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SYNTHESIS OF PROTEIN-PROTEIN INTERACTION INHIBITORS AND
DEVELOPMENT OF NEW CATALYTIC METHODS
by
Jamie A. Jarusiewicz
A Dissertation Presented to the
FACULTY OF THE USC GRADUATE SCHOOL
UNIVERSITY OF SOUTHERN CALIFORNIA
In Partial Fulfillment of the
Requirements for the Degree
DOCTOR OF PHILOSOPY
(CHEMISTRY)
August 2012
Copyright 2012 Jamie A. Jarusiewicz
Object Description
| Title | Synthesis of protein-protein interaction inhibitors and development of new catalytic methods |
| Author | Jarusiewicz, Jamie A. |
| Author email | jarusiew@usc.edu;jarusiej@yahoo.com |
| Degree | Doctor of Philosophy |
| Document type | Dissertation |
| Degree program | Chemistry |
| School | College of Letters, Arts And Sciences |
| Date defended/completed | 2012-07-31 |
| Date submitted | 2012-07-31 |
| Date approved | 2012-07-31 |
| Restricted until | 2012-07-31 |
| Date published | 2012-07-31 |
| Advisor (committee chair) | Petasis, Nicos A. |
| Advisor (committee member) |
Jung, Kyung W. Davies, Daryl |
| Abstract | This dissertation comprises three projects, two related to the synthesis and evaluation of small molecule inhibitors of protein-protein interactions, and one related to development of palladium-assisted reaction methodologies. ❧ The introduction (Chapter 1) briefly provides an overview of the challenges associated with developing small molecule inhibitors of protein-protein interactions in relation to drug discovery efforts. ❧ Chapter 2 reviews the biological importance of the transcription factor MEF2 and details its interaction with HDACs. The synthesis of a diverse set of over 100 molecules, including compounds structurally related to the natural product trichostatin A, aimed at directly targeting MEF2 is described. Evaluation of small molecule ligand/protein binding via 19F NMR spectroscopy is presented. The synthesis of helix-constrained peptides for investigation of their interaction with MEF2 is discussed as well. ❧ Chapter 3 describes the role of Bcl-2/Bcl-xL in apoptosis and cancer treatment. The construction of a small molecule of benzimidazole-based inhibitors for investigation of their structure-activity relationship is discussed. ❧ Chapter 4 provides a brief description of the utility of Heck and Strecker reactions in organic synthesis. Novel methodologies using palladium-promoted chemistry to form arylated cyclic enol ethers and α-aminonitriles is described. The use of palladium-catalysis to achieve selective oxidations is also briefly presented. |
| Keyword | organic synthesis; Heck reaction; Strecker reaction; N-heterocyclic carbenes; BCL-2 inhibitors; MEF2 |
| Language | English |
| Part of collection | University of Southern California dissertations and theses |
| Publisher (of the original version) | University of Southern California |
| Place of publication (of the original version) | Los Angeles, California |
| Publisher (of the digital version) | University of Southern California. Libraries |
| Provenance | Electronically uploaded by the author |
| Type | texts |
| Legacy record ID | usctheses-m |
| Rights | Jarusiewicz, Jamie A. |
| Access conditions | The author retains rights to his/her dissertation, thesis or other graduate work according to U.S. copyright law. Electronic access is being provided by the USC Libraries in agreement with the author, as the original true and official version of the work, but does not grant the reader permission to use the work if the desired use is covered by copyright. It is the author, as rights holder, who must provide use permission if such use is covered by copyright. The original signature page accompanying the original submission of the work to the USC Libraries is retained by the USC Libraries and a copy of it may be obtained by authorized requesters contacting the repository e-mail address given. |
| Repository name | University of Southern California Digital Library |
| Repository address | USC Digital Library, University of Southern California, University Park Campus MC 7002, 106 University Village, Los Angeles, California 90089-7002, USA |
| Repository email | cisadmin@usc.edu |
| Archival file | uscthesesreloadpub_Volume4/etd-Jarusiewic-1079.pdf |
Description
| Title | Page 1 |
| Full text | SYNTHESIS OF PROTEIN-PROTEIN INTERACTION INHIBITORS AND DEVELOPMENT OF NEW CATALYTIC METHODS by Jamie A. Jarusiewicz A Dissertation Presented to the FACULTY OF THE USC GRADUATE SCHOOL UNIVERSITY OF SOUTHERN CALIFORNIA In Partial Fulfillment of the Requirements for the Degree DOCTOR OF PHILOSOPY (CHEMISTRY) August 2012 Copyright 2012 Jamie A. Jarusiewicz |
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