Article
Biochemistry & Molecular Biology
Arno Kirchhain, Asta Zubriene, Visvaldas Kairys, Federico Vivaldi, Andrea Bonini, Denise Biagini, Delio Santalucia, Daumantas Matulis, Fabio Di Francesco
Summary: Matrix metalloproteinases play a crucial role in cancer progression and metastasis, and molecular probes have been successfully used to study their activity. In this study, a series of MMP-2 and MMP-9 binding probes were synthesized, showing high selectivity against MMP-2 and potential for sensor fabrication. The experimental results were confirmed by molecular modeling, indicating the potential application of these probes for targeted enzyme detection.
BIOORGANIC CHEMISTRY
(2021)
Article
Oncology
Haohao Lu, Bin Liang, Xiangwen Xia, Chuansheng Zheng
Summary: TACE combined with Donafenib and Toripalimab demonstrates superior efficacy and safety compared to TACE combined with Sorafenib in treating unresectable HCC patients. This combination therapy not only improves the objective response rate and disease control rate, but also prolongs progression-free survival and overall survival. Additionally, the occurrence of treatment-related adverse events is lower in the TACE + Donafenib + Toripalimab group compared to the TACE + Sorafenib group.
Review
Oncology
Ruihua Duan, Fen Gong, Yan Wang, Caixia Huang, Jiaming Wu, Leihao Hu, Min Liu, Shijun Qiu, Liming Lu, Yisheng Lin
Summary: This meta-analysis suggests that TACE plus TKIs may have benefits for patients with unresectable hepatocellular carcinoma in terms of TTP, OS, and tumor response rates. However, combination therapy is also associated with a significantly increased risk of adverse reactions. Therefore, the clinical benefits and risks of combination therapy must be evaluated.
WORLD JOURNAL OF SURGICAL ONCOLOGY
(2023)
Review
Biochemistry & Molecular Biology
Il-Sup Kim, Woong-Suk Yang, Cheorl-Ho Kim
Summary: MMPs are enzymes that play a key role in promoting cell migration by degrading the extracellular matrix (ECM). They are upregulated in cancers and inflamed regions. TIMPs are highly specific inhibitors of MMPs, regulating their activity and potentially playing a role in inhibiting MMP-dependent diseases.
CURRENT MEDICINAL CHEMISTRY
(2023)
Article
Gastroenterology & Hepatology
Jiaxi Liu, Peng Wang, Liqi Shang, Zhoubo Zhang, Yulong Tian, Xiaowei Chen, Yanan Ma, Haibo Shao
Summary: Based on the meta-analysis and trial sequential analysis, TACE + T + I demonstrated better therapeutic efficacy compared to TACE + T for patients with BCLC intermediate- or advanced-stage HCC, without a significant increase in adverse events.
HEPATOLOGY INTERNATIONAL
(2023)
Article
Multidisciplinary Sciences
Kohei Umedera, Atsushi Yoshimori, Juergen Bajorath, Hiroyuki Nakamura
Summary: New inhibitors of matrix metalloproteinase 1 (MMP-1) were predicted using the structure-activity relationship (SAR) transfer method based on analogues of kinesin-like protein 11 (KIF11) inhibitors. Synthesized compounds 5-7 showed high potency against MMP-1, with compound 6 having about 3.5 times higher inhibitory activity than compound 4. This increased activity may be attributed to a halogen bond interaction between the Cl substituent of compound 6 and residue ARG214 of MMP-1.
SCIENTIFIC REPORTS
(2022)
Article
Oncology
Suellen Herbster, Marina Trombetta-Lima, Paulo Thiago de Souza-Santos, Andressa Paladino, Caio Raony Farina Silveira, Mari Cleide Sogayar, Luisa Lina Villa, Ana Paula Lepique, Enrique Boccardo
Summary: Studies have shown that overexpression of RECK (Reversion-inducing Cysteine-rich protein with Kazal motifs) reduces the tumorigenic potential of cervical cancer cells and can alter the inflammatory infiltrating cells in tumors. Additionally, down regulation of RECK is a consistent and clinically relevant event in the natural history of cervical cancer.
Article
Chemistry, Applied
Gemma Leone, Simone Pepi, Marco Consumi, Stefania Lamponi, Marco Fragai, Marco Martinucci, Veronica Baldoneschi, Oscar Francesconi, Cristina Nativi, Agnese Magnani
Summary: The functionalization of sodium hyaluronate with a small molecule MMPI resulted in the derivative HA-MMPI, which showed increased resistance to degradation, viscoelastic properties similar to healthy human synovial fluid, compatibility with chondrocytes, and affinity towards MMP12. Therefore, HA-MMPI can be considered a promising viscosupplement for the treatment of knee osteoarticular disease.
