Article
Pediatrics
Danijela Petkovic Ramadza, Ivana Kuhtic, Kamelija Zarkovic, Hanns Lochmuller, Mislav Cavka, Ida Kovac, Ivo Baric, Maja Prutki
Summary: This study analyzed the skeletal muscles of three brothers with S-Adenosylhomocysteine hydrolase deficiency (SAHHD) using MRI and MRS, and found that the extent of muscle involvement increased with age, especially in the proximal skeletal muscle groups of the lower extremities. These findings demonstrate the importance of MRI and MRS in understanding muscle involvement and treatment response in SAHHD.
FRONTIERS IN PEDIATRICS
(2022)
Article
Biochemistry & Molecular Biology
Yiran You, Xu Chen, Yu Chen, Juan Pang, Qian Chen, Qiannan Liu, Hongliang Xue, Yupeng Zeng, Jinghe Xiao, Jiaxin Mi, Yi Tang, Wenhua Ling
Summary: This study aimed to investigate whether the inhibition of S-adenosylhomocysteine hydrolase (SAHH) accelerates vascular senescence and the development of atherosclerosis. The results showed that SAHH inhibition leads to vascular senescence and atherosclerosis by repressing DNA methylation and upregulating Drp1 expression. This identifies SAHH or SAH as potential therapeutic targets for vascular senescence and cardiovascular diseases.
Article
Chemistry, Multidisciplinary
Jose J. Garrido-Gonzalez, Estela Sanchez-Santos, Asmaa Habib, Angel Cuevas Ferreras, Francisca Sanz, Joaquin R. Moran, Angel L. Fuentes de Arriba
Summary: In recent decades, there has been much interest in synthesizing small molecules that can mimic the active site of hydrolytic enzymes, but it remains challenging to prepare suitable small-molecule mimics. The newly proposed synthetic artificial enzymes are able to perform transesterification of non-activated esters under mild and neutral reaction conditions.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Article
Biochemistry & Molecular Biology
Masayuki Nakanishi, Mami Hino, Hiroshi Nomoto
Summary: In this study, a null mutant of the SAH hydrolase gene was created in Trypanosoma brucei and surprisingly, despite the observed SAH accumulation, the mutant exhibited normal cell proliferation. This suggests that inhibiting SAH hydrolase may not be an effective approach to suppressing T. brucei proliferation, making the enzyme a less promising target for antitrypanosome drug development.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2023)
Review
Biochemistry & Molecular Biology
Atif Khurshid Wani, Nahid Akhtar, Tahir ul Gani Mir, Rattandeep Singh, Prakash Kumar Jha, Shyam Kumar Mallik, Shruti Sinha, Surya Kant Tripathi, Abha Jain, Aprajita Jha, Hari Prasad Devkota, Ajit Prakash
Summary: Apoptosis is the process of eliminating non-essential, neoplastic, and infected cells through regulated pathways. Loss of apoptosis control can lead to cancer cell survival, accumulation of mutations, and tumor progression. The apoptotic pathway has been studied as a potential drug target in cancer treatment, but concerns regarding off-target activities have emerged. Phytochemicals and plant-based nanoparticles show promise in cancer treatment by targeting programmed cell death network.
Article
Biochemistry & Molecular Biology
Gokhan Zengin, Dejan Stojkovic, Mohamad Fawzi Mahomoodally, Bibi Sharmeen Jugreet, Mehmet Yavuz Paksoy, Marija Ivanov, Uros Gasic, Monica Gallo, Domenico Montesano
Summary: This study demonstrated interesting bioactive components in two Seseli species, particularly polyphenolics, and showed several biological properties that could be further investigated for their potential exploitation as healing agents.
Article
Multidisciplinary Sciences
Katsutaka Mitachi, Kyohei Ariake, Hiroki Shima, Satoko Sato, Takayuki Miura, Shimpei Maeda, Masaharu Ishida, Masamichi Mizuma, Hideo Ohtsuka, Takashi Kamei, Kazuhiko Igarashi, Michiaki Unno
Summary: The study identified C1TC and SAHH as novel biomarkers for predicting the sensitivity of PDAC patients to 5-FU chemotherapy based on CD-DST results. These proteins significantly improved recurrence-free survival in patients and showed potential for use as substitutes for CD-DST in adjuvant chemotherapy for PDAC.
SCIENTIFIC REPORTS
(2021)
Article
Chemistry, Medicinal
Alessandro Papa, Silvia Pasquini, Francesca Galvani, Mariarosaria Cammarota, Chiara Contri, Gabriele Carullo, Sandra Gemma, Anna Ramunno, Stefania Lamponi, Beatrice Gorelli, Simona Saponara, Katia Varani, Marco Mor, Giuseppe Campiani, Francesca Boscia, Fabrizio Vincenzi, Alessio Lodola, Stefania Butini
Summary: The neuroprotective performance of the endocannabinoid system (ECS) against neuroinflammation can be significantly enhanced by inhibiting the key ECS enzyme FAAH. In this study, a series of carbamate-based FAAH inhibitors were developed with improved drug properties compared to previous analogues. These inhibitors showed nanomolar potency, good water solubility, and chemical stability. They exhibited excellent selectivity against monoacylglycerol lipase and cannabinoid receptors, and demonstrated reversible mechanisms of action without toxicity or cardiac effects. Selected analogues displayed notable neuroprotective effects against oxidative stress and neuroinflammation.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Pharmacology & Pharmacy
Swati Lamba, Amit Roy
Summary: DNA topoisomerases are enzymes found in all organisms and play a crucial role in maintaining DNA structure during various cellular processes. The structure of topoisomerases in protozoan parasites differs from that of humans, making it a promising target for drug development against parasitic diseases. This review discusses the recent progress in the development of investigational and repurposed topoisomerase inhibitors for protozoan parasites.
DRUG DISCOVERY TODAY
(2023)
Article
Chemistry, Multidisciplinary
Lilian Penalver, Philipp Schmid, David Szamosvari, Stefan Schildknecht, Christoph Globisch, Kevin Sawade, Christine Peter, Thomas Boettcher
Summary: Activity-based probes are valuable tools for chemical biology, but the challenge of finding probes that specifically target enzyme active sites remains. A ligand selection strategy was introduced to tailor electrophilic probes to a desired target, showcasing its efficacy on the cysteine proteases of SARS-CoV-2. This strategy enabled the development of specific probes for active site labeling with sufficient selectivity, leading to the discovery of potential inhibitors.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Multidisciplinary Sciences
Lena Barra, Takayoshi Awakawa, Kohei Shirai, Zhijuan Hu, Ghader Bashiri, Ikuro Abe
Summary: Beta-NAD functions as a key metabolite in living organisms, playing roles in diverse biological processes including secondary metabolite biosynthesis pathways. This study's findings set the stage for the discovery and exploitation of natural products derived from beta-NAD.
Review
Medicine, Research & Experimental
YoungJo Yoo, Eun Choi, Yejin Kim, Yunyoung Cha, Eunhye Um, Younghwa Kim, Yunji Kim, Yun-Sil Lee
Summary: CTSS overexpression can lead to various pulmonary pathological processes, including pulmonary fibrosis. Compared to other members of the cysteine cathepsin family, CTSS has unique characteristics, retaining its enzyme activity at neutral pH. Studies have shown that CTSS mediates pulmonary fibrosis in a unique manner.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Review
Biochemistry & Molecular Biology
Malcolm A. Leissring, Carlos M. Gonzalez-Casimiro, Beatriz Merino, Caitlin N. Suire, German Perdomo
Summary: Hepatic insulin clearance and the activity of insulin-degrading enzyme might be involved in the pathogenesis of type 2 diabetes mellitus, and the development of IDE inhibitors as therapeutics for diabetic patients has garnered attention.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Oncology
Abdelhakim Bouyahya, Aicha El Allam, Sara Aboulaghras, Saad Bakrim, Naoual El Menyiy, Mohammed Merae Alshahrani, Ahmed Abdullah Al Awadh, Taoufiq Benali, Learn-Han Lee, Nasreddine El Omari, Khang Wen Goh, Long Chiau Ming, Mohammad S. Mubarak
Summary: This review provides an overview of the recent developments in the mTOR signaling pathway and its molecular involvement in various human cancer types, as well as the research progress of different mTOR inhibitors and their rational combinations with immunotherapies.
Review
Biochemistry & Molecular Biology
Siqi Peng, Huizhen Wang, Zhengtao Wang, Qingzhong Wang
Summary: Viral DNA and RNA polymerases are crucial enzymes in synthesizing genetic materials of viruses, serving as attractive targets for antiviral drug development. Due to similarities in viral polymerases, inhibitors designed for one type of virus can be effective on others. This review discusses the development of viral polymerase inhibitors and proposes future strategies for antiviral drug development.
