☆ 4.7 Article

Discovery of a Novel Bifunctional Steroid Analog, YXG-158, as an Androgen Receptor Degrader and CYP17A1 Inhibitor for the Treatment of Enzalutamide-Resistant Prostate Cancer

JOURNAL OF MEDICINAL CHEMISTRY (2023)

相关参考文献

注意：仅列出部分参考文献，下载原文获取全部文献信息。

Article Oncology

Cancer statistics, 2022

Rebecca L. Siegel et al.

Summary: Each year, the American Cancer Society compiles data on cancer occurrence and outcomes in the United States. The latest data shows that breast and prostate cancer progress has stagnated, while lung cancer has shown improvements in survival rates. Lung cancer incidence for advanced disease has declined while localized-stage rates have increased, resulting in higher survival rates. Mortality patterns align with incidence trends, with lung cancer deaths declining rapidly, breast cancer deaths slowing, and prostate cancer deaths stabilizing.

CA-A CANCER JOURNAL FOR CLINICIANS (2022)

添加到收藏夹

Article Chemistry, Medicinal

A Comprehensive Overview of Small-Molecule Androgen Receptor Degraders: Recent Progress and Future Perspectives

Si Ha et al.

Summary: This article summarizes the current development of strategies targeting the abnormal activation of androgen receptor (AR) signaling in prostate cancer. The authors discuss the mechanisms and clinical studies of various small-molecule AR degraders, and explore their potential value in treating castration-resistant prostate cancer (CRPC).

JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Chemistry, Medicinal

Design, Synthesis, and Biological Evaluation of Androgen Receptor Degrading and Antagonizing Bifunctional Steroidal Analogs for the Treatment of Advanced Prostate Cancer

Ao Wang et al.

Summary: This study discovered a bifunctional agent called 67-b, which has the ability to both antagonize and degrade androgen receptor (AR). In vitro and in vivo experiments demonstrated the potential therapeutic effect of 67-b for treating mCRPC patients.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Oncology

Phase II Multicenter Study of Enzalutamide in Metastatic Castration-Resistant Prostate Cancer to Identify Mechanisms Driving Resistance

Rana R. McKay et al.

Summary: Enzalutamide has shown improved overall survival in metastatic CRPC, but resistance eventually develops. This study found baseline and progression alterations in AR pathway and tumor suppressor genes in a large proportion of patients. Post-enzalutamide, there was an increase in BRCA2 alterations, emphasizing the importance of serial tumor sampling in CRPC.

CLINICAL CANCER RESEARCH (2021)

添加到收藏夹

Review Oncology

Androgen Receptor Signaling in Prostate Cancer and Therapeutic Strategies

Aasems Jacob et al.

Summary: Prostate cancer growth is primarily mediated by androgen signaling pathways, but resistance mechanisms are complex. Treatment strategies focus on inhibiting androgen signaling through various pathways, yet disease progression eventually occurs in patients. Multiple clinical trials are exploring therapeutic strategies to overcome these resistance mechanisms.

CANCERS (2021)

添加到收藏夹

Article Chemistry, Medicinal

Exploration and Biological Evaluation of Basic Heteromonocyclic Propanamide Derivatives as SARDs for the Treatment of Enzalutamide-Resistant Prostate Cancer

Yali He et al.

Summary: A series of propanamide derivatives were designed, synthesized, and characterized as selective androgen receptor degraders (SARDs) and pan-antagonists, showing efficacy against enzalutamide-resistant prostate cancers.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer

Xin Han et al.

Summary: This study outlines strategies for discovering highly potent PROTAC degraders of androgen receptor (AR) with excellent oral pharmacokinetics, successfully identifying compound ARD-2128 as the most effective in inhibiting tumor growth in mice with good oral bioavailability.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Oncology

Comprehensive Analysis of AR Alterations in Circulating Tumor DNA from Patients with Advanced Prostate Cancer

Elisa M. Ledet et al.