CARBOHYDRATE POLYMERS
(2021)
Review
Biochemistry & Molecular Biology
Zainab Ahmed Rashid, Sanaa K. Bardaweel
Summary: Matrix metalloproteinases (MMPs), especially MMP-9, play a significant role in cancer pathogenesis and progression. However, no effective MMP-9 inhibitor has been approved by the FDA. This review focuses on exploring the strategies for designing MMP-9 inhibitors and their anticancer effects.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Oncology
Haohao Lu, Chuansheng Zheng, Bin Xiong, Xiangwen Xia
Summary: This study aimed to investigate the need for combining transcatheter arterial chemoembolization (TACE) with antiviral therapy in HBV-related hepatocellular carcinoma (HCC) patients. The results showed that TACE combined with entecavir and TACE combined with tenofovir had higher efficacy and safety, but tenofovir had some impact on renal function.
Article
Chemistry, Medicinal
Ariel Buchler, Uzair S. Ismailani, Nicole MacMullin, Faduma Abdirahman, Myriam Adi, Christina Bi, Catherine Jany, Jeffrey W. Keillor, Benjamin H. Rotstein
Summary: A series of MMP-13 inhibitors were synthesized and radiolabeled to visualize atherosclerotic plaques. Three promising radiotracer candidates were identified and characterized in atherosclerotic mice. [18F]5j was found to specifically bind to MMP-13 within plaques and demonstrate favorable pharmacokinetic properties for vascular imaging.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Liyun Zheng, Shiji Fang, Fazong Wu, Weiqian Chen, Minjiang Chen, Qiaoyou Weng, Xulu Wu, Jingjing Song, Zhongwei Zhao, Jiansong Ji
Summary: The study compared the efficacy and safety of TACE+Sor group and TACE+Sor+ICIs group in treating intermediate and advanced TACE-refractory HCC, showing that TACE+Sor+ICIs group had a higher disease control rate and prolonged PFS and OS.
FRONTIERS IN MOLECULAR BIOSCIENCES
(2021)
Review
Pharmacology & Pharmacy
Kang Fu, Xueyao Zheng, Yuhan Chen, Liuying Wu, Zhiming Yang, Xu Chen, Wei Song
Summary: Diabetic foot ulcers (DFUs) are serious complications of diabetes mellitus, characterized by tissue destruction in the foot. Matrix metalloproteinases (MMPs) play crucial roles in the pathogenesis and wound healing process of DFUs. Overexpression of MMPs in DFUs can result in excessive tissue degradation and impaired wound healing. Regulation of MMP levels may facilitate wound healing in DFUs.
FRONTIERS IN PHARMACOLOGY
(2022)
Review
Biochemistry & Molecular Biology
Gianmarco Marciano, Cristina Vocca, Vincenzo Rania, Rita Citraro, Giovambattista De Sarro, Luca Gallelli
Summary: Matrix metalloproteinases (MMPs) are zinc-dependent proteolytic enzymes involved in extracellular matrix protein turnover and tissue degradation. They have been found to play a role in the modulation of neuropathic and nociceptive pain. However, the heterogeneity of clinical and pre-clinical data poses a challenge in this experimental context. Despite numerous studies on MMP inhibitors, these drugs have shown limited efficacy and significant side effects. This manuscript reviews the literature on the possible role of MMPs in pain and the effects of their modulation.
