Alan C Saghatelian

US Patent:

20050266505, Dec 1, 2005

Filed:

Jun 1, 2005

Appl. No.:

11/143009

Inventors:

Benjamin Cravatt - La Jolla CA, US
Alan Saghatelian - San Diego CA, US
Nadim Jessani - Los Altos CA, US
Arul Joseph - Cambridge MA, US

Assignee:

THE SCRIPPS RESEARCH INSTITUTE - La Jolla CA

International Classification:

C12Q001/68
G01N033/53
C12Q001/37

US Classification:

435007500, 435023000, 435006000

Abstract:

Activity-based compositions for analyzing metalloproteases are disclosed, where the compositions include a chemical compound including a hydroxamate moiety and a benzophenone moiety. Methods for synthesizing these compounds are also disclosed, as well as methods of using them for determining the bioactivity of a compositions comprising active compounds toward a metalloproteases and for determining the potency of an inhibitor against a metalloprotease.

US Patent:

20090068107, Mar 12, 2009

Filed:

Oct 2, 2007

Appl. No.:

11/866349

Inventors:

Benjamin F. Cravatt - La Jolla CA, US
Kyle P. Chiang - Cardiff CA, US
Sherry Niessen - San Diego CA, US
Alan Saghatelian - Cambridge MA, US

Assignee:

The Scripps Research Institute - La Jolla CA

International Classification:

A61K 49/00
A61K 31/27
C12Q 1/68
A61P 31/00
G01N 33/00
C12N 5/06

US Classification:

424 91, 514478, 435375, 514484, 435 6, 436 63

Abstract:

A multidimensional profiling strategy that combines activity-based proteomics and metabolomics was used to determine that an active protein, which is a previously uncharacterized enzyme highly elevated in aggressive cancer cells, serves as a central node in an ether lipid signaling network that bridges platelet-activating factor and the lysophospholipids. Biochemical studies confirmed that the active protein regulates this pathway by hydrolyzing the metabolic intermediate 2-acetyl monoalkylglycerol. Inactivation of the active protein disrupted ether lipid metabolism in cancer cells and impaired cell migration and tumor growth in vivo.

US Patent:

20130164758, Jun 27, 2013

Filed:

Aug 14, 2012

Appl. No.:

13/585298

Inventors:

Benjamin F. Cravatt - La Jolla CA, US
Kyle P. Chiang - Cardiff CA, US
Sherry Niessen - San Diego CA, US
Alan Saghatelian - Cambridge MA, US

Assignee:

The Scripps Research Institute - La Jolla CA

International Classification:

G01N 33/92

US Classification:

435 613, 435 618, 435 18

Abstract:

A multidimensional profiling strategy that combines activity-based proteomics and metabolomics was used to determine that an active protein, which is a previously uncharacterized enzyme highly elevated in aggressive cancer cells, serves as a central node in an ether lipid signaling network that bridges platelet-activating factor and the lysophospholipids. Biochemical studies confirmed that the active protein regulates this pathway by hydrolyzing the metabolic intermediate 2-acetyl monoalkylglycerol. Inactivation of the active protein disrupted ether lipid metabolism in cancer cells and impaired cell migration and tumor growth in vivo.

US Patent:

20180194714, Jul 12, 2018

Filed:

Mar 8, 2018

Appl. No.:

15/915957

Inventors:

- Boston MA, US
- Cambridge MA, US
Alan Saghatelian - La Jolla CA, US
Edwin Homan - New York NY, US
Mark M. Yore - Boston MA, US
Ismail Syed - Revere MA, US
Pedro M.M. Moraes Vieira - Brookline MA, US

International Classification:

C07C 69/22
G01N 33/543
G01N 33/92
C07C 69/58
C07C 69/533
C07C 69/24
C07D 495/04

Abstract:

The invention provides, inter alia, fatty acyl hydroxy fatty acid (FAHFA; a novel class of estolide-related molecules) and diagnostic and treatment methods for a variety of disorders—including diabetes-related disorders, Metabolic Syndrome, polycyctic ovarian syndrome, cancer, and inflammatory disorders—using them; as well as methods of screening for additional compounds that are useful in treating these disorders and/or that modulate FAHFA levels, FAHFA-mediated signaling, and FAHFA-mediated biological effects.

US Patent:

20170320928, Nov 9, 2017

Filed:

Jul 13, 2017

Appl. No.:

15/648937

Inventors:

- Madison WI, US
- Cambridge MA, US
Alan Attie - Madison WI, US
Mark P. Keller - McFarland WI, US
Alan Saghatelian - Cambridge MA, US

International Classification:

C07K 14/605
A61K 38/00

Abstract:

Described herein are peptide analogs of glucagon-like peptide 1 (GLP-1) that retain agonist activity, but are more resistant to proteolytic degradation than native GLP-1. In the analogs, at least one α-amino acid found in the native GLP-1 is replaced with a β-amino acid residue, which may or may not be cyclically constrained. Pharmaceutical compositions containing the analogs are described, as are methods to treat diabetes, and methods to make proteolytically resistant GLP-1 analogs.

US Patent:

20160282364, Sep 29, 2016

Filed:

Nov 6, 2014

Appl. No.:

15/034731

Inventors:

- Cambridge MA, US
Amanda McFedries - Lowell MA, US
Ralph E. Kleiner - New York NY, US
Alan Saghatelian - Somerville MA, US
David R. Liu - Lexington MA, US

Assignee:

President and Fellows of Harvard College - Cambridge MA

International Classification:

G01N 33/68
C07K 5/087
C07K 5/09
C07K 5/083
C12Q 1/68
G01N 33/58

Abstract:

IDE-binding probes and assays for the identification of IDE-binding and IDE-inhibiting compounds are provided. Pharmaceutical compositions of macrocyclic IDE inhibitors are also provided, including compositions in which such IDE inhibitors are combined with an additional therapeutic agent. Methods of using IDE inhibitors for transiently inhibiting IDE in a subject in need thereof, for example, for the transient inhibition of IDE in a subject exhibiting aberrant IDE activity, impaired isulin signaling, or insulin resistance, for example, a subject having diabetes, are also provided. Methods of using IDE inhibitors for transiently modulating heart rate and/or blood pressure in a subject are also provided.

US Patent:

20160221925, Aug 4, 2016

Filed:

Mar 14, 2014

Appl. No.:

14/775399

Inventors:

- Boston MA, US
- Cambridge MA, US
Alan SAGHATELIAN - La Jolla CA, US
Edwin HOMAN - New York NY, US

International Classification:

C07C 69/22
G01N 33/53
C07D 495/04

Abstract:

The invention provides, inter alia, fatty acyl hydroxy fatty acid (FAHFA; a novel class of estolide-related molecules) and diagnostic and treatment methods for a variety of disorders—including diabetes-related disorders, Metabolic Syndrome, polycystic ovarian syndrome, cancer, and inflammatory disorders—using them; as well as methods of screening for additional compounds that are useful in treating these disorders and/or that modulate FAHFA levels, FAHFA-mediated signaling, and FAHFA-mediated biological effects.

US Patent:

20160213744, Jul 28, 2016

Filed:

Jan 22, 2016

Appl. No.:

15/004862

Inventors:

- Cambridge MA, US
Juan Pablo Maianti - Cambridge MA, US
Alan Saghatelian - Somerville MA, US
Ralph E. Kleiner - New York NY, US

Assignee:

President and Fellows of Harvard College - Cambridge MA

International Classification:

A61K 38/12

Abstract:

Macrocyclic compounds that specifically inhibit insulin degrading enzyme (IDE) are provided. Pharmaceutically acceptable salts, solvates, hydrates, stereoisomers, polymorphs, tautomers, isotopically enriched forms, and prodrugs of the macrocyclic IDE inhibitors are also described. Pharmaceutical compositions are also provided. In vivo and in vitro methods of using the IDE inhibitor, and pharmaceutical compositions comprising the IDE inhibitor, for example, for the inhibition of IDE in a subject exhibiting aberrant IDE activity, impaired insulin signaling, or insulin resistance, for example, a subject having diabetes, are also provided.