Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors

被引：150

作者：

Dales, NA

Gould, AE

Brown, JA

Calderwood, EF

Guan, B

Minor, CA

Gavin, JM

Hales, P

Kaushik, VK

Stewart, M

Tummino, PJ

Vickers, CS

Ocain, TD

Patane, MA

机构：

[1] Millennium Pharmaceut Inc, Med Chem, Cambridge, MA 02139 USA

[2] Millennium Pharmaceut Inc, Lead Discovery, Cambridge, MA 02139 USA

[3] Millennium Pharmaceut Inc, Biochem Enzymol, Cambridge, MA 02139 USA

来源：

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | 2002年 / 124卷 / 40期

关键词：

D O I：

10.1021/ja0277226

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Angiotensin-converting enzyme-related carboxypeptidase (ACE2) is a recently identified zinc metalloprotease with carboxypeptidase activity that was identified using our genomics platform. We implemented a rational design approach to identify potent and selective ACE2 inhibitors. To this end, picomolar inhibitors of ACE2 were designed and synthesized. Copyright © 2002 American Chemical Society.

引用

页码：11852 / 11853

页数：2

共 11 条

[1] Reductive amination of aldehydes and ketones with sodium triacetoxyborohydride. Studies on direct and indirect reductive amination procedures
AbdelMagid, AF
Carson, KG
Harris, BD
Maryanoff, CA
Shah, RD
[J]. JOURNAL OF ORGANIC CHEMISTRY, 1996, 61 (11) : 3849 - 3862
[2] Design and in vivo analysis of potent non-thiol inhibitors of farnesyl protein transferase
Anthony, NJ
Gomez, RP
Schaber, MD
Mosser, SD
Hamilton, KA
O'Neil, TJ
Koblan, KS
Graham, SL
Hartman, GD
Shah, D
Rands, E
Kohl, NE
Gibbs, JB
Oliff, AI
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (17) : 3356 - 3368
[3] SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF A NOVEL SERIES OF NONPEPTIDE ANGIOTENSIN-II RECEPTOR-BINDING INHIBITORS SPECIFIC FOR THE AT2 SUBTYPE
BLANKLEY, CJ
HODGES, JC
KLUTCHKO, SR
HIMMELSBACH, RJ
CHUCHOLOWSKI, A
CONNOLLY, CJ
NEERGAARD, SJ
VANNIEUWENHZE, MS
SEBASTIAN, A
QUIN, J
ESSENBURG, AD
COHEN, DM
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (11) : 3248 - 3260
[4] Synthesis and evaluation of deglycobleomycin A(2) analogues containing a tertiary N-methyl amide and simple ester replacement for the L-histidine secondary amide: Direct functional characterization of the requirement for secondary amide metal complexation
Boger, DL
Teramoto, S
Cai, H
[J]. BIOORGANIC & MEDICINAL CHEMISTRY, 1996, 4 (02) : 179 - 193
[5] BINDING OF BY-PRODUCT ANALOG BENZYLSUCCINIC ACID BY CARBOXYPEPTIDASE A
BYERS, LD
WOLFENDEN, R
[J]. BIOCHEMISTRY, 1973, 12 (11) : 2070 - 2078
[6] A novel angiotensin-converting enzyme-related carboxypeptidase (ACE2) converts angiotensin I to angiotensin 1-9
Donoghue, M
Hsieh, F
Baronas, E
Godbout, K
Gosselin, M
Stagliano, N
Donovan, M
Woolf, B
Robison, K
Jeyaseelan, R
Breitbart, RE
Acton, S
[J]. CIRCULATION RESEARCH, 2000, 87 (05) : E1 - E9
[7] DESIGN OF SPECIFIC INHIBITORS OF ANGIOTENSIN-CONVERTING ENZYME - NEW CLASS OF ORALLY ACTIVE ANTIHYPERTENSIVE AGENTS
ONDETTI, MA
CUSHMAN, DW
[J]. SCIENCE, 1977, 196 (4288) : 441 - 444
[8] PATCHETT AA, 1980, NATURE, V288, P280, DOI 10.1038/288280a0
[9] A human homolog of angiotensin-converting enzyme - Cloning and functional expression as a captopril-insensitive carboxypeptidase
Tipnis, SR
Hooper, NM
Hyde, R
Karran, E
Christie, G
Turner, AJ
[J]. JOURNAL OF BIOLOGICAL CHEMISTRY, 2000, 275 (43) : 33238 - 33243
[10] Hydrolysis of biological peptides by human angiotensin-converting enzyme-related carboxypeptidase
Vickers, C
Hales, P
Kaushik, V
Dick, L
Gavin, J
Tang, J
Godbout, K
Parsons, T
Baronas, E
Hsieh, F
Acton, S
Patane, M
Nichols, A
Tummino, P
[J]. JOURNAL OF BIOLOGICAL CHEMISTRY, 2002, 277 (17) : 14838 - 14843

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