Article
Biochemistry & Molecular Biology
Mohammed M. M. Alshehri, Ammar Usman Danazumi, Mohammed Kanan Alshammari, Ridwan Opeyemi Bello, Mohammed Khalid Alghazwni, Ahmed Mughram Alshehri, Omaymah Mohammed Alshlali, Haruna Isiyaku Umar
Summary: Ubiquitin specific protease 30 (USP30) has been identified as a key player in mitochondrial dysfunction and impaired mitophagy in Parkinson's disease (PD). By recruiting ubiquitin that is supposed to bind with damaged mitochondria, USP30 poses a challenge when PINK1 and Parkin lose their functions. This study aims to repurpose approved inhibitors of MMP-9 and SGLT-2 as potential inhibitors of USP30 in PD through computational modeling. The findings suggest canagliflozin and empagliflozin as promising candidates for the treatment of PD. However, further experimental validation is needed.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Chemistry, Medicinal
Michael G. Yang, T. G. Murali Dhar, Zili Xiao, Hai-Yun Xiao, James J. -W. Duan, Bin Jiang, Michael A. Galella, Mark Cunningham, Jinhong Wang, Sium Habte, David Shuster, Kim W. McIntyre, Julie Carman, Deborah A. Holloway, John E. Somerville, Steven G. Nadler, Luisa Salter-Cid, Joel C. Barrish, David S. Weinstein
JOURNAL OF MEDICINAL CHEMISTRY
(2015)
Article
Chemistry, Medicinal
Hua Gong, David S. Weinstein, Zhonghui Lu, James J. -W. Duan, Sylwia Stachura, Lauren Haque, Ananta Karmakar, Hemalatha Hemagiri, Dhanya Kumar Raut, Arun Kumar Gupta, Javed Khan, Dan Camac, John S. Sack, Andrew Pudzianowski, Dauh-Rurng Wu, Melissa Yarde, Ding-Ren Shen, Virna Borowski, Jenny H. Xie, Huadong Sun, Celia D'Arienzo, Marta Dabros, Michael A. Galella, Faye Wang, Carolyn A. Weigelt, Qihong Zhao, William Foster, John E. Somerville, Luisa M. Salter-Cid, Joel C. Barrish, Percy H. Carter, T. G. Murali Dhar
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2018)
Article
Chemistry, Medicinal
James J. -W. Duan, Lihua Chen, Zhonghui Lu, Chu-Biao Xue, Rui-Qin Liu, Maryanne B. Covington, Mingxin Qian, Zelda R. Wasserman, Krishna Vaddi, David D. Christ, James M. Trzaskos, Robert C. Newton, Carl P. Decicco
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2008)
Article
Chemistry, Medicinal
Gregory R. Ott, Naoyuki Asakawa, Rui-Qin Liu, Maryanne B. Covington, Mingxin Qian, Krishna Vaddi, Robert C. Newton, James M. Trzaskos, David D. Christ, Laurine Galya, Thomas Scholz, Will Marshall, James J. -W. Duan
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2008)
Article
Chemistry, Medicinal
Gregory R. Ott, Naoyuki Asakawa, Zhonghui Lu, Rajan Anand, Rui-Qin Liu, Maryanne B. Covington, Krishna Vaddi, Mingxin Qian, Robert C. Newton, David D. Christ, James M. Trzaskos, James J. -W. Duan
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2008)
Article
Chemistry, Medicinal
Gregory R. Ott, Naoyuki Asakawa, Zhonghui Lu, Rui-Qin Liu, Maryanne B. Covington, Krishna Vaddi, Mingxin Qian, Robert C. Newton, David D. Christ, James M. Traskos, Carl P. Decicco James
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2008)
Article
Chemistry, Medicinal
James J. -W. Duan, Zhonghui Lu, Bin Jiang, Bingwei V. Yang, Lidia M. Doweyko, David S. Nirschl, Lauren E. Haque, Shuqun Lin, Gregory Brown, John Hynes, John S. Tokarski, John S. Sack, Javed Khan, Jonathan S. Lippy, Rosemary F. Zhang, Sidney Pitt, Guoxiang Shen, William J. Pitts, Percy H. Carter, Joel C. Barrish, Steven G. Nadler, Luisa M. Salter-Cid, Murray McKinnon, Aberra Fura, Gary L. Schieven, Stephen T. Wrobleski
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2014)
Article
Chemistry, Medicinal
Kan He, Mingxin Qian, Harvey Wong, Stephen A. Bai, Bing He, Bernice Brogdon, James E. Grace, Baomin Xin, Jingtao Wu, Shelly X. Ren, Hang Zeng, Yuzhong Deng, Danielle M. Graden, Timothy V. Olah, Steve E. Unger, Joseph M. Luettgen, Robert M. Knabb, Donald J. Pinto, Patrick Y. S. Lam, James Duan, Ruth R. Wexler, Carl P. Decicco, David D. Christ, Scott J. Grossman
