Results 151 to 160 of about 13,195 (282)

Rapid and high-throughput screening of proteolysis targeting chimeras using a dual-reporter system expressing fluorescence protein and luciferase

BMC Biology
Background Proteolysis targeting chimera (PROTAC), a novel drug discovery strategy, utilizes the ubiquitin–proteasome system to degrade target proteins in cells.
Shuai Meng, Yuan Meng, Xuena Yang, Wenwen Yu, Bole Li, Tianjun Liu, Jie Zhang, Xiubao Ren, Lin Zhang   +8 more
doaj   +1 more source

Opportunities and challenges of PROTAC in the treatment of protein-driven diseases

Results in Chemistry
Targeted protein degradation (TPD) has transformed the landscape of drug discovery by exploiting the ubiquitin-proteasome system (UPS) to eliminate, rather than inhibit, pathogenic proteins.
Zhe Zhou, Peng Liu, Yang Li, Xuelian Liu, Jinyao Li   +4 more
doaj   +1 more source

Smart Integration of Structural Biology and Medicinal Chemistry to Unlock Target‐Driven Drug Discovery

Medicinal Research Reviews, EarlyView.
ABSTRACT To enhance drug discovery efforts, medicinal chemists should evaluate, filter, and utilize relevant structural information about target proteins. Acquiring and interpreting protein structures is crucial for elucidating ligand‐receptor interactions and addressing ADME‐related considerations, making it an essential aspect of medicinal chemistry.
Matteo Rossi Sebastiano, Giulia Apprato, Serena Francisco, Giuseppe Ermondi, Giulia Caron   +4 more
wiley   +1 more source

Prospects and advances of PROTAC in the treatment of hematologic malignancies

Experimental Hematology & Oncology
Over the past years, target protein degradation (TPD) has emerged as a hot topic in treating hematologic malignancies out of its strong ability to eliminate