ONCOLOGIST (2020)

添加到收藏夹

Article Chemistry, Medicinal

Monomeric Targeted Protein Degraders

Emily J. Hanan et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Pyrazol-1-yl-propanamides as SARD and Pan-Antagonists for the Treatment of Enzalutamide-Resistant Prostate Cancer

Yali He et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Review Urology & Nephrology

Therapeutic targeting of the androgen receptor (AR) and AR variants in prostate cancer

Ramesh Narayanan

ASIAN JOURNAL OF UROLOGY (2020)

添加到收藏夹

Review Andrology

Role of Androgen Receptor in Prostate Cancer: A Review

Kazutoshi Fujita et al.

WORLD JOURNAL OF MENS HEALTH (2019)

添加到收藏夹

Article Oncology

Galeterone and The Next Generation Galeterone Analogs, VNPP414 and VNPP433-3β Exert Potent Therapeutic Effects in Castration-/Drug-Resistant Prostate Cancer Preclinical Models In Vitro and In Vivo

Andrew K. Kwegyir-Afful et al.

CANCERS (2019)

添加到收藏夹

Article Chemistry, Medicinal

New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity

Dong-Jin Hwang et al.

JOURNAL OF MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Article Urology & Nephrology

Role of Androgen Receptor Variants in Prostate Cancer: Report from the 2017 Mission Androgen Receptor Variants Meeting

Jun Luo et al.

EUROPEAN UROLOGY (2018)

添加到收藏夹

Article Chemistry, Applied

Improved Procedures for Gram-Scale Synthesis of Galeterone 3β-Imidazole and Galeterone 3β-Pyridine Methoxylate, Potent Androgen Receptor/Mnk Degrading Agents

Puranik Purushottamachar et al.

ORGANIC PROCESS RESEARCH & DEVELOPMENT (2016)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of MK-7145, an Oral Small Molecule ROMK Inhibitor for the Treatment of Hypertension and Heart Failure

Haifeng Tang et al.

ACS MEDICINAL CHEMISTRY LETTERS (2016)

添加到收藏夹

Article Oncology

Genomic Alterations in Cell-Free DNA and Enzalutamide Resistance in Castration-Resistant Prostate Cancer

Alexander W. Wyatt et al.

JAMA ONCOLOGY (2016)

添加到收藏夹

Article Oncology

AZD3514, an oral selective androgen receptor down-regulator in patients with castration-resistant prostate cancer - results of two parallel first-in-human phase I studies

A. Omlin et al.

INVESTIGATIONAL NEW DRUGS (2015)

添加到收藏夹

Article Chemistry, Medicinal

Discovery and Development of Galeterone (TOK-001 or VN/124-1) for the Treatment of All Stages of Prostate Cancer

Vincent C. O. Njar et al.

JOURNAL OF MEDICINAL CHEMISTRY (2015)

添加到收藏夹

Article Oncology

Galeterone and VNPT55 induce proteasomal degradation of AR/AR-V7, induce significant apoptosis via cytochrome c release and suppress growth of castration resistant prostate cancer xenografts in vivo

Andrew K. Kwegyir-Afful et al.

ONCOTARGET (2015)

添加到收藏夹

Article Chemistry, Medicinal

Successful reduction of off-target hERG toxicity by structural modification of a T-type calcium channel blocker

Yeon Jae Choi et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2014)

添加到收藏夹

Review Oncology

MG132, a proteasome inhibitor, induces apoptosis in tumor cells

Na Guo et al.

ASIA-PACIFIC JOURNAL OF CLINICAL ONCOLOGY (2013)

添加到收藏夹

Article Endocrinology & Metabolism

Drug Safety Is a Barrier to the Discovery and Development of New Androgen Receptor Antagonists

William R. Foster et al.

PROSTATE (2011)

添加到收藏夹

Article Oncology

Integrative Genomic Profiling of Human Prostate Cancer

Barry S. Taylor et al.

CANCER CELL (2010)

添加到收藏夹

Article Oncology

Overcoming Persistent Dependency on Androgen Signaling after Progression to Castration-Resistant Prostate Cancer

Masuo Yamaoka et al.

CLINICAL CANCER RESEARCH (2010)

添加到收藏夹

Article Biochemistry & Molecular Biology

Androgen receptor: A key molecule in the progression of prostate cancer to hormone independence

ME Taplin et al.

JOURNAL OF CELLULAR BIOCHEMISTRY (2004)

添加到收藏夹

© Peeref 2019-2024. All rights reserved.