G. Sheppard

发表

Discovery of Potent Nonpeptide Inhibitors of Stromelysin Using SAR by NMR

Jean M. Severin, S. Davidsen, P. Hajduk, 1997 .

Methionine Aminopeptidase 2 Inhibition Is an Effective Treatment Strategy for Neuroblastoma in Preclinical Models

Scott A. Erickson, J. Maris, Jieyi Wang, 2005, Clinical Cancer Research.

Studies directed toward the total synthesis of lonomycin A (emericid). Asymmetric synthesis of the C1-C11 synthon

Davidr . Evans, G. Sheppard, D. A. Evans, 1990 .

Total Synthesis of the Polyether Antibiotic Lonomycin A (Emericid)

Davidr . Evans, G. Sheppard, B. Huff, 1995 .

Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists.

S. Davidsen, P. Tapang, D. Albert, 1998, Journal of Medicinal Chemistry.

Mild alcohol methylation procedure for the synthesis of polyoxygenated natural products. Applications to the synthesis of lonomycin A

Davidr . Evans, G. Sheppard, B. Huff, 1994 .

Reversal of oncogene transformation and suppression of tumor growth by the novel IGF1R kinase inhibitor A-928605

S. Davidsen, Eric F. Johnson, N. Soni, 2009, BMC Cancer.

Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies.

L. Lam, Xin Lu, S. Rosenberg, 2017, Cancer research.

Electrospray tandem mass spectrometric measurements of organotin compounds

J. Banoub, G. Sheppard, H. J. Hodder, 2004 .

Electrospray tandem mass-spectrometric analysis of diastereo- and stereoisomeric pyrimidine nucleoside analogues based on the 1,3-dihydrobenzo[c]furan core

C. Len, J. Banoub, G. Mackenzie, 2003 .

Structural Characterization of Intact Covalently Linked DNA Adducts by Electrospray Mass Spectrometry

G. Sheppard, H. J. Hodder, J. Miller-Banoub, 1999 .

Correlation of tumor growth suppression and methionine aminopetidase-2 activity blockade using an orally active inhibitor

Qian Zhang, L. Tucker, Jieyi Wang, 2008, Proceedings of the National Academy of Sciences.

Analyzing the binding of Co(II)-specific inhibitors to the methionyl aminopeptidases from Escherichia coli and Pyrococcus furiosus

Jieyi Wang, G. Sheppard, S. Mitra, 2009, JBIC Journal of Biological Inorganic Chemistry.

Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding.

Scott A. Erickson, S. Davidsen, A. Petros, 2006, Journal of medicinal chemistry.

Acetamido-group participation in lysozyme catalysis

G. Lowe, G. Sheppard, 1968 .

Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

L. Lam, Chaohong Sun, S. Rosenberg, 2020, Nature.

The role of platelet-activating factor (PAF) and the efficacy of ABT-491, a highly potent and selective PAF antagonist, in experimental allergic rhinitis.

S. Davidsen, C. Wegner, P. Tapang, 1998, The Journal of pharmacology and experimental therapeutics.

Pharmacology of ABT-491, a highly potent platelet-activating factor receptor antagonist.

S. Davidsen, P. Tapang, D. Albert, 1997, European journal of pharmacology.

Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.

Chaohong Sun, L. Hasvold, Chang H. Park, 2017, Journal of Medicinal Chemistry.

3-(2-(3-Pyridinyl)thiazolidin-4-oyl)indoles, a novel series of platelet activating factor antagonists.

S. Davidsen, M. Bures, G. Sheppard, 1994, Journal of medicinal chemistry.

Discovery of N-ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET bromodomain inhibitor with selectivity for the second bromodomain.

K. Longenecker, P. Kovar, L. Hasvold, 2020, Journal of medicinal chemistry.

Evaluation of the inhibition of other metalloproteinases by matrix metalloproteinase inhibitors.

