M. Mckinnon

发表

Oxysterols are agonist ligands of RORγt and drive Th17 cell differentiation

A. Bittner, Jiejun Wu, T. Rao, 2014, Proceedings of the National Academy of Sciences.

Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor.

James Lin, K. McIntyre, D. Shuster, 2015, Journal of medicinal chemistry.

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.

Functional T Cells Phosphodiesterase 7 A-Deficient Mice Have

Nadler, K. McIntyre, W. Pitts, 2003 .

Phosphodiesterase 7A-Deficient Mice Have Functional T Cells

K. McIntyre, S. Nadler, W. Pitts, 2003, The Journal of Immunology.

A potent dimeric peptide antagonist of interleukin-5 that binds two interleukin-5 receptor alpha chains.

E. Whitehorn, R. Barrett, P. Schatz, 2000, Proceedings of the National Academy of Sciences of the United States of America.

Identification of potent pyrimidine inhibitors of phosphodiesterase 7 (PDE7) and their ability to inhibit T cell proliferation.

J. Barrish, S. Nadler, W. Pitts, 2009, Bioorganic & medicinal chemistry letters.

Co-stimulatory molecules as therapeutic targets in allergic airways disease

S. Nadler, J. Trzăskos, M. Mckinnon, 2007 .

Cytokine-Specific Transcriptional Regulation Through an IL-5Rα Interacting Protein

John Armstrong, P. Coffer, L. Koenderman, 2001, Science.

An Interleukin 5 Mutant Distinguishes between Two Functional Responses in Human Eosinophils

R. Solari, I. Uings, A. Proudfoot, 1997, The Journal of experimental medicine.

Modified peptide antagonists of interleukin 5 exhibit extended in vivo persistence but restricted species specificity.

A. Beresford, R. Barrett, I. Uings, 2001, Cytokine.

INTERLEUKIN-5 AND THE INTERLEUKIN-5 RECEPTOR : TARGETS FOR DRUG DISCOVERY IN ASTHMA

R. Solari, M. Mckinnon, M. Banks, 1999 .

Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.

David S. Nirschl, David S Nirschl, Sidney Pitt, 2014, Bioorganic & medicinal chemistry letters.

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.

Identification of Key Charged Residues of Human Interleukin-5 in Receptor Binding and Cellular Activation (*)

M. Peitsch, R. Solari, A. Proudfoot, 1995, The Journal of Biological Chemistry.

Spatial Orientation of the α and βc Receptor Chain Binding Sites on Monomeric Human Interleukin-5 Constructs*

M. Peitsch, M. Edgerton, I. Uings, 1997, The Journal of Biological Chemistry.

Development of IL-5 receptor antagonists.

I. Uings, M. Mckinnon, 2002, Current pharmaceutical design.

The carboxy-terminal region of human interleukin-5 is essential for maintenance of tertiary structure but not for dimerization

M. Peitsch, S. Brown, R. Solari, 1996, Journal of protein chemistry.

Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase.

S. Spergel, R. Moquin, K. McIntyre, 2009, Bioorganic & medicinal chemistry letters.

A CCR2/CCR5-dual antagonist, BMS-A, offers a potential novel oral therapy for the treatment of autoimmune disease (92.6)

K. McIntyre, J. Barrish, S. Mandlekar, 2009, Journal of Immunology.

Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).

David S. Nirschl, David S Nirschl, Michael A. Galella, 2011, Bioorganic & medicinal chemistry letters.

Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.

David S. Nirschl, David S Nirschl, S. Spergel, 2011, Bioorganic & medicinal chemistry letters.

Defining the Regions of Human Interleukin‐5 Important in Receptor Binding and Cellular Activation

R. Solari, A. Proudfoot, T. Wells, 1996, Annals of the New York Academy of Sciences.

Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors.

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

Benzothiazole based inhibitors of p38alpha MAP kinase.

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

A collaborative hit-to-lead investigation leveraging medicinal chemistry expertise with high throughput library design, synthesis and purification capabilities.

X Yang, D Parker, L Whitehead, 2006, Combinatorial chemistry & high throughput screening.

Design of LFA-1 antagonists based on a 2,3-dihydro-1H-pyrrolizin-5(7aH)-one scaffold.

J. Barrish, S. Sheriff, M. Poss, 2007, Bioorganic & medicinal chemistry letters.

An LFA-1 (αLβ2) Small-Molecule Antagonist Reduces Inflammation and Joint Destruction in Murine Models of Arthritis

P. M. Davis, K. McIntyre, D. Shuster, 2010, The Journal of Immunology.

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.

Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinic acid (BMS-688521).

P. M. Davis, K. McIntyre, J. Barrish, 2010, Journal of medicinal chemistry.

A new siglec family member, siglec-10, is expressed in cells of the immune system and has signaling properties similar to CD33.

K. Cheng, W. P. Yang, H. Chang, 2001, European journal of biochemistry.

Discovery and development of 5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl-methyl]-3-thiophenecarboxylic acid (BMS-587101)--a small molecule antagonist of leukocyte function associated antigen-1.

P. M. Davis, V. Goldfarb, D. Cheney, 2006, Journal of medicinal chemistry.

Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds.

David S. Nirschl, David S Nirschl, Arthur M Doweyko, 2007, Bioorganic & medicinal chemistry letters.

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.

A comparison of demethoxyviridin and wortmannin as inhibitors of phosphatidylinositol 3‐kinase

M. Waterfield, P. Parker, T. Kodaki, 1994, FEBS letters.

Novel tricyclic inhibitors of IKK2: Discovery and SAR leading to the identification of 2-methoxy- N-

David S Nirschl, Michael A. Galella, S. Spergel, 2012 .

Novel tricyclic inhibitors of IkappaB kinase.

David S Nirschl, S. Spergel, R. Moquin, 2009, Journal of medicinal chemistry.

Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.

S. Spergel, R. Moquin, K. McIntyre, 2016, Journal of medicinal chemistry.

Synthesis and evaluation of carbamoylmethylene linked prodrugs of BMS-582949, a clinical p38α inhibitor.

Michael A. Galella, James Lin, G. Schieven, 2013, Bioorganic & Medicinal Chemistry Letters.

Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1).

S. Spergel, K. McIntyre, D. Shuster, 2016, Bioorganic & medicinal chemistry letters.

The shared susceptibility epitope of HLA-DR4 binds citrullinated self-antigens and the TCR

Jia Jia Lim, J. Rossjohn, A. Purcell, 2021, Science Immunology.

Phospholipase-D activation can be negatively regulated through the action of protein kinase C.

P. Parker, M. Mckinnon, 1994, Biochimica et biophysica acta.

A MURINE MODEL OF CIGARETTE SMOKE-INDUCED PULMONARY INFLAMMATION USING INTRANASALLY ADMINISTERED SMOKE-CONDITIONED MEDIUM

D. Dambach, L. Killar, M. Mckinnon, 2002, Experimental lung research.

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.