Title:
MODULATORS OF SREBP PROCESSING
Document Type and Number:
WIPO Patent Application WO2001027138
Kind Code:
A3
Abstract:
Compounds, compositions and methods are provided for the inhibition of S1 protease and for the modulation of cholesterol homeostasis in a cell.
Inventors:
JAEN JUAN C
LI LEPING
BROWN MICHAEL S
GOLDSTEIN JOSEPH L
CHENG DONG
LI LEPING
BROWN MICHAEL S
GOLDSTEIN JOSEPH L
CHENG DONG
Application Number:
PCT/US2000/028428
Publication Date:
November 29, 2001
Filing Date:
October 11, 2000
Export Citation:
Assignee:
TULARIK INC (US)
UNIV TEXAS SOUTHWESTERN MED CT (US)
UNIV TEXAS SOUTHWESTERN MED CT (US)
International Classes:
C07K5/09; C07K5/11; A61K38/00; (IPC1-7): C07K14/81; A61K38/55; A61P3/00; C07K5/11; C07K5/09
Domestic Patent References:
| WO1994025049A1 | 1994-11-10 | |||
| WO2000026348A2 | 2000-05-11 | |||
| WO2000009677A2 | 2000-02-24 |
Other References:
CHENG DONG ET AL: "Secreted Site-1 protease cleaves peptides corresponding to luminal loop of sterol regulatory element-binding proteins.", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 274, no. 32, 6 August 1999 (1999-08-06), pages 22805 - 22812, XP002171384, ISSN: 0021-9258
ESPENSHADE PETER J ET AL: "Autocatalytic processing of Site-1 protease removes propeptide and permits cleavage of sterol regulatory element-binding proteins", JOURNAL OF BIOLOGICAL CHEMISTRY,US,AMERICAN SOCIETY OF BIOLOGICAL CHEMISTS, BALTIMORE, MD, vol. 274, no. 32, 6 August 1999 (1999-08-06), pages 22795 - 22804, XP002136835, ISSN: 0021-9258
SEIDAH NABIL G ET AL: "Mammalian subtilisin/kexin isozyme SKI-1: A widely expressed proprotein convertase with a unique cleavage specificity and cellular localization.", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES, vol. 96, no. 4, 16 February 1999 (1999-02-16), Feb. 16, 1999, pages 1321 - 1326, XP002171385, ISSN: 0027-8424
DEMUTH H -U: "RECENT DEVELOPMENTS IN INHIBITING CYSTEINE AND SERINE PROTEASES", JOURNAL OF ENZYME INHIBITION,US,NEW YORK, NY, vol. 3, no. 4, 1990, pages 249 - 278, XP002041620
IMPERIALI B ET AL: "INHIBITION OF SERINE PROTEASES BY PEPTIDYL FLUOROMETHYL KETONES", BIOCHEMISTRY,US,AMERICAN CHEMICAL SOCIETY. EASTON, PA, vol. 25, no. 13, 1 July 1986 (1986-07-01), pages 3760 - 3767, XP000572386, ISSN: 0006-2960
SHEPHERD T A ET AL: "Small peptidic aldehyde inhibitors of human rhinovirus 3C protease", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,GB,OXFORD, vol. 6, no. 23, 3 December 1996 (1996-12-03), pages 2893 - 2896, XP004136100, ISSN: 0960-894X
SIEZEN R J ET AL: "SUBTILASES: THE SUPERFAMILY OF SUBTILISIN-LIKE SERINE PROTEASES", PROTEIN SCIENCE,CAMBRIDGE UNIVERSITY PRESS, CAMBRIDGE,GB, vol. 6, no. 3, March 1997 (1997-03-01), pages 501 - 523, XP000856203, ISSN: 0961-8368
ESPENSHADE PETER J ET AL: "Autocatalytic processing of Site-1 protease removes propeptide and permits cleavage of sterol regulatory element-binding proteins", JOURNAL OF BIOLOGICAL CHEMISTRY,US,AMERICAN SOCIETY OF BIOLOGICAL CHEMISTS, BALTIMORE, MD, vol. 274, no. 32, 6 August 1999 (1999-08-06), pages 22795 - 22804, XP002136835, ISSN: 0021-9258
SEIDAH NABIL G ET AL: "Mammalian subtilisin/kexin isozyme SKI-1: A widely expressed proprotein convertase with a unique cleavage specificity and cellular localization.", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES, vol. 96, no. 4, 16 February 1999 (1999-02-16), Feb. 16, 1999, pages 1321 - 1326, XP002171385, ISSN: 0027-8424
DEMUTH H -U: "RECENT DEVELOPMENTS IN INHIBITING CYSTEINE AND SERINE PROTEASES", JOURNAL OF ENZYME INHIBITION,US,NEW YORK, NY, vol. 3, no. 4, 1990, pages 249 - 278, XP002041620
IMPERIALI B ET AL: "INHIBITION OF SERINE PROTEASES BY PEPTIDYL FLUOROMETHYL KETONES", BIOCHEMISTRY,US,AMERICAN CHEMICAL SOCIETY. EASTON, PA, vol. 25, no. 13, 1 July 1986 (1986-07-01), pages 3760 - 3767, XP000572386, ISSN: 0006-2960
SHEPHERD T A ET AL: "Small peptidic aldehyde inhibitors of human rhinovirus 3C protease", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,GB,OXFORD, vol. 6, no. 23, 3 December 1996 (1996-12-03), pages 2893 - 2896, XP004136100, ISSN: 0960-894X
SIEZEN R J ET AL: "SUBTILASES: THE SUPERFAMILY OF SUBTILISIN-LIKE SERINE PROTEASES", PROTEIN SCIENCE,CAMBRIDGE UNIVERSITY PRESS, CAMBRIDGE,GB, vol. 6, no. 3, March 1997 (1997-03-01), pages 501 - 523, XP000856203, ISSN: 0961-8368
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