S. Davidsen, D. Albert, M. Curtin, 1999, Journal of enzyme inhibition.

Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax)

C. Tse, D. Anderson, Daniel J. Anderson, 2015, Cell Death and Disease.

Correction to Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity.

Scott A. Erickson, C. Tse, A. Petros, 2015, Journal of medicinal chemistry.

Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.

S. Davidsen, Eric F. Johnson, J. Wilsbacher, 2010, Bioorganic & medicinal chemistry letters.

Physiologically relevant metal cofactor for methionine aminopeptidase-2 is manganese.

D. Egan, Chang H. Park, J. Henkin, 2003, Biochemistry.

Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.

Scott A. Erickson, K. Comess, A. Vasudevan, 2006, Bioorganic & medicinal chemistry letters.

Lysyl 4-aminobenzoic acid derivatives as potent small molecule mimetics of plasminogen kringle 5.

J. Henkin, D. Davidson, G. Sheppard, 2004, Bioorganic & medicinal chemistry letters.

Pyrazolo[3,4-d]pyrimidines as potent inhibitors of the insulin-like growth factor receptor (IGF-IR).

S. Davidsen, Eric F. Johnson, J. Wilsbacher, 2007, Bioorganic & medicinal chemistry letters.

3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2.

Scott A. Erickson, Jyoti R. Patel, Chang H. Park, 2004, Bioorganic & medicinal chemistry letters.

Copper(II) Pivalate/Oxone: An Improved Promoter System for Aryl Transfer via Organo-Bismuth Reagents

G. Sheppard, 1999 .

Enamine chemistry. Part XIV. Reaction of αβ-unsaturated acid chlorides with tertiary enamino-ketones and -esters

P. Hickmott, G. Sheppard, 1972 .

Enamine chemistry. Part XVII. Reaction of αβ-unsaturated acid chlorides with enamines. Further mechanistic investigations. Effect of triethylamine on the reaction path

P. Hickmott, G. Sheppard, R. Urbani, 1973 .

Enamine chemistry. Part XVI. Reaction of αβ-unsaturated acid chlorides with 1,4-dimorpholinocyclohexa-1,3-diene. Synthesis of 7-morpholino- and 4,7-dimorpholino-indan-1-ones

P. Hickmott, G. Sheppard, B. Hopkins, 1972 .

Diastereoselective aldol reactions using .beta.-keto imide derived enolates. A versatile approach to the assemblage of polypropionate systems

Davidr . Evans, G. Sheppard, J. S. Clark, 1990 .

Enamine chemistry. Part XIII. Reaction of αβ-unsaturated acid chlorides with primary and secondary enamines. Synthesis of tetrahydro-2-oxopyridines and octahydro-2-oxoquinolines

P. Hickmott, G. Sheppard, 1971 .

Cobalt-mediated [2 + 2 + 2] cycloadditions of alkynes to the pyrrole 2,3-double bond: novel construction of fused dihydroindoles

K. Vollhardt, G. Sheppard, 1986 .

Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids.

Gary T. Wang, Chang H. Park, Jieyi Wang, 2007, Bioorganic & medicinal chemistry letters.

Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.

A. Petros, Chaohong Sun, P. Kovar, 2017, Journal of medicinal chemistry.

Enamine chemistry. Part XI. Reaction of αβ-unsaturated acids and acid chlorides with imines. Synthesis of 2-oxotetrahydropyridines and 2-oxo-octahydroquinolines

P. Hickmott, G. Sheppard, 1971 .

Electrospray tandem mass-spectrometric analysis of diastereo- and stereoisomeric pyrimidine nucleoside analogues based on the 1,3-dihydrobenzo[c]furan core.

C. Len, J. Banoub, G. Mackenzie, 2003, Carbohydrate research.

Synthesis of 6- and 7-Arylindoles via Palladium-Catalyzed Cross-Coupling of 6- and 7-Bromoindole with Arylboronic Acids

G. Sheppard, G. M. Carrera, 1994 .

Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.

S. Davidsen, D. Albert, J. Summers, 1998, Bioorganic & medicinal chemistry letters.

Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity.

Scott A. Erickson, C. Tse, A. Petros, 2015, Journal of medicinal chemistry.

Tumor suppression by a rationally designed reversible inhibitor of methionine aminopeptidase-2.

Scott A. Erickson, J. Maris, Chang H. Park, 2003, Cancer research.

Ectopic expression of methionine aminopeptidase-2 causes cell transformation and stimulates proliferation

S. Davidsen, Qian Zhang, L. Tucker, 2008, Oncogene.

Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.

Scott A. Erickson, S. Davidsen, K. Swinger, 2010, Bioorganic & medicinal chemistry letters.

MCL-1 Is a Key Determinant of Breast Cancer Cell Survival: Validation of MCL-1 Dependency Utilizing a Highly Selective Small Molecule Inhibitor

Xin Lu, J. Leverson, W. N. Pappano, 2015, Molecular Cancer Therapeutics.

Why optimize cancer drugs for ADMET

G. Sheppard, J. Bouska, 2005 .

Transforming growth factor beta mimetics: discovery of 7-[4-(4-cyanophenyl)phenoxy]-heptanohydroxamic acid, a biaryl hydroxamate inhibitor of histone deacetylase.

K. Glaser, H. Moses, G. Sheppard, 2002, Molecular cancer therapeutics.

Discovery and optimization of indole pyrrolothiazole paf antagonists

S. Davidsen, P. Tapang, D. Albert, 1995 .

ChemInform Abstract: Discovery of Potent Nonpeptide Inhibitors of Stromelysin Using SAR by NMR.

Karl A. Walter, Jean M. Severin, Stephen W. Fesik, 1997 .

Methylpyrrole inhibitors of BET bromodomains.

A. Petros, Chaohong Sun, N. Soni, 2017, Bioorganic & medicinal chemistry letters.

Insulin-like Growth Factor-1 Receptor and ErbB Kinase Inhibitor Combinations Block Proliferation and Induce Apoptosis through Cyclin D1 Reduction and Bax Activation*

S. Davidsen, J. Wilsbacher, Gary T. Wang, 2008, Journal of Biological Chemistry.

Lysozyme-catalysed hydrolysis of some β-aryl di-N-acetylchitobiosides

M. Sinnott, G. Lowe, G. Sheppard, 1967 .

Development of multitargeted inhibitors of both the insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor family of receptor tyrosine kinases.

Scott A. Erickson, S. Davidsen, Eric F. Johnson, 2009, Bioorganic & medicinal chemistry letters.

Lysozyme-catalysed hydrolysis of some beta-aryl di-N-acetylchitobiosides.

M. Sinnott, G. Lowe, G. Sheppard, 1967, The Biochemical journal.

Discovery, identification, and characterization of candidate pharmacodynamic markers of methionine aminopeptidase-2 inhibition.

S. Davidsen, P. Richardson, Qian Zhang, 2008, Journal of proteome research.

MCL-1 Is a Key Determinant of Breast Cancer Cell Survival: Validation of MCL-1 Dependency Utilizing a Highly Selective Small Molecule Inhibitor

Xin Lu, J. Leverson, S. Elmore, 2015, Molecular Cancer Therapeutics.

Correlation of tumor growth suppression and methionine aminopetidase-2 activity blockade using an orally active inhibitor

Qian Zhang, L. Tucker, Jieyi Wang, 2008, Proceedings of the National Academy of Sciences.

Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.

A. Petros, P. Kovar, Chang H. Park, 2017, Journal of medicinal chemistry.

Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors.

Ana L. Aguirre, A. Bogdan, Justin D Dietrich, 2018, Bioorganic & medicinal chemistry letters.

Methylpyrrole inhibitors of BET bromodomains.

A. Petros, N. Soni, P. Kovar, 2017, Bioorganic & medicinal chemistry letters.

Chang H. Park, D. Albert, Emily J. Faivre, 2017, Journal of medicinal chemistry.