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Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2S,3R)‑N‑((S)‑3-(Cyclopent-1-en-1-yl)-1-((R)‑2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-((S)‑2-(2-morpholinoacetamido)propanamido)propenamide)

Journal of medicinal chemistry, 2018-12, Vol.61 (24), p.11127-11143

2018

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The role and significance of unconventional hydrogen bonds in small molecule recognition by biological receptors of pharmaceutical relevance

Current pharmaceutical design, 2007-12, Vol.13 (34), p.3476-3493

2007

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Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors

Bioorganic & medicinal chemistry letters, 2013-05, Vol.23 (10), p.3075-3080

2013

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Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors

Bioorganic & medicinal chemistry letters, 2013-05, Vol.23 (9), p.2743-2749

2013

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Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model

Bioorganic & medicinal chemistry letters, 2010-11, Vol.20 (21), p.6231-6236

2010

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Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor

Bioorganic & medicinal chemistry letters, 2011-03, Vol.21 (6), p.1838-1843

2011

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Antibody–Drug Conjugates (ADCs) Derived from Interchain Cysteine Cross-Linking Demonstrate Improved Homogeneity and Other Pharmacological Properties over Conventional Heterogeneous ADCs

Molecular pharmaceutics, 2015-11, Vol.12 (11), p.3986-3998

2015

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Biosynthetic studies on the α-glucosidase inhibitor acarbose: the chemical synthesis of isotopically labeled 2- epi-5- epi-valiolone analogs

Carbohydrate research, 2003-09, Vol.338 (20), p.2075-2082

2003

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Biosynthetic studies on the α-glucosidase inhibitor acarbose: the chemical synthesis of dTDP-4-amino-4,6-dideoxy-α- d-glucose

Carbohydrate research, 2002-02, Vol.337 (4), p.297-304

2002

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Application of the 2,5-Dimethylpyrrole Group as a New and Orthogonal Amine-Protecting Group in Oligosaccharide Synthesis

Journal of organic chemistry, 1998-07, Vol.63 (14), p.4570-4571

1998

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Trityl ethers in oligosaccharide synthesis: A novel strategy for the convergent assembly of oligosaccharides

Tetrahedron letters, 1997-05, Vol.38 (21), p.3773-3776

1997

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Biosynthesis of the Cyclitol Moiety of Pyralomicin 1a in Nonomuraea spiralis MI178-34F18

The Journal of Antibiotics, 2002/06/25, Vol.55(6), pp.578-584

2002

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Pharmacological inhibition of Polo Like Kinase 2 (PLK2) does not cause chromosomal damage or result in the formation of micronuclei

Toxicology and applied pharmacology, 2013-05, Vol.269 (1), p.1-7

2013

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Novel cinnoline-based inhibitors of LRRK2 kinase activity

Bioorganic & medicinal chemistry letters, 2013-01, Vol.23 (1), p.71-74

2013

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Discovery of ( R )-4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1 H -pyrazolo[4,3- c ]quinoline (ELND006) and ( R )-4-Cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2 H -pyrazolo[4,3- c ]quinoline (ELND007): Metabolically Stable γ-Secretase Inhibitors that Selectively Inhibit the Production of Amyloid-β over Notch

Journal of medicinal chemistry, 2013-07, Vol.56 (13), p.5261-5274

2013

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Discovery of (R)‑4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro‑1H‑pyrazolo[4,3‑c]quinoline (ELND006) and (R)‑4-Cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro‑2H‑pyrazolo[4,3‑c]quinoline (ELND007): Metabolically Stable γ‑Secretase Inhibitors that Selectively Inhibit the Production of Amyloid‑β over Notch

Journal of medicinal chemistry, 2013-07, Vol.56 (13), p.5261-5274

2013

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Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration

Bioorganic & medicinal chemistry letters, 2011-09, Vol.21 (18), p.5521-5527

2011

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Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration

Bioorganic & medicinal chemistry letters, 2011-01, Vol.21 (1), p.315-319

2011

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Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates

Bioorganic & medicinal chemistry letters, 2013-04, Vol.23 (7), p.2181-2186

2013

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Design, synthesis, and structure–activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline γ-secretase inhibitors

Bioorganic & medicinal chemistry letters, 2009-09, Vol.19 (17), p.4920-4923

2009

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Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: Prime side chromane-containing inhibitors

Bioorganic & medicinal chemistry letters, 2013-08, Vol.23 (16), p.4674-4679

2013

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Biosynthesis of the Cyclitol Moiety of Pyralomicin la in Nonomuraea spiralis MI178-34F18

Journal of antibiotics, 2002, Vol.55 (6), p.578-584

2002

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Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK

Bioorganic & medicinal chemistry letters, 2010-12, Vol.20 (24), p.7303-7307

2010

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Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2S,3R)‑N‑((S)‑3-(Cyclopent-1-en-1-yl)-1-((R)‑2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-((S)‑2-(2-morpholinoacetamido)propanamido)propenamide)

The role and significance of unconventional hydrogen bonds in small molecule recognition by biological receptors of pharmaceutical relevance

Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors

Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors

Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model

Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor

Antibody–Drug Conjugates (ADCs) Derived from Interchain Cysteine Cross-Linking Demonstrate Improved Homogeneity and Other Pharmacological Properties over Conventional Heterogeneous ADCs

Biosynthetic studies on the α-glucosidase inhibitor acarbose: the chemical synthesis of isotopically labeled 2- epi-5- epi-valiolone analogs

Biosynthetic studies on the α-glucosidase inhibitor acarbose: the chemical synthesis of dTDP-4-amino-4,6-dideoxy-α- d-glucose

Application of the 2,5-Dimethylpyrrole Group as a New and Orthogonal Amine-Protecting Group in Oligosaccharide Synthesis

Trityl ethers in oligosaccharide synthesis: A novel strategy for the convergent assembly of oligosaccharides

Biosynthesis of the Cyclitol Moiety of Pyralomicin 1a in Nonomuraea spiralis MI178-34F18

Pharmacological inhibition of Polo Like Kinase 2 (PLK2) does not cause chromosomal damage or result in the formation of micronuclei

Novel cinnoline-based inhibitors of LRRK2 kinase activity

Selective and Brain-Permeable Polo-like Kinase-2 (Plk-2) Inhibitors That Reduce [alpha]-Synuclein Phosphorylation in Rat Brain

Selective and Brain-Permeable Polo-like Kinase-2 (Plk-2) Inhibitors That Reduce α-Synuclein Phosphorylation in Rat Brain

Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration

Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration

Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates

Design, synthesis, and structure–activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline γ-secretase inhibitors

Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: Prime side chromane-containing inhibitors

Biosynthesis of the Cyclitol Moiety of Pyralomicin la in Nonomuraea spiralis MI178-34F18

Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK

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