JOURNAL OF PHARMACEUTICAL SCIENCES
(2008)
Article
Chemistry, Medicinal
James J. -W. Duan, Zhohghui Lu, Bin Jiang, Sylwia Stachura, Carolyn A. Weigelt, John S. Sack, Javed Khan, Max Ruzanov, Michael A. Galella, Dauh-Rurng Wu, Melissa Yarde, Ding-Ren Shen, David J. Shuster, Virna Borowski, Jenny H. Xie, Lisa Zhang, Sridhar Vanteru, Arun Kumar Gupta, Arvind Mathur, Qihong Zhao, William Foster, Luisa M. Salter-Cid, Percy H. Carter, T. G. Murali Dhar
ACS MEDICINAL CHEMISTRY LETTERS
(2019)
Article
Chemistry, Medicinal
David Marcoux, James J. -W. Duan, Qing Shi, Robert J. Cherney, Anurag S. Srivastava, Lyndon Cornelius, Douglas G. Batt, Qingjie Liu, Myra Beaudoin-Bertrand, Carolyn A. Weigelt, Purnima Khandelwal, Sureshbabu Vishwakrishnan, Kumaravel Selvakumar, Ananta Karmakar, Arun Kumar Gupta, Mushkin Basha, Sridharan Ramlingam, Naveen Manjunath, Sridhar Vanteru, Sukhen Karmakar, Nageswara Maddala, Muthalagu Vetrichelvan, Anuradha Gupta, Richard A. Rainpulla, Arvind Mathur, Shiuhang Yip, Peng Li, Dauh-Rurng Wu, Javed Khan, Max Ruzanov, John S. Sack, Jinhong Wang, Melissa Yarde, Mary Ellen Cvijic, Sha Li, David J. Shuster, Virna Borowski, Jenny H. Xie, Kim W. McIntyre, Mary T. Obermeier, Aberra Fura, Kevin Stefanski, Georgia Cornelius, John Hynes, Joseph A. Tino, John E. Macor, Luisa Salter-Cid, Rex Denton, Qihong Zhao, Percy H. Carter, T. G. Murali Dhare
JOURNAL OF MEDICINAL CHEMISTRY
(2019)
Article
Chemistry, Medicinal
Robert J. Cherney, Lyndon A. M. Cornelius, Anurag Srivastava, Carolyn A. Weigelt, David Marcoux, James J-W Duan, Qing Shi, Douglas G. Batt, Qingjie Liu, Shiuhang Yip, Dauh-Rurng Wu, Max Ruzanov, John Sack, Javed Khan, Jinhong Wang, Melissa Yarde, Mary Ellen Cvijic, Arvind Mathur, Sha Li, David Shuster, Purnima Khandelwal, Virna Borowski, Jenny Xie, Mary Obermeier, Aberra Fura, Kevin Stefanski, Georgia Cornelius, Joseph A. Tino, John E. Macor, Luisa Salter-Cid, Rex Denton, Qihong Zhao, Percy H. Carter, T. G. Murali Dhar
ACS MEDICINAL CHEMISTRY LETTERS
(2020)
Article
Chemistry, Medicinal
Bin Jiang, James J. -W. Duan, Sylwia Stachura, Ananta Karmakar, Hemalatha Hemagiri, Dhanya Kumar Raut, Arun Kumar Gupta, Carolyn A. Weigelt, Javed Khan, John S. Sack, Dauh-Rurng Wu, Melissa Yarde, Ding-Ren Shen, Michael A. Galella, Arvind Mathur, Qihong Zhao, Luisa M. Salter-Cid, Percy H. Carter, T. G. Murali Dhar
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2020)
Article
Chemistry, Medicinal
Hai-Yun Xiao, Ning Li, James J-W Duan, Bin Jiang, Zhonghui Lu, Khehyong Ngu, Joseph Tino, Lisa M. Kopcho, Hao Lu, Jing Chen, Andrew J. Tebben, Steven Sheriff, ChiehYing Y. Chang, Joseph Yanchunas, Deepa Calambur, Mian Gao, David J. Shuster, Vojkan Susulic, Jenny H. Xie, Victor R. Guarino, Dauh-Rurng Wu, Kurt R. Gregor, Christine B. Goldstine, John Hynes, John E. Macor, Luisa Salter-Cid, James R. Burke, Patrick J. Shaw, T. G. Murali Dhar
JOURNAL OF MEDICINAL CHEMISTRY
(2020)
Article
Chemistry, Medicinal
James Kempson, Damaso Ovalle, Junqing Guo, Stephen T. Wrobleski, Shuqun Lin, Steven H. Spergel, James J. -W. Duan, Bin Jiang, Zhonghui Lu, Jagabandhu Das, Bingwei V. Yang, John Hynes, Hong Wu, John Tokarski, John S. Sack, Javed Khan, Gary Schieven, Yuval Blatt, Charu Chaudhry, Luisa M. Salter-Cid, Aberra Fura, Joel C. Barrish, Percy H. Carter, William J. Pitts
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2017)
Article
Chemistry, Medicinal
John Hynes, Hong Wu, James Kempson, James J. -W. Duan, Zhonghui Lu, Bin Jiang, Sylwia Stachura, John S. Tokarski, John S. Sack, Javed A. Khan, Jonathan S. Lippy, Rosemary F. Zhang, Sidney Pitt, Guoxiang Shen, Kate Gillooly, Kim McIntyre, Percy H. Carter, Joel C. Barrish, Steven G. Nadler, Luisa M. Salter-Cid, Aberra Fura, Gary L. Schieven, William J. Pitts, Stephen T. Wrobleski
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(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)