S. E. Kiefer

发表

Characterization of a 78-residue fragment of c-Raf-1 that comprises a minimal binding domain for the interaction with Ras-GTP.

A. Neri, J. E. Losardo, D. Waugh, 1994, The Journal of biological chemistry.

Assessing compound binding to the Eg5 motor domain using a thermal shift assay.

M. Doyle, V. Goldfarb, W. Metzler, 2009, Analytical biochemistry.

Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors.

A. Doweyko, K. McIntyre, D. Shuster, 2011, Bioorganic & medicinal chemistry letters.

5-amino-pyrazoles as potent and selective p38α inhibitors.

A. Doweyko, R. Moquin, K. McIntyre, 2010, Bioorganic & medicinal chemistry letters.

Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.

A. Doweyko, R. Moquin, K. McIntyre, 2008, Bioorganic & medicinal chemistry letters.

Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis.

J. Barrish, D. Xie, N. Murugesan, 2020, ACS medicinal chemistry letters.

Crystal structure of microtubule affinity-regulating kinase 4 catalytic domain in complex with a pyrazolopyrimidine inhibitor.

J. Sack, Chunhong Yan, S. E. Kiefer, 2015, Acta crystallographica. Section F, Structural biology communications.

Cloning, purification, crystallization and preliminary X-ray analysis of the catalytic domain of human receptor-like protein tyrosine phosphatase γ in three different crystal forms.

V. Goldfarb, W. Metzler, K. Kish, 2011, Acta crystallographica. Section F, Structural biology and crystallization communications.

Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases.

A. Doweyko, James Lin, J. Wityak, 2010, Journal of medicinal chemistry.

The Crystal Structure of Abl Kinase with BMS-354825, a Dual SRC/ABL Kinase Inhibitor.

J. Tokarski, K. Kish, H. Klei, 2004 .

Crystallographic structures of the ligand-binding domains of the androgen receptor and its T877A mutant complexed with the natural agonist dihydrotestosterone

Howard M. Einspahr, Stanley R. Krystek, K. Kish, 2001, Proceedings of the National Academy of Sciences of the United States of America.

Benzothiazole based inhibitors of p38alpha MAP kinase.

A. Doweyko, James Lin, Sidney Pitt, 2008, Bioorganic & medicinal chemistry letters.

Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors.

John Dodd, John S Tokarski, Arthur M Doweyko, 2008, Journal of medicinal chemistry.

Bicyclic Heterocyclic Replacement of an Aryl Amide Leading to Potent and Kinase-Selective Adaptor Protein 2-Associated Kinase 1 Inhibitors.

Vijay T. Ahuja, J. Macor, S. E. Kiefer, 2022, Journal of medicinal chemistry.

Structural basis for the high-affinity binding of pyrrolotriazine inhibitors of p38 MAP kinase.

K. Kish, D. Xie, J. Sack, 2008, Acta Crystallographica Section D: Biological Crystallography.

Solution structure of the Ras-binding domain of c-Raf-1 and identification of its Ras interaction surface.

D. Fry, R. Palermo, V. Madison, 1995, Biochemistry.

The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode.

A. Doweyko, Sidney Pitt, M. Witmer, 2013, Bioorganic & medicinal chemistry letters.

Multiple and single binding modes of fragment-like kinase inhibitors revealed by molecular modeling, residue type-selective protonation, and nuclear overhauser effects.

Wayne Vaccaro, Luciano Mueller, K. Constantine, 2008, Journal of medicinal chemistry.

The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants.

M. Wittekind, J. Tokarski, K. Kish, 2006, Cancer research.

Discovery of BMS-986339, a Pharmacologically Differentiated Farnesoid X Receptor Agonist for the Treatment of Nonalcoholic Steatohepatitis.

S. E. Kiefer, J. Krupinski, Srinivas Cheruku, 2022, Journal of medicinal chemistry.

Discovery, Structure-Activity Relationships, and In Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2-Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain.

Vijay T. Ahuja, J. Macor, L. Bristow, 2021, Journal of medicinal chemistry.

Utilization of a nitrogen-sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase inhibitors.

A. Doweyko, Sidney Pitt, G. Schieven, 2010, Bioorganic & medicinal chemistry letters.

Small molecule receptor protein tyrosine phosphatase γ (RPTPγ) ligands that inhibit phosphatase activity via perturbation of the tryptophan-proline-aspartate (WPD) loop.

V. Goldfarb, B. Beno, J. Macor, 2011, Journal of medicinal chemistry.

Crystal structures of apo and inhibitor-bound TGFβR2 kinase domain: insights into TGFβR isoform selectivity.

D. Xie, S. Sheriff, Chunhong Yan, 2016, Acta crystallographica. Section D, Structural biology.

Time-resolved limited proteolysis of mitogen-activated protein kinase-activated protein kinase-2 determined by LC/MS only

M. Doyle, D. Xie, J. Bryson, 2008, Journal of the American Society for Mass Spectrometry.

The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.

A. Doweyko, K. McIntyre, D. Shuster, 2008, Bioorganic & medicinal chemistry letters.

Crystal structure of microtubule affinity-regulating kinase 4 catalytic domain in complex with a pyrazolopyrimidine inhibitor.

J. Sack, Chunhong Yan, S. E. Kiefer, 2015, Acta crystallographica. Section F, Structural biology communications.

The structure of human tau-tubulin kinase 1 both in the apo form and in complex with an inhibitor.

A. Cacace, D. Xie, Yaqun Zhang, 2014, Acta crystallographica. Section F, Structural biology communications.

A high-yield method to extract peptides from rat brain tissue.

G. Opiteck, J. Scheffler, S. E. Kiefer, 2003, Analytical biochemistry.