K. R. Criscione

发表

Application of the Goldilocks effect to the design of potent and selective inhibitors of phenylethanolamine N-methyltransferase: balancing pKa and steric effects in the optimization of 3-methyl-1,2,3,4-tetrahydroisoquinoline inhibitors by beta-fluorination.

Mitchell R Seim, G. L. Grunewald, Jian Lu, 2006, Journal of medicinal chemistry.

Exploring the active site of phenylethanolamine N-methyltransferase with 1,2,3,4-tetrahydrobenz[h]isoquinoline inhibitors.

Mitchell R Seim, Rachel C Regier, G. L. Grunewald, 2007, Bioorganic & medicinal chemistry.

Synthesis and evaluation of 3-trifluoromethyl-7-substituted-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.

G. L. Grunewald, T. Caldwell, K. R. Criscione, 1999, Journal of medicinal chemistry.

Effects of a 3-alkyl-, 4-hydroxy- and/or 8-aromatic-substituent on the phenylethanolamine N-methyltransferase inhibitor potency and alpha2-adrenoceptor affinity of 2,3,4,5-tetrahydro-1H-2-benzazepines.

G. L. Grunewald, V. Dahanukar, K. R. Criscione, 2001, Bioorganic & medicinal chemistry.

Synthesis and Evaluation of 4-Fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor.

G. L. Grunewald, T. Caldwell, Qifang Li, 2001 .

1,3-Dimethyl-7-substituted-1,2,3,4-tetrahydroisoquinolines as probes for the binding orientation of tetrahydroisoquinoline at the active site of phenylethanolamine N-methyltransferase.

G. L. Grunewald, T. Caldwell, K. R. Criscione, 1999, Bioorganic & medicinal chemistry.

Structure-Based Drug Design of Bisubstrate Inhibitors of Phenylethanolamine N-Methyltransferase Possessing Low Nanomolar Affinity at Both Substrate Binding Domains1.

M. McLeish, E. Scott, G. L. Grunewald, 2020, Journal of medicinal chemistry.

Synthesis of 4,5,6,7-tetrahydrothieno[3,2-c]pyridines and comparison with their isosteric 1,2,3,4-tetrahydroisoquinolines as inhibitors of phenylethanolamine N-methyltransferase.

Mitchell R Seim, G. L. Grunewald, K. R. Criscione, 2008, Bioorganic & medicinal chemistry.

Inhibitors of phenylethanolamine N-methyltransferase devoid of alpha2-adrenoceptor affinity.

Cosmas O. Okoro, G. L. Grunewald, Jian Lu, 2005, Bioorganic & medicinal chemistry letters.

Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase.

Christine L Gee, Jennifer L. Martin, C. Gee, 2006, Journal of medicinal chemistry.

Synthesis and Biochemical Evaluation of 3-Fluoromethyl-1,2,3,4-tetrahydroisoquinolines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor1

R. Borchardt, G. L. Grunewald, Wen Wang, 1999 .

Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase.

G. L. Grunewald, V. Dahanukar, K. R. Criscione, 1996, Journal of medicinal chemistry.

3,7-Disubstituted-1,2,3,4-tetrahydroisoquinolines display remarkable potency and selectivity as inhibitors of phenylethanolamine N-methyltransferase versus the alpha2-adrenoceptor.

G L Grunewald, V H Dahanukar, B Teoh, 1999, Journal of medicinal chemistry.

Molecular recognition of physiological substrate noradrenaline by the adrenaline-synthesizing enzyme PNMT and factors influencing its methyltransferase activity.

Munish Puri, Christine L Gee, Jennifer L. Martin, 2009, The Biochemical journal.

Fragment-based screening by X-ray crystallography, MS and isothermal titration calorimetry to identify PNMT (phenylethanolamine N-methyltransferase) inhibitors.

Hoan Vu, Sally-Ann Poulsen, Thomas E Prisinzano, 2010, The Biochemical journal.

Enantiospecific synthesis of 3-fluoromethyl-, 3-hydroxymethyl-, and 3-chloromethyl-1,2,3,4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.

G. L. Grunewald, T. Caldwell, V. Dahanukar, 1999, Journal of medicinal chemistry.

Comparative molecular field analysis (CoMFA) models of phenylethanolamine N-methyltransferase (PNMT) and the alpha2-adrenoceptor: the development of new, highly selective inhibitors of PNMT.

G. L. Grunewald, T. Caldwell, V. Dahanukar, 1999, Bioorganic & medicinal chemistry letters.

Exploring the active site of phenylethanolamine N-methyltransferase with 3-hydroxyethyl- and 3-hydroxypropyl-7-substituted-1,2,3,4-tetrahydroisoquinolines.

D. Bylund, F. A. Romero, Mitchell R Seim, 2005, Bioorganic & medicinal chemistry letters.

Examination of the role of the acidic hydrogen in imparting selectivity of 7-(aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) toward inhibition of phenylethanolamine N-methyltransferase vs the alpha 2-adrenoceptor.

G. L. Grunewald, T. Caldwell, V. Dahanukar, 1997, Journal of Medicinal Chemistry.

Phenylethanolamine N-methyltransferase kinetics: bovine versus recombinant human enzyme.

M. McLeish, G. L. Grunewald, K. R. Criscione, 2001, Bioorganic & medicinal chemistry letters.

Exploring the active site of phenylethanolamine N-methyltransferase: 3-alkyl-7-substituted-1,2,3,4-tetrahydroisoquinoline inhibitors.

F. A. Romero, G. L. Grunewald, K. R. Criscione, 2005, Bioorganic & medicinal chemistry.

Phenylethanolamine N-methyltransferase inhibition: re-evaluation of kinetic data.

M. McLeish, G. L. Grunewald, Qian Wu, 2004, Bioorganic & medicinal chemistry letters.

Nanomolar inhibitors of CNS epinephrine biosynthesis: (R)-(+)-3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines as potent and highly selective inhibitors of phenylethanolamine N-methyltransferase1.

F. A. Romero, G. L. Grunewald, K. R. Criscione, 2005, Journal of medicinal chemistry.

Inhibitors of phenylethanolamine N-methyltransferase that are predicted to penetrate the blood-brain barrier: design, synthesis, and evaluation of 3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines that possess low affinity toward the alpha2-adrenoceptor.

F. A. Romero, M. McLeish, G. L. Grunewald, 2004, Journal of medicinal chemistry.

Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase.

Jennifer L. Martin, J. Archbold, M. McLeish, 2004, Journal of medicinal chemistry.