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Design of Protease Stable Therapeutic Peptides by Non-Perturbative Modification

Award Information
Agency: Department of Health and Human Services
Branch: National Institutes of Health
Contract: 1R41GM130257-01
Agency Tracking Number: R41GM130257
Amount: $222,678.00
Phase: Phase I
Program: STTR
Solicitation Topic Code: 300
Solicitation Number: PA17-303
Solicitation Year: 2017
Award Year: 2018
Award Start Date (Proposal Award Date): 2018-08-07
Award End Date (Contract End Date): 2019-07-31
Small Business Information
254 UPLAND RD, #3
Cambridge, MA 02140-3605
United States
DUNS: 080572483
HUBZone Owned: No
Woman Owned: No
Socially and Economically Disadvantaged: No
Principal Investigator
 (617) 500-9099
Business Contact
Phone: (617) 564-3586
Research Institution
136 Harrison Avenue
BOSTON, MA 02111-1901
United States

 Nonprofit College or University

Peptide therapeutics combine high potency and selectivityand engender fewer side
effects than traditional small moleculesThis has fueled interest in peptides filling the
gap between `biologicsandaposand small molecules as compounds that have key desired
properties from both the other classesThere are however some challengesthe major
one being susceptibility to enzyme catalyzed hydrolytic cleavage and inactivationWe
propose here a strategy targeted towards an important class of peptide ligands that have
therapeutic valueVia chemical modification using rapidhigh yielding reactions and
through careful analysis of the key proteases involved in inactivationwe are able to
generate large number of compounds that retain activities at their cognate receptor but
are completely refractory to the frontline hydrolytic enzymesAt the end of Phase I
studiescandidate peptides will be chosen to advance furtherBecause of the large
number of derivatives possiblefine tuning of the pharmacological properties is achieved
in a short period of timeOur technology also provides an easily adaptable platform to
the broader community to stabilize their own peptide templates for preclinical
The work proposed will create a platform technology to stabilize therapeutic
peptides from being degraded by enzymesthus increasing their half lives in
serumwhile maintaining biological activityThis should result in the
improvement of potency and duration of effectfor an array of peptides that are
suitable for treatment in a variety of disease conditions

* Information listed above is at the time of submission. *

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