Review
Biotechnology & Applied Microbiology
Renlun Huang, Lang Guo, Menghan Gao, Jing Li, Songtao Xiang
Summary: Prostate cancer (PCa) is the most common cancer of urologic neoplasms, and the CCL5/CCR5 axis plays a significant role in its development, but challenges remain in precision oncology.
ONCOTARGETS AND THERAPY
(2021)
Article
Urology & Nephrology
William T. Lowrance, Rodney H. Breau, Roger Chou, Brian F. Chapin, Tony Crispino, Robert Dreicer, David F. Jarrard, Adam S. Kibel, Todd M. Morgan, Alicia K. Morgans, William K. Oh, Matthew J. Resnick, Anthony L. Zietman, Michael S. Cookson
Summary: This summary focuses on Part I of the series dedicated to Advanced Prostate Cancer: AUA/ASTRO/SUO Guideline, providing prognostic and treatment recommendations for patients with advanced prostate cancer. The guideline includes evidence- and consensus-based statements to improve patient care, with the need for continued research to enhance treatment outcomes in the future.
JOURNAL OF UROLOGY
(2021)
Article
Chemistry, Medicinal
Marius Patberg, Andreas Isaak, Friederike Fuesser, Natalia V. Ortiz Zacarias, Laura Vinnenberg, Janine Schulte, Lucia Michetti, Lucie Grey, Cas van der Horst, Petra Hundehege, Oliver Koch, Laura H. Heitman, Thomas Budde, Anna Junker
Summary: The P2X7 receptor plays a crucial role in regulating tumor growth and immune responses, with its antagonists showing promising therapeutic effects in cancer, inflammatory diseases, and chronic pain. Novel P2X7R antagonists incorporating piperazine squaric diamides have been developed with improved potency and drug-like properties through optimization of ADME characteristics. Docking studies revealed the antagonists binding to allosteric pockets in two distinct poses, depending on the substitution of the central piperazine moiety.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Zhifu Wang, Danyi Zheng, Ye Sing Tan, Qiang Yuan, Fang Yuan, Su-Chun Zhang
Summary: A chemical cocktail consisting of fibrinogen and CCR5 antagonist maraviroc supports the survival and maturation of neural precursors that are transplanted into the ischemic stroke cavity by blocking the inflammatory cascade, enabling the reconstitution of the damaged central nervous system by grafted neural cells.
Article
Urology & Nephrology
Samuel Tremblay, Lily Summers-Trasiewicz, Frederic Pouliot, Juanita M. Crook, Keyue Ding, Laurence Klotz, Paul Toren
Summary: This study aimed to evaluate the relationship between testosterone levels and PSA levels during ADT and its impact on clinical outcomes. The results showed that testosterone levels had a smaller prognostic effect compared to PSA levels on outcomes. Specifically, there was no significant association between the cumulative testosterone exposure and outcomes.
JOURNAL OF UROLOGY
(2021)
Review
Urology & Nephrology
Timothy J. Wilt, Kristen E. Ullman, Eric J. Linskens, Roderick MacDonald, Michelle Brasure, Elizabeth Ester, Victoria A. Nelson, Jayati Saha, Shahnaz Sultan, Philipp Dahm
Summary: - Watchful waiting for clinically detected localized prostate cancer may increase mortality and metastases, but decrease urinary and erectile dysfunction compared to radical prostatectomy.
- Radical prostatectomy reduces mortality but causes more harms compared to watchful waiting, while active monitoring shows little to no mortality difference versus radical prostatectomy or external beam radiation plus androgen deprivation.
- Limited data exist on the effectiveness of other treatments for clinically localized prostate cancer.
JOURNAL OF UROLOGY
(2021)
Article
Biochemical Research Methods
George Makris, Antonio Shegani, Pavithra H. A. Kankanamalage, Marina Kuchuk, Rajendra P. Bandari, Charles J. Smith, Heather M. Hennkens
Summary: This study presents the preclinical evaluation of novel [Cu-64]Cu-GRPR-targeting tracers, demonstrating high binding affinities and favorable biodistribution for potential PET imaging of GRPR-expressing tumors. The synthesized tracers showed excellent stability and receptor-mediated tumor uptake, as validated by imaging studies, supporting their further development as diagnostic agents.
BIOCONJUGATE CHEMISTRY
(2021)
Review
Oncology
Marzieh Ehsani, Faith Oluwakemi David, Aria Baniahmad
Summary: Prostate cancer can develop resistance to hormone treatment and chemotherapy, mainly due to the androgen receptor (AR). There are genomic and non-genomic signaling bypass mechanisms that tumor cells may develop to escape therapy. As resistance progresses, tumors may evolve further adaptive pathways which lead to increased aggressiveness and metastatic ability.
Article
Chemistry, Multidisciplinary
Jordan M. Mattheisen, Chris Limberakis, Roger B. Ruggeri, Matthew S. Dowling, Christopher W. am Ende, Emilie Ceraudo, Thomas Huber, Christopher L. McClendon, Thomas P. Sakmar
Summary: We developed a strategy to covalently tether drug fragments adjacent to allosteric sites in GPCRs to enhance their potency and enable fragment-based drug screening in cell-based systems.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2023)
Review
Biochemistry & Molecular Biology
Navid Sobhani, Praveen Kumar Neeli, Alberto D'Angelo, Matteo Pittacolo, Marianna Sirico, Ilaria Camilla Galli, Giandomenico Roviello, Gabriella Nesi
Summary: Metastatic prostate cancer is the most common cancer in males with a poor prognosis, and many patients develop the AR-V7 variant. AR-V7 acts as a transcription factor in the nucleus, repressing crucial tumor suppressor genes. Anti-AR-V7 drugs show promise for this subset of patients.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Urology & Nephrology
Keith T. Schmidt, Alwin D. R. Huitema, Cindy H. Chau, William D. Figg
Summary: The introduction of second-generation androgen receptor antagonists has revolutionized the treatment of metastatic prostate cancer, offering tolerable and effective alternatives to chemotherapy. However, the issue of treatment resistance remains a significant challenge, and researchers are exploring various approaches to address this issue.
NATURE REVIEWS UROLOGY
(2021)
Article
Urology & Nephrology
Kathleen W. Zhang, Melissa A. Reimers, Adam Christopher Calaway, Michael G. Fradley, Lee Ponsky, Jorge A. Garcia, Jennifer Cullen, Brian C. Baumann, Daniel Addison, Courtney M. Campbell, Arjun K. Ghosh, Daniel J. Lenihan, Nihar R. Desai, Neal Weintraub, Avirup Guha
Summary: In men treated for prostate cancer, arterial vascular events were the most commonly reported cardiovascular adverse events. GnRH antagonists were associated with fewer cardiovascular adverse events compared to GnRH agonists.
JOURNAL OF UROLOGY
(2021)
Article
Oncology
Linglong Yin, Yubing Ye, Ling Zou, Jinli Lin, Yi Dai, Yongming Fu, Youhong Liu, Yuchong Peng, Yingxue Gao, Yuxin Fu, Xuli Qi, Tanggang Deng, Songwei Zhang, Xiong Li
Summary: The degradation of TOMM20 protein induced by AR antagonists promotes the transdifferentiation of prostate cancer to neuroendocrine prostate cancer, revealing a novel molecular mechanism by which AR antagonists develop drug resistance through the mitochondrial outer membrane-mediated signaling pathway.
JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH
(2023)
Article
Chemistry, Medicinal
Veronica Di Sarno, Pia Giovannelli, Alicia Medina-Peris, Tania Ciaglia, Marzia Di Donato, Simona Musella, Gianluigi Lauro, Vincenzo Vestuto, Gerardina Smaldone, Francesca Di Matteo, Giuseppe Bifulco, Gabriella Castoria, Antimo Migliaccio, Asia Fernandez-Carvajal, Pietro Campiglia, Isabel Gomez-Monterrey, Carmine Ostacolo, Alessia Bertamino
Summary: This study describes the design and synthesis of a new series of TRPM8 antagonists, which were preliminarily characterized for potency and selectivity in vitro, showing remarkable efficacy in inhibiting the growth of prostate cancer cells.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Urology & Nephrology
Alexander Pan, Rachel E. Reingold, Jimmy L. Zhao, Andrea Moy, Lukas Kraehenbuehl, George Dranitsaris, Sean M. McBride, Howard Scher, Marisa A. Kollmeier, Han Xiao, Dana E. Rathkopf, Mario E. Lacouture
Summary: Patients with prostate cancer treated with apalutamide frequently develop dermatological adverse events, such as rash. Common adverse events include maculopapular rashes and xerosis. Clinical trial patients and those receiving abiraterone/prednisone are more likely to experience these events. Most adverse events can be managed with topical or oral steroids.
JOURNAL OF UROLOGY
(2022)
Article
Chemistry, Medicinal
Yunyun Yuan, Xia Li, Saheem A. Zaidi, Christopher K. Arnatt, Xiaofei Yu, Chunqing Guo, Xiang-Yang Wang, Yan Zhang
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2015)
Meeting Abstract
Cell & Tissue Engineering
C. Arnatt, G. Cooksey, A. Tona, J. Elliot
Article
Biochemistry & Molecular Biology
Christopher K. Arnatt, Bethany A. Falls, Yunyun Yuan, Thomas J. Raborg, Ruturaj R. Masvekar, Nazira El-Hage, Dana E. Selley, Anthony V. Nicola, Pamela E. Knapp, Kurt F. Hauser, Yan Zhang
BIOORGANIC & MEDICINAL CHEMISTRY
(2016)
Review
Chemistry, Medicinal
Christopher Kent Arnatt, Yan Zhang
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2014)
Article
Chemistry, Medicinal
Christopher K. Arnatt, Yan Zhang
MOLECULAR INFORMATICS
(2013)
Article
Chemistry, Medicinal
Austin O'Dea, Chelsea Sondergard, Patrick Sweeney, Christopher Kent Arnatt
ACS MEDICINAL CHEMISTRY LETTERS
(2018)
Article
Chemistry, Organic
John T. Petroff, Kristin N. Skubic, Christopher K. Arnatt, Ryan D. McCulla
JOURNAL OF ORGANIC CHEMISTRY
(2018)
Meeting Abstract
Biochemistry & Molecular Biology
Kristin Skubic, Christopher K. Arnatt
Meeting Abstract
Biochemistry & Molecular Biology
Chelsea Sondergard, Christopher Arnatt
Meeting Abstract
Biochemistry & Molecular Biology
Kristin Skubic, Miranda Adams, Jill Horn, Anna Priddy, Renae Oelrich, Michael Lewis, Brent Znosko, Christopher Arnatt
Meeting Abstract
Biochemistry & Molecular Biology
Chlelsea DeLeon, McKenna Wilhelm, Patrick Sweeney, Christopher Arnatt
Meeting Abstract
Chemistry, Multidisciplinary
Austin O'Dea, Christopher Arnatt
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY
(2017)
Meeting Abstract
Chemistry, Multidisciplinary
Chelsea DeLeon, Christopher Arnatt, David Q. -H. Wang, McKenna Wilhelm, Patrick Sweeney
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY
(2017)
Meeting Abstract
Chemistry, Multidisciplinary
Kristin Skubic, Miranda Adams, Jill Horn, Anna Priddy, Renae Oelrich, Michael Lewis, Brent Znosko, Christopher Arnatt
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY
(2017)
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
