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1.
Fragment-based screening by X-ray crystallography, MS and isothermal titration calorimetry to identify PNMT (phenylethanolamine N-methyltransferase) inhibitors.
Biochem J
; 431(1): 51-61, 2010 Oct 01.
Article
in English
| MEDLINE | ID: mdl-20642456
2.
Molecular recognition of physiological substrate noradrenaline by the adrenaline-synthesizing enzyme PNMT and factors influencing its methyltransferase activity.
Biochem J
; 422(3): 463-71, 2009 Aug 27.
Article
in English
| MEDLINE | ID: mdl-19570037
3.
Structure-Based Drug Design of Bisubstrate Inhibitors of Phenylethanolamine N-Methyltransferase Possessing Low Nanomolar Affinity at Both Substrate Binding Domains1.
J Med Chem
; 63(22): 13878-13898, 2020 11 25.
Article
in English
| MEDLINE | ID: mdl-33147410
4.
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.
Bioorg Med Chem
; 16(1): 542-59, 2008 Jan 01.
Article
in English
| MEDLINE | ID: mdl-18024134
5.
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.
J Med Chem
; 49(10): 2939-52, 2006 May 18.
Article
in English
| MEDLINE | ID: mdl-16686536
6.
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.
J Med Chem
; 49(18): 5424-33, 2006 Sep 07.
Article
in English
| MEDLINE | ID: mdl-16942016
7.
3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity.
J Med Chem
; 48(1): 134-40, 2005 Jan 13.
Article
in English
| MEDLINE | ID: mdl-15634007
8.
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.
J Med Chem
; 48(6): 1806-12, 2005 Mar 24.
Article
in English
| MEDLINE | ID: mdl-15771426
9.
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.
J Med Chem
; 47(18): 4483-93, 2004 Aug 26.
Article
in English
| MEDLINE | ID: mdl-15317460
10.
Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase.
J Med Chem
; 47(1): 37-44, 2004 Jan 01.
Article
in English
| MEDLINE | ID: mdl-14695818
11.
Exploring the active site of phenylethanolamine N-methyltransferase with 1,2,3,4-tetrahydrobenz[h]isoquinoline inhibitors.
Bioorg Med Chem
; 15(3): 1298-310, 2007 Feb 01.
Article
in English
| MEDLINE | ID: mdl-17126018
12.
Inhibitors of phenylethanolamine N-methyltransferase devoid of alpha2-adrenoceptor affinity.
Bioorg Med Chem Lett
; 15(23): 5319-23, 2005 Dec 01.
Article
in English
| MEDLINE | ID: mdl-16169723
13.
Exploring the active site of phenylethanolamine N-methyltransferase: 3-alkyl-7-substituted-1,2,3,4-tetrahydroisoquinoline inhibitors.
Bioorg Med Chem
; 13(4): 1261-73, 2005 Feb 15.
Article
in English
| MEDLINE | ID: mdl-15670935
14.
Exploring the active site of phenylethanolamine N-methyltransferase with 3-hydroxyethyl- and 3-hydroxypropyl-7-substituted-1,2,3,4-tetrahydroisoquinolines.
Bioorg Med Chem Lett
; 15(4): 1143-7, 2005 Feb 15.
Article
in English
| MEDLINE | ID: mdl-15686930
15.
Phenylethanolamine N-methyltransferase inhibition: re-evaluation of kinetic data.
Bioorg Med Chem Lett
; 14(16): 4217-20, 2004 Aug 16.
Article
in English
| MEDLINE | ID: mdl-15261273
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