Browsing by Author "Verdine, Gregory"
Now showing items 1-9 of 9
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All-Atom Model for Stabilization of α-Helical Structure in Peptides by Hydrocarbon Staples
Kutchukian, Peter S.; Yang, Jae Shick; Verdine, Gregory L.; Shakhnovich, Eugene Isaacovitch (American Chemical Society (ACS), 2009)Recent work has shown that the incorporation of an all-hydrocarbon “staple” into peptides can greatly increase their α-helix propensity, leading to an improvement in pharmaceutical properties such as proteolytic stability, ... -
Evolving a Direct Inhibitor of the Ras Proteins
McGee, John Hanney (2013-08-12)In recent years, great advances have been made in understanding the molecular causes of human disease, but our ability to exploit these discoveries for therapeutic benefit is frequently limited by the inability to make ... -
I. Targeted β-catenin Ubiquitination and Degradation Using Bifunctional Stapled Peptides II. Studies on Cell Penetration by Stapled Peptides
Chu, Qian (2014-02-25)Hydrocarbon-stapled alpha-helical peptides represent a relatively new class of synthetic peptidomimetics capable of inhibiting protein-protein interactions. It has been shown that hydrocarbon "staples" spanning one or two ... -
Inhibition of Oncogenic Wnt Signaling through Direct Targeting of β-Catenin
Grossmann, Tom N.; Yeh, Johannes Johannes; Bowman, Brian R.; Chu, Qian; Moellering, Raymond E.; Verdine, Gregory L. (Proceedings of the National Academy of Sciences, 2012)Aberrant activation of signaling by the Wnt pathway is strongly implicated in the onset and progression of numerous types of cancer. Owing to the persistent dependence of these tumors on Wnt signaling for growth and survival, ... -
Lessons From Cyclosporine A: Structural Determinants of Conformation-Switching and Passive Membrane Penetration
May, Erin Mallory (2015-10-15)The structural complexity of ‘beyond-rule-of-5’ compounds, such as peptide macrocycles, may facilitate access to additional biological target space beyond the enzymatic active site. Naturally occurring cyclic peptides, in ... -
Non-genotoxic conditioning for hematopoietic stem cell transplantation using a hematopoietic-cell-specific internalizing immunotoxin
Palchaudhuri, Rahul; Saez, Borja; Hoggatt, Jonathan George; Schajnovitz, Amir; Sykes, David Brian; Tate, Tiffany A; Czechowicz, Agnieszka; Kfoury, Youmna Sami; Ruchika, FNU; Rossi, Derrick J; Verdine, Gregory L.; Mansour, Michael Karim; Scadden, David Thomas (Springer Nature, 2016)Hematopoietic stem cell transplantation (HSCT) offers curative therapy for patients with hemoglobinopathies, congenital immunodeficiencies, and other conditions, possibly including AIDS. Autologous HSCT using genetically ... -
Probing Protein Interactions with Stapled Peptides: Myc Family and Insulin Receptor
Liang, Rebecca Yue (2013-10-15)One of the most exciting frontiers of expanding pharmacopeia to combat currently untreatable diseases is achieving specifically and potently disruption of unwanted protein-protein interactions where traditional small ... -
A Structural Model for the Damage-sensing Complex in Bacterial Nucleotide Excision Repair
Pakotiprapha, Danaya; Liu, Yi; Verdine, Gregory L.; Jeruzalmi, David (American Society for Biochemistry & Molecular Biology (ASBMB), 2009)Nucleotide excision repair is distinguished from other DNA repair pathways by its ability to process a wide range of structurally unrelated DNA lesions. In bacteria, damage recognition is achieved by the UvrA·UvrB ensemble. ... -
Structural Studies of the Bacterial MutY Adenine DNA Glycosylase and Its Human Homolog MUTYH
Wang, Lan (2016-09-15)Cellular DNA is under constant threat of reactive oxygen species (ROS) produced by either endogenous or exogenous sources. One of the major forms of DNA damages caused by ROS is 8-oxoguanine (oxoG), which is highly mutagenic, ...