University of South Florida

H. Lee Moffitt Cancer Center and Research Institute, Inc.

Wisconsin Alumni Research Foundation

The United States Government As Represented by the Department of Veterans Affairs

Jianfeng Cai

Chuanhai Cao

Alekhya Nimmagadda

Peng Teng

Haifan Wu

Youhong Niu

Said M Sebti

Shruti Padhee

Yan Shi

Niketa A Patel

Ma Su

Yaqiong Li

Ge Bai

Vrushank G Davé

Haitao Ji

Weibo Cai

Sami Abdulkadir

Mengmeng Zheng

Peng Sang

Min Zhang

Hao Hong

Disclosed herein is a series of helical sulfono-γ-AApeptides that mimic the binding mode of the α-helical HD2 domain of B-Cell Lymphoma 9 (BCL9). As disclosed herein, sulfono-γ-AApeptides can structurally and functionally mimic the α-helical domain of BCL9, and selectively disrupt β-catenin/BCL9 PPIs with even higher potency. More intriguingly, these sulfono-γ-AApeptides can enter cancer cells, bind with β-catenin and disrupt β-catenin/BCL PPI, and exhibit excellent cellular activity, which is much more potent than the BCL9 peptide. Furthermore, enzymatic stability studies demonstrated the remarkable stability of the helical sulfono-γ-AApeptides, with no degradation in the presence of pronase for 24 h, augmenting their biological potential.

B-catenin/B-cell Lymphoma 9 protein-protein interaction inhibiting peptidomimetics

Disclosed are cyclic γ-amino acid peptide compounds, methods of using said compounds, and kits comprising said compounds. More specifically, disclosed are human epidermal growth factor receptor 2 (HER2) specific cyclic γ-amino acid peptide compounds, methods of using said compounds in the treatment of cell proliferative diseases or disorders, methods of detecting HER2 using the compounds, and kits comprising the compounds.

Peptidomimetic-based antibody surrogate for HER2

Provided herein are compounds, compositions, pharmaceutical compositions, kits, and methods relating to novel sulfono-γ-AA peptides. Novel sulfono-γ-AA peptides as described herein can have the structure according to Formula 1: In embodiments according to the present disclosure, novel sulfono-γ-AA peptides as described herein have minimal toxicity, can repair neuronal damage, inhibit Amyloid beta aggregation, and promote cellular growth and viability.

Compositions and methods relating to novel sulfono-gamma-AA peptides

Provided herein are novel VEGF mimics, pharmaceutical compositions thereof, and methods of their use in increasing or reducing angiogenesis.

Modulating angiogenesis by proteomimetics of vascular endothelial growth factor

Provided are novel bis-cyclic guanidine compounds, and the use thereof for treating bacterial infection.

Bis-cyclic guanidines as antibacterial agents

Provided herein are compounds that can bind GAS5 long non-coding RNA, compositions thereof, and uses thereof.

GAS5 binding compounds, formulations, and uses thereof

Disclosed herein are compounds for the treatment of neurodegenerative diseases and compositions comprising the same.

Compounds and methods for reducing or inhibiting aggregation of proteins in a subject

Described herein are assays, methods, and devices for diagnosing/prognosing Alzheimer's disease (AD) and/or a neurodegenerative disease in a subject. The assays, methods, and/or devices described herein can be configured to detect GAS5 long-coding RNAs and/or expression thereof in a sample from a subject.

Methods and compositions for diagnosis and management of neurodegerative diseases

A one-bead-two-compound combinatorial synthesis technique provides libraries of macrocyclic peptidomimetic compounds and compositions with use as ligands for the Ephrin type-A receptor 2 (EphA2). The one-bead-two-compound technique and libraries of macrocyclic compounds are useful as research tools in drug discovery and/or to treat or prevent a range of diseases or disorders.

One-bead-two-compound macrocyclic library and methods of preparation and use

Described herein are compounds and formulations thereof that can bind PTEN. Also described herein are methods of using the compounds and formulations thereof that can bind PTEN. In some embodiments, the method can include administering an amount of a compound or formulation described herein to a subject in need thereof.

PTEN binding compounds, formulations, and uses thereof

Compounds for the treatment of neurodegenerative diseases

The present disclosure provides compositions including a hydantoin derivative compound, pharmaceutical compositions including a hydantoin derivative compound, methods of treatment of a condition (e.g., bacterial infection) or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.

Growing community of inventors

Tampa, FL, United States of America

Jianfeng Cai