A. Gilbert

发表

3,5-Dioxopyrazolidines, Novel Inhibitors of UDP-N- Acetylenolpyruvylglucosamine Reductase (MurB) with Activity against Gram-Positive Bacteria

R. Chopra, K. Svenson, G. Krishnamurthy, 2006, Antimicrobial Agents and Chemotherapy.

Developing predictive assays: The phenotypic screening “rule of 3”

P. Loria, C. Steppan, Fabien Vincent, 2015, Science Translational Medicine.

Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes

Stephen Brown, R. Horst, Yilin Meng, 2020, Nature Chemical Biology.

Amphotericin B, identified from a natural product screen, antagonizes CNS inhibitors to promote axon growth via activation of an Akt pathway in neurons

Z. Cao, F. Walsh, P. Doherty, 2010, Journal of neurochemistry.

3-(Pyridin-2-yl-ethynyl)benzamide metabotropic glutamate receptor 5 negative allosteric modulators: hit to lead studies.

J. Dwyer, Z. Hughes, A. Gilbert, 2011, Bioorganic & medicinal chemistry letters.

Clearance Prediction of Targeted Covalent Inhibitors by In Vitro-In Vivo Extrapolation of Hepatic and Extrahepatic Clearance Mechanisms

M. Dowty, A. Thorarensen, C. Banfield, 2017, Drug Metabolism and Disposition.

Chiral Sulfoxide-Induced Single Turn Peptide α-Helicity

F. Jiang, David A. Price, S. Liras, 2016, Scientific Reports.

Recent advances in irreversible kinase inhibitors.

A. Gilbert, 2014, Pharmaceutical patent analyst.

Yeast-based screening for inhibitors of RGS proteins.

Seena K. Ajit, Yuren Wang, A. Gilbert, 2004, Methods in enzymology.

A kinetic proofreading model for bispecific protein degraders

D. Bartlett, A. Gilbert, 2020, Journal of pharmacokinetics and pharmacodynamics.

Translational PK-PD for targeted protein degradation.

D. Bartlett, A. Gilbert, 2022, Chemical Society reviews.

Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition.

J. Bauman, J. D. Clark, M. Hegen, 2016, ACS chemical biology.

Optimization of a Dicarboxylic Series for in Vivo Inhibition of Citrate Transport by the Solute Carrier 13 (SLC13) Family.

T. Rolph, M. Hayward, D. Erion, 2016, Journal of medicinal chemistry.

5'-Phenyl-3'H-spiro[indoline-3,2'-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (aggrecanase-2).

A. Gilbert, M. Bursavich, C. Flannery, 2007, Bioorganic & medicinal chemistry letters.

5-((1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5.

A. Gilbert, M. Bursavich, C. Flannery, 2007, Bioorganic & medicinal chemistry letters.

Synthetic studies towards the total synthesis of olivin: Synthesis of a fully functionalized alkyne appropriate for the benzannulation reaction

A. Gilbert, Ross A. Miller, W. Wulff, 1999 .

De novo synthesis of teleocidin B analogs

A. Gilbert, Kangwen Deng, J. Butera, 2010 .

N-((8-hydroxy-5-substituted-quinolin-7-yl)(phenyl)methyl)-2-phenyloxy/amino-acetamide inhibitors of ADAMTS-5 (Aggrecanase-2).

A. Gilbert, M. Bursavich, C. Flannery, 2008, Bioorganic & medicinal chemistry letters.

Modulation of selective serotonin reuptake inhibitor and 5-HT1A antagonist activity in 8-aza-bicyclo[3.2.1]octane derivatives of 2,3-dihydro-1,4-benzodioxane.

R. Nilakantan, G. Stack, A. Gilbert, 2004, Bioorganic & medicinal chemistry letters.

Benchmarking in vitro covalent binding burden as a tool to assess potential toxicity caused by nonspecific covalent binding of covalent drugs.

R. Obach, A. Gilbert, Upendra P. Dahal, 2013, Chemical research in toxicology.

Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation.

Timothy L. Foley, J. Pandit, J. Cianfrogna, 2018, Journal of medicinal chemistry.

The effect of mGlu5 receptor positive allosteric modulators on signaling molecules in brain slices.

F. Liu, K. Marquis, M. Bowlby, 2006, European journal of pharmacology.

Hit to lead studies on (hetero)arylpyrimidines--agonists of the canonical Wnt-beta-catenin cellular messaging system.

John A. Robinson, Raymond J. Unwalla, G. Krishnamurthy, 2010, Bioorganic & medicinal chemistry letters.

Advances in the development of novel analgesics

W. Childers, A. Gilbert, J. Kennedy, 2008 .

Expedient parallel synthesis of 2-amino-4-heteroarylpyrimidines.

A. Gilbert, M. Bursavich, S. Lombardi, 2005, Organic letters.

Novel aryloxy-8-azabicyclo[3.2.1]oct-3-enes with 5-HT transporter and 5-HT1A affinity.

T. Coleman, A. Gilbert, L. Schechter, 2004, Bioorganic & medicinal chemistry letters.

Pyrazolidine-3,5-diones and 5-hydroxy-1H-pyrazol-3(2H)-ones, inhibitors of UDP-N-acetylenolpyruvyl glucosamine reductase.

Youjun Yang, A. Severin, Guy Singh, 2006, Journal of medicinal chemistry.

Novel benzofuran-3-one indole inhibitors of PI3 kinase-alpha and the mammalian target of rapamycin: hit to lead studies.

N. Brooijmans, Steven C. Kim, L. Feldberg, 2010, Bioorganic & medicinal chemistry letters.

Novel purine and pyrazolo[3,4-d]pyrimidine inhibitors of PI3 kinase-alpha: Hit to lead studies.

N. Brooijmans, Steven C. Kim, L. Feldberg, 2010, Bioorganic & medicinal chemistry letters.

Pyrazolopyrimidine-2,4-dione sulfonamides: novel and selective calcitonin inducers.

J. Ellingboe, F. Koehn, A. Gilbert, 2002, Journal of medicinal chemistry.

Reactions of Group 6 Fischer carbene complexes with alkynes: effect of the metal on the product distribution and the isolation of a nontautomerized cyclohexadienone complex

J. Clardy, R. Hsung, J. Mitchell, 1994 .

Synthesis and evaluation of aryl thioxothiazolidinone inhibitors of ADAMTS-5 (Aggrecanase-2).

A. Gilbert, M. Bursavich, C. Flannery, 2007, Bioorganic & medicinal chemistry letters.

(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate.

Raymond J. Unwalla, P. Bodine, R. Magolda, 2009, Journal of medicinal chemistry.

PALLADIUM-CATALYZED CROSS-COUPLING OF ARENE-CHROMIUM TRICARBONYL TRIFLATE COMPLEXES

A. Gilbert, W. Wulff, 1994 .

Biphenyl-bridged metallocenes that are chiral, configurationally stable, and free of diastereomers

A. Gilbert, T. J. Katz, H. Brintzinger, 1992 .

Metal-Catalyzed Cyclopropene Rearrangements for Benzannulation: Evaluation of an Anthraquinone Synthesis Pathway and Reevaluation of the Parallel Approach via Carbene-Chromium Complexes

M. Steigerwald, A. Gilbert, R. Ball, 1994 .

Synthesis and properties of an optically active helical bis-cobaltocenium ion

A. Rheingold, A. Gilbert, T. J. Katz, 1993 .

Synthesis and Properties of Optically Active Helical Metallocene Oligomers

M. Ward, A. Gilbert, T. J. Katz, 1993 .

1-(2-Hydroxy-2-methyl-3-phenoxypropanoyl)indoline-4-carbonitrile derivatives as potent and tissue selective androgen receptor modulators.

D. Powell, P. Verhoest, S. Nagpal, 2014, Journal of medicinal chemistry.

PHENOL FORMATION FROM THE REACTIONS OF AMINO-STABILIZED ALKENYL FISCHER CARBENE COMPLEXES

R. Hsung, A. Gilbert, W. Wulff, 1995 .

Palladium-catalyzed coupling of 2,2tdihalobiaryls with metallated cyclopentenes. An easy synthesis for spiro[cyclopentene-1,9−[9H]fluorene]s

A. Gilbert, T. J. Katz, H. Brintzinger, 1993 .

Design and SAR of novel potassium channel openers targeted for urge urinary incontinence. 2. Selective and potent benzylamino cyclobutenediones.

A. Gilbert, G. Francisco, T. Argentieri, 2000, Journal of medicinal chemistry.

Know your target, know your molecule.

Mark E Bunnage, Erik C Hett, M. Bunnage, 2015, Nature chemical biology.

Delineating the role of cooperativity in the design of potent PROTACs for BTK

Graham M. West, James Smith, V. Shanmugasundaram, 2018, Proceedings of the National Academy of Sciences.

A roadmap to evaluate the proteome-wide selectivity of covalent kinase inhibitors

Benjamin F. Cravatt, Theodore O. Johnson, Matthew M. Hayward, 2014, Nature chemical biology.

Inducing protein-protein interactions with molecular glues.

V. Shanmugasundaram, Ye Che, A. Gilbert, 2018, Bioorganic & medicinal chemistry letters.

Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors.

R. Abraham, N. Brooijmans, L. Feldberg, 2010, Bioorganic & medicinal chemistry letters.

Targeted Covalent Enzyme Inhibitors

A. Gilbert, M. C. Noe, 2012 .

The Metabotropic Glutamate Receptor 7 Allosteric Modulator AMN082: A Monoaminergic Agent in Disguise?

J. Dwyer, L. Di, A. Randall, 2011, Journal of Pharmacology and Experimental Therapeutics.

Old and New Pharmacology: Positive Allosteric Modulation of the α 7 Nicotinic Acetylcholine Receptor by the 5-HT 2B/C Receptor Antagonist SB-206553

S. Grauer, Jon T. Brown, A. Randall, 2008 .

Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans.

M. Hegen, J. Telliez, J. Chrencik, 2017, Journal of medicinal chemistry.

Structure-Based Approach To Identify 5-[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators.

K. Parris, D. Powell, S. Nagpal, 2017, Journal of medicinal chemistry.

Prodrugs of CL316243: a selective beta3-adrenergic receptor agonist for treating obesity and diabetes.

M. Malamas, Z. Chen, J. Ellingboe, 1999, Bioorganic & medicinal chemistry letters.

Anthranilate 4H-oxazol-5-ones: novel small molecule antibacterial acyl carrier protein synthase (AcpS) inhibitors.

D. Joseph-McCarthy, C. Fritz, I. McFadyen, 2004, Bioorganic & medicinal chemistry letters.

ADX47273 [S-(4-Fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl}-methanone]: A Novel Metabotropic Glutamate Receptor 5-Selective Positive Allosteric Modulator with Preclinical Antipsychotic-Like and Procognitive Activities

F. Liu, M. Day, T. Comery, 2008, Journal of Pharmacology and Experimental Therapeutics.

High-Throughput Screening for the Discovery of Inhibitors of Fatty Acid Amide Hydrolase Using a Microsome-Based Fluorescent Assay

G. Krishnamurthy, Yuren Wang, A. Gilbert, 2006, Journal of biomolecular screening.

Intrinsic reactivity profile of electrophilic moieties to guide covalent drug design: N-α-acetyl-L-lysine as an amine nucleophile

R. Obach, A. Gilbert, M. Flanagan, 2016 .

Chemical and computational methods for the characterization of covalent reactive groups for the prospective design of irreversible inhibitors.

G. S. Walker, V. Shanmugasundaram, R. Obach, 2014, Journal of medicinal chemistry.

Use of structure-based drug design approaches to obtain novel anthranilic acid acyl carrier protein synthase inhibitors.

Dominick Quagliato, Diane Joseph-McCarthy, Elena Severina, 2005, Journal of medicinal chemistry.

Discovery and characterization of novel potent PARP-1 inhibitors endowed with neuroprotective properties: From TIQ-A to HYDAMTIQ

Gabriele Costantino, Emidio Camaioni, Andrea Carotti, 2011 .

Discovery of a Selective Covalent Inhibitor of Lysophospholipase-like 1 (LYPLAL1) as a Tool to Evaluate the Role of this Serine Hydrolase in Metabolism.

K. Fennell, J. Pandit, K. Parris, 2016, ACS chemical biology.

Azaindolines: derisking the indoline structural alert

P. Verhoest, A. Gilbert, Raghuram S. Tangirala, 2012 .

Amphotericin B, identified from a natural product screen, antagonizes CNS inhibitors to promote axon growth via activation of an Akt pathway in neurons

F. Walsh, P. Doherty, F. Koehn, 2010, Journal of neurochemistry.

Chemical and computational methods for the characterization of covalent reactive groups for the prospective design of irreversible inhibitors.

G. S. Walker, V. Shanmugasundaram, M. Hayward, 2014, Journal of medicinal chemistry.

Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors.

R. Abraham, N. Brooijmans, R. Mallon, 2010, Bioorganic & medicinal chemistry letters.