Sookhee Ha

Đề xuất hệ thống xác thực khuôn mặt đa camera dựa trên trí tuệ nhân tạo để quản lý nhân sự

Ngô Quốc Khiêm, Sookhee Ha

Nghiên cứu này trình bày việc phát triển một hệ thống xác thực khuôn mặt đa camera nhằm nâng cao hiệu quả quản lý điểm danh cho nhân viên và sinh viên. Hệ thống tích hợp các công nghệ phát hiện, nhận …

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Orally Bioavailable Macrocyclic Peptide That Inhibits Binding of PCSK9 to the Low Density Lipoprotein Receptor

Douglas G. Johns, Louis‐Charles Campeau, Puja Banka, An Bautmans et autres

BACKGROUND: Inhibition of PCSK9 (proprotein convertase subtilisin/kexin type 9)-low density lipoprotein receptor interaction with injectable monoclonal antibodies or small interfering RNA lowers plasma low density lipoprotein-cholesterol, but despite nearly 2 decades of effort, an oral inhibitor of PCSK9 is not available. Macrocyclic …

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Discovery and Structure-Based Design of Macrocyclic Peptides Targeting STUB1

Simon Ng, Alexander C. Brueckner, Soheila Bahmanjah, Qiaolin Deng et autres

Recent evidence suggests that deletion of STUB1─a pivotal negative regulator of interferon-γ sensing─may potentially clear malignant cells. However, current studies rely primarily on genetic approaches, as pharmacological inhibitors of STUB1 are lacking. Identifying a tool compound will be a step toward validating …

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Discovery and Structure-Based Design of Macrocyclic Peptides Targeting STUB1

Simon Ng, Alexander C. Brueckner, Soheila Bahmanjah, Qiaolin Deng et autres

STIP1 homology and U-Box containing protein 1 (STUB1) plays a key role in maintaining cell health during stress and aging. Recent evidence suggested STUB1 also helps regulate immunity with the potential of clearing malignant cells. Indeed, we and others have shown that …

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A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors

Thomas J. Tucker, Mark W. Embrey, Candice Alleyne, Rupesh P. Amin et autres

Proprotein convertase subtilisin-like/kexin type 9 (PCSK9) is a key regulator of plasma LDL-cholesterol (LDL-C) and a clinically validated target for the treatment of hypercholesterolemia and coronary artery disease. Starting from second-generation lead structures such as 2, we were able to refine these …

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From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9

Whitney L. Petrilli, Gregory C. Adam, Roman S. Erdmann, Pravien Abeywickrema et autres

Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design

Candice Alleyne, Rupesh P. Amin, Bhavana Bhatt, Elisabetta Bianchi et autres

Proprotein convertase subtilisin-like/kexin type 9 (PCSK9) is a key regulator of plasma LDL-cholesterol (LDL-C) and a clinically validated target for the treatment of hypercholesterolemia and coronary artery disease. In this paper, we describe a series of novel cyclic peptides derived from an …

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From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9

Whitney L. Petrilli, Gregory C. Adam, Roman S. Erdmann, Pravien Abeywickrema et autres

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From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9

Whitney L. Petrilli, Gregory C. Adam, Roman S. Erdmann, Pravien Abeywickrema et autres

Proprotein convertase substilisin-like/kexin type 9 (PCSK9) is a serine protease involved in a protein-protein interaction with the low-density lipoprotein (LDL) receptor that has both human genetic and clinical validation. Our pursuit of small molecule direct binders for this difficult to drug PPI …

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From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9

Whitney L. Petrilli, Gregory C. Adam, Roman S. Erdmann, Pravien Abeywickrema et autres

Proprotein convertase substilisin-like/kexin type 9 (PCSK9) is a serine protease involved in a protein-protein interaction with the low-density lipoprotein (LDL) receptor that has both human genetic and clinical validation. Our pursuit of small molecule direct binders for this difficult to drug PPI …

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Incorporation of Putative Helix-Breaking Amino Acids in the Design of Novel Stapled Peptides: Exploring Biophysical and Cellular Permeability Properties

Anthony W. Partridge, Hung Yi Kristal Kaan, Yu‐Chi Juang, Ahmad Sadruddin et autres

Stapled α-helical peptides represent an emerging superclass of macrocyclic molecules with drug-like properties, including high-affinity target binding, protease resistance, and membrane permeability. As a model system for probing the chemical space available for optimizing these properties, we focused on dual Mdm2/MdmX antagonist …

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Development of a Platform To Enable Efficient Permeability Evaluation of Novel Organo-Peptide Macrocycles

Brett A. Hopkins, Hyelee Lee, Sookhee Ha, Lisa Nogle et autres

As more macrocycle structures are utilized to drug intracellular targets, new platforms are needed to facilitate the discovery of cell permeable compounds in this unique chemical space. Herein, a method is disclosed that allows for the efficient synthesis and permeability evaluation of …

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