H. Tecle

发表

The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901.

A. Doherty, J. Warmus, A. Bridges, 2008, Bioorganic & medicinal chemistry letters.

Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition

J. Warmus, J. Sebolt-Leopold, Chunhong Yan, 2004, Nature Structural &Molecular Biology.

Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo

Alan R. Saltiel, A. Bridges, W. Leopold, 1999, Nature Medicine.

Enhanced selectivity profile of pyrazole-urea based DFG-out p38alpha inhibitors.

S. Kazmirski, A. Cheng, F. Féru, 2010, Bioorganic & medicinal chemistry letters.

4-anilino-5-carboxamido-2-pyridone derivatives as noncompetitive inhibitors of mitogen-activated protein kinase kinase.

Daniel F Ortwine, J. A. Spicer, W. Denny, 2007, Journal of medicinal chemistry.

2-Alkylamino- and alkoxy-substituted 2-amino-1,3,4-oxadiazoles-O-Alkyl benzohydroxamate esters replacements retain the desired inhibition and selectivity against MEK (MAP ERK kinase).

J. Warmus, A. Bridges, W. Leopold, 2008, Bioorganic & medicinal chemistry letters.

Corrigendum: Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition

J. Warmus, J. Sebolt-Leopold, Chunhong Yan, 2005, Nature Structural &Molecular Biology.

Milameline (CI-979/RU35926): a muscarinic receptor agonist with cognition-activating properties: biochemical and in vivo characterization.

H. Tecle, R. Schwarz, J. Kinsora, 1999, The Journal of pharmacology and experimental therapeutics.

CI-1017, a functionally M1-selective muscarinic agonist: design, synthesis, and preclinical pharmacology.

M. Emmerling, S. Barrett, H. Tecle, 2000, Pharmaceutica acta Helvetiae.

Novel Muscarinic Agonists for the Treatment of Alzheimer’s Disease

D. T. Dudley, H. Tecle, W. Moos, 1991 .

The biological profile of PD 0325901: A second generation analog of CI-1040 with improved pharmaceutical potential

A. Bridges, W. Leopold, J. Sebolt-Leopold, 2004 .

Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents.

H. Tecle, L. Wise, D. A. Downs, 1985, Journal of medicinal chemistry.

4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: a novel class of compounds with central dopamine agonist properties.

T. Heffner, C. Humblet, H. Tecle, 1990, Journal of medicinal chemistry.

Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.

J. A. Spicer, P. Ellis, W. Denny, 2016, Journal of medicinal chemistry.

EFFICIENT SYNTHESIS OF EXO-1-AZABICYCLO[2.2.1]HEPTAN-3-OL

S. Barrett, H. Tecle, J. Jaén, 1997 .

N-(6,7-dichloro-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-N-alkylsulfonamides as peripherally restricted N-methyl-D-aspartate receptor antagonists for the treatment of pain.

B. Finzel, J. Brieland, S. Przybranowski, 2007, Bioorganic & Medicinal Chemistry Letters.

Development of M1 subtype selective muscarinic agonists for Alzheimer's disease: Translation of in vitro selectivity into in vivo efficacy

H. Tecle, J. Jaén, R. Davis, 1997 .

Mutations of aspartate 103 in the Hm2 receptor and alterations in receptor binding properties of muscarinic agonists.

H. Tecle, T. Mirzadegan, J. Jaén, 1995, Life sciences.

Chapter 54: Subtype selective muscarinic agonists: potential therapeutic agents for Alzheimer's disease

D. T. Dudley, H. Tecle, J. Jaén, 1993 .

Synthesis and SAR of bulky 1-azabicyclo[2.2.1]-3-one oximes as muscarinic receptor subtype selective agonists.

H. Tecle, T. Mirzadegan, W. Moos, 1993, Life sciences.

Characterization of muscarinic agonists in recombinant cell lines.

H. Tecle, J. Jaén, R. Davis, 1993, Life sciences.

A rationale for the design and synthesis of m1 selective muscarinic agonists.

H. Tecle, T. Mirzadegan, W. Moos, 1992 .

Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor

P. Ellis, A. Bridges, D. W. Fry, 2008, Molecular Cancer Therapeutics.

Central role of the MEK/ERK MAP kinase pathway in a mouse model of rheumatoid arthritis: potential proinflammatory mechanisms.

S. Barrett, D. T. Dudley, H. Tecle, 2007, Arthritis and rheumatism.

Effect of mutating aspart ate 103 to glutamate or asparagine in the Hm2 subtype on binding of agonists and antagonists of varied pKa and subtype selectivity

H. Tecle, R. Schwarz, A. Thomas, 1995 .

The Design, Synthesis and Potential Utility of Fluorescence Probes that Target DFG‐out Conformation of p38α for High Throughput Screening Binding Assay

S. Kazmirski, A. Cheng, Qing Cao, 2009, Chemical biology & drug design.

Cholinergic agents: effect of methyl substitution in a series of arecoline derivatives on binding to muscarinic acetylcholine receptors.

H. Tecle, W. Moos, R. Davis, 1992, Journal of Pharmacy and Science.

Beyond the MEK-pocket: can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK?

S. Kazmirski, J. Penzotti, H. Tecle, 2009, Bioorganic & medicinal chemistry letters.

Design and synthesis of m1-selective muscarinic agonists: (R)-(-)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3'-methoxyphenyl)-2-propynyl)oxime maleate (CI-1017), a functionally m1-selective muscarinic agonist.

M. Brann, S. Barrett, H. Tecle, 1998, Journal of medicinal chemistry.

Alkyl substituted 3-PPP derivatives. Synthesis and biological investigation

T. Heffner, H. Tecle, L. Wise, 1989 .

Alkyl Substituted 3-PPP Derivatives. Synthesis and Biological Investigation.

T. Heffner, H. Tecle, L. Wise, 1990 .

The Pharmacology of the Novel and Selective Sigma Ligand, PD 144418

T. Heffner, H. Tecle, H. Akunne, 1997, Neuropharmacology.

Subtype selective muscarinic agonists: potential therapeutic agents for Alzheimer's disease.

D. T. Dudley, H. Tecle, J. Jaén, 1993, Progress in brain research.

The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901.

J. Warmus, J. Sebolt-Leopold, A. Saltiel, 2008, Bioorganic & medicinal chemistry letters.