Thrombosis and Thrombolysis.

Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.

Brandon L. Parkhurst, Wen Jiang, D. Cheney, 2016, Journal of medicinal chemistry.

Design and Synthesis of Phenylpyrrolidine Phenylglycinamides As Highly Potent and Selective TF-FVIIa Inhibitors.

Wen Jiang, D. Cheney, Yan Zou, 2014, ACS medicinal chemistry letters.

Novel phenylalanine derived diamides as Factor XIa inhibitors.

P. Lam, P. Morin, D. Seiffert, 2016, Bioorganic & medicinal chemistry letters.

Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications.

P. Lam, D. Cheney, K. He, 2007, Bioorganic & medicinal chemistry letters.

Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.

P. Lam, K. He, R. Knabb, 2014, Bioorganic & medicinal chemistry letters.

Characterization of Apo‐Form Selective Inhibition of Indoleamine 2,3‐Dioxygenase **

Douglas W. Thomson, Rodrigo F. Ortiz-Meoz, G. Bergamini, 2020, Chembiochem : a European journal of chemical biology.

Characterization of apo-form selective inhibition of indoleamine 2,3-dioxygenase

Douglas W. Thomson, Rodrigo F. Ortiz-Meoz, G. Bergamini, 2020, bioRxiv.

Characterization of novel inhibition of indoleamine 2,3-dioxygenase by targeting its apo form.

Douglas W. Thomson, Rodrigo F. Ortiz-Meoz, G. Bergamini, 2018 .

BMS-593214, an active site-directed factor VIIa inhibitor: Enzyme kinetics, antithrombotic and antihaemostatic studies

R. Knabb, A. Rendina, B. Xin, 2010, Thrombosis and Haemostasis.

Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors.

D. Cheney, A. Rendina, R. Wexler, 2015, Journal of medicinal chemistry.

Design and Synthesis of Novel Meta-Linked Phenylglycine Macrocyclic FVIIa Inhibitors.

D. Cheney, D. Seiffert, A. Rendina, 2017, ACS medicinal chemistry letters.

Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.

Angela Smallwood, Stephanie Koch, P. Lam, 2007, Journal of medicinal chemistry.

SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa.

Chong-Hwan Chang, Daniel L Cheney, Chong-Hwan Chang, 2007, Bioorganic & medicinal chemistry letters.

Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.

P. Lam, K. He, R. Knabb, 2009, Bioorganic & medicinal chemistry letters.

Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.

P. Lam, D. Cheney, K. He, 2008, Bioorganic & medicinal chemistry letters.

Sulfonamidolactam inhibitors of coagulation factor Xa.

P. Lam, R. Knabb, A. Rendina, 2008, Bioorganic & medicinal chemistry letters.

Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.

E. Liu, P. Stein, A. Rendina, 2005, Bioorganic & medicinal chemistry letters.

Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity.

A. Mathur, P. Morin, D. Seiffert, 2014, Journal of medicinal chemistry.

Apixaban inhibition of factor Xa: Microscopic rate constants and inhibition mechanism in purified protein systems and in human plasma

K. He, R. Knabb, A. Rendina, 2011, Journal of enzyme inhibition and medicinal chemistry.

Dethiobiotin synthetase: the carbonylation of 7,8-diaminonanoic acid proceeds regiospecifically via the N7-carbamate.

G. Lorimer, A. Nudelman, A. Rendina, 1995, Biochemistry.

Catalysis of the decomposition of hydrogen peroxide by a complex of iron(III) with a synthetic macrocyclic ligand

D. Busch, A. Rendina, N. Kildahl, 1979 .

Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.

S. Sheriff, D. Seiffert, A. Rendina, 2016, Bioorganic & medicinal chemistry.

DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors.

Deepak Bandyopadhyay, Lauren Dare, Michelle C. Schaeffer, 2016, Journal of medicinal chemistry.

Substrate synergism and the kinetic mechanism of yeast hexokinase.

F. Raushel, W. Cleland, R. Viola, 1982, Biochemistry.

Mechanisms of aldehyde-induced adenosinetriphosphatase activities of kinases.

W. Cleland, A. Rendina, 1984, Biochemistry.

The design and synthesis of inhibitors of dethiobiotin synthetase as potential herbicides

Y. Lindqvist, G. Lorimer, A. Nudelman, 1999 .

Mutant IDH1 enhances the production of 2-hydroxyglutarate due to its kinetic mechanism.

Nicholas D. Adams, S. Thrall, C. Duraiswami, 2013, Biochemistry.

A novel method for determining rate constants for dehydration of aldehyde hydrates.

W. Cleland, J. Hermes, A. Rendina, 1984, Biochemistry.

Glutamate synthase: on the kinetic mechanism of the enzyme from Escherichia coli W.

W. Orme-Johnson, A. Rendina, 1978, Biochemistry.

Use of multiple isotope effects to study the mechanism of 6-phosphogluconate dehydrogenase.

W. Cleland, J. Hermes, A. Rendina, 1984, Biochemistry.

Characterization of the inactivation of rat fatty acid synthase by C75: inhibition of partial reactions and protection by substrates.

A. Rendina, D. Cheng, 2005, The Biochemical journal.

Inhibition of acetyl-coenzyme A carboxylase by two classes of grass-selective herbicides

A. Rendina, Alan R. Rendina, Adrienne C. Craig-Kennard, 1990 .

Kinetic characterization, stereoselectivity, and species selectivity of the inhibition of plant acetyl-CoA carboxylase by the aryloxyphenoxypropionic acid grass herbicides.

A. Rendina, J. Hagenah, A. Craig-Kennard, 1988, Archives of biochemistry and biophysics.

Cyclohexanedione Herbicides Are Selective and Potent Inhibitors of Acetyl-CoA Carboxylase from Grasses.

A. Rendina, J. Felts, 1988, Plant physiology.

Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer

P. A. Harris, J. Bertin, M. Mahajan, 2019, ACS medicinal chemistry letters.

The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure.

Paul N. Mortenson, D. J. Price, L. Shewchuk, 2020, Bioorganic & medicinal chemistry.

Mechanism of an ATP-dependent carboxylase, dethiobiotin synthetase, based on crystallographic studies of complexes with substrates and a reaction intermediate.

G. Schneider, Y. Lindqvist, W. Huang, 1995, Biochemistry.

Characterization of 3-iron ferredoxins by means of the linear electric field effect in EPR.

H. Beinert, W. Orme-Johnson, N. Orme-Johnson, 1983, The Journal of biological chemistry.

Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.

S. Sheriff, P. Morin, D. Seiffert, 2015, Bioorganic & medicinal chemistry letters.

Discovery of a Novel 2,6-Disubstituted Glucosamine Series of Potent and Selective Hexokinase 2 Inhibitors.

Yong Jiang, Jacques Briand, Junya Qu, 2016, ACS medicinal chemistry letters.

Phosphorylated thiosugars: synthesis, properties, and reactivity in enzymatic reactions.

D. Sem, W. Cleland, H. Miziorko, 1991, Biochemistry.

Active site mutants of Escherichia coli dethiobiotin synthetase: effects of mutations on enzyme catalytic and structural properties.

Y. Lindqvist, K. Lohman, A. Rendina, 1997, Biochemistry.

The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors.

I. E. Smith, Paul N. Mortenson, D. J. Price, 2019, Bioorganic & medicinal chemistry.

Reverse Hydroxamate Inhibitors of Bone Morphogenetic Protein 1.

R. A. Reid, D. Holt, R. Gampe, 2018, ACS medicinal chemistry letters.

Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.

David S Nirschl, P. Lam, S. Sheriff, 2019, Bioorganic & medicinal chemistry letters.

BMS-593214, an active site-directed factor VIIa inhibitor: Enzyme kinetics, antithrombotic and antihaemostatic studies

R. Knabb, A. Rendina, B. Xin, 2017 .

Use of the kinetic equilibrium between aminoacyl-tRNA formation and hydrolysis in inhibition assays of aminoacyl-tRNA synthetase.

D. Jordan, L. Abell, A. Rendina, 2001, Analytical Biochemistry.

Determination of the screw sense specificity of bovine liver fructokinase.

W. Cleland, V. Pecoraro, A. Rendina, 1985, Biochemistry.

A human fatty acid synthase inhibitor binds β-ketoacyl reductase in the keto-substrate site.

Ramona N Plant, K. Brown, J. Briand, 2014, Nature chemical biology.