Ho Yeon Nam

Abstract 5782: Machine learning and structure-guided discovery of EP300-selective, orally bioavailable degraders for cancer therapy

Ho Yeon Nam, Sun Young Jang, SeokJong Kang, Yongtaek Lee et autres

Abstract EP300 and CBP are closely related transcriptional co-activators with histone acetyltransferase (HAT) activity that regulate gene expression, cell proliferation, and differentiation. In normal tissues, EP300 and CBP compensate for each other; however, CBP-deficient tumor cells become selectively dependent on overexpressed EP300, …

kr (code pays fourni par la source)

Abstract 5882: Structure- and bioinformatics-driven development of a selective, orally bioavailable HER2 small molecule inhibitor (HM100714) for cancer therapy

Ho Yeon Nam, Sun Young Jang, Jiyoung Jeon, HyungSeok Yoo et autres

Abstract HER2 alterations, encompassing overexpression, amplification, and activating or other mutations, occur across multiple solid tumors and can drive cancer cell growth and metastatic progression. To address these alterations, HER2-targeted therapeutics are under development and clinical evaluation for breast, gastric, cholangiocarcinoma, colorectal, …

kr (code pays fourni par la source)

Abstract B117: Discovery of potent, selective, and orally bioavailable heterobifunctional EP300 degraders

Yongtaek Lee, Sun Young Jang, Seok-Jong Kang, Ho Yeon Nam et autres

Abstract EP300 and CBP are closely related transcriptional coactivators possessing histone acetyltransferase (HAT) activity, playing essential roles in the regulation of gene expression, cell proliferation, and differentiation. Both are frequently dysregulated or overexpressed in various cancers. In normal tissues, EP300 and CBP …

kr (code pays fourni par la source)

Abstract 1744: Preclinical efficacy of a selective, orally bioavailable HER2 small molecule inhibitor targeting HER2 alterations and Enhertu-resistant cancers

Ji‐Young Jeon, Sun Young Jang, Ho Yeon Nam, HyungSeok Yoo et autres

Abstract HER2 alterations, including overexpression, amplification, and other mutations are found in various solid tumors and have a significant impact on cancer cell growth and metastasis. To address this issue, HER2-targeted therapeutics are being developed and evaluated across multiple tumor types, including …

kr (code pays fourni par la source)

A bleomycin-mimicking manganese-porphyrin-conjugated mitochondria-targeting peptoid for cancer therapy

Veena Vijayan, Seung‐Heon Shin, Ho Yeon Nam, Dasom Song et autres

kr (code pays fourni par la source)

Impact of Conjugation of the Reactive Oxygen Species (ROS)-Generating Catalytic Moiety with Membrane-Active Antimicrobial Peptoids: Promoting Multitarget Mechanism and Enhancing Selectivity

Dasom Song, Byeongkwon Kim, Minsang Kim, Jin Kyeong Lee et autres

Antimicrobial peptides (AMPs) represent promising therapeutic modalities against multidrug-resistant bacterial infections. As a mimic of natural AMPs, peptidomimetic oligomers like peptoids (i.e., oligo- N -substituted glycines) have been utilized for antimicrobials with resistance against proteolytic degradation. Here, we explore the conjugation of …

kr (code pays fourni par la source)

Abstract 1970: Discovery and characterization of potent and selective HER2 exon20 insertion mutant inhibitors

Ho Yeon Nam, Sun Young Jang, Ji‐Young Jeon, HyungSeok Yoo et autres

Abstract Non-small cell lung cancer (NSCLC) is the most common type of lung cancer, accounting for over 85% of all cases. Among NSCLC, approximately 2-4% of patients have mutations in the HER2, a member of the ErbB family of receptor tyrosine kinases …

kr (code pays fourni par la source)

Real‐Time Monitoring of Multitarget Antimicrobial Mechanisms of Peptoids Using Label‐Free Imaging with Optical Diffraction Tomography (Adv. Sci. 24/2023)

Minsang Kim, Yeongmi Cheon, Dongmin Shin, Jieun Choi et autres

Optical Diffraction Tomography Article number 2302483 by Seongsoo Lee, Jiwon Seo, and co-workers presents the first demonstration of optical diffraction tomography (ODT) being successfully applied to monitor bacterial phenotypical changes in a real-time and label-free manner upon treatment of antimicrobial peptides (AMPs) …

Real‐Time Monitoring of Multitarget Antimicrobial Mechanisms of Peptoids Using Label‐Free Imaging with Optical Diffraction Tomography

Minsang Kim, Yeongmi Cheon, Dongmin Shin, Jieun Choi et autres

Antimicrobial peptides (AMPs) are promising therapeutics in the fight against multidrug-resistant bacteria. As a mimic of AMPs, peptoids with N-substituted glycine backbone have been utilized for antimicrobials with resistance against proteolytic degradation. Antimicrobial peptoids are known to kill bacteria by membrane disruption; …

kr, dk, us, no (code pays fourni par la source)

Synthesis and structure‐activity relationship of mitochondria‐targeting peptoids with varying hydrophobicity and cationic charge

Soyoung Kim, Ji‐Yu Lee, Jieun Choi, Ho Yeon Nam et autres

Abstract Mitochondria‐targeted delivery methods offer a straightforward approach for studying mitochondria‐related diseases and potentially streamlining therapeutic development. Peptoids (oligo‐N‐substituted glycines) are biocompatible peptidomimetics that display similar physicochemical properties as peptides with the added advantage of enhanced resistance to proteolytic cleavage. In particular, …

kr (code pays fourni par la source)

Helicity Modulation Improves the Selectivity of Antimicrobial Peptoids

Ho Yeon Nam, Jieun Choi, S. Dinesh Kumar, Josefine Eilsø Nielsen et autres

Abstract The modulation of conformational flexibility in antimicrobial peptides (AMPs) has been investigated as a strategy to improve their efficacy against bacterial pathogens while reducing their toxicity. Here, we synthesized a library of helicity-modulated antimicrobial peptoids by the position-specific incorporation of helix-inducing …

kr, no, dk (code pays fourni par la source)

Activity-Based Probes for the High Temperature Requirement A Serine Proteases

Ho Yeon Nam, Dasom Song, Jinny Eo, Na-Eun Choi et autres

The high temperature requirement A (HTRA) family of serine proteases mediates protein quality control. These proteins process misfolded proteins in several diseases including Alzheimer's disease (AD) and Parkinson's disease (PD). While their structures and activation mechanisms have been studied, the precise details …

kr (code pays fourni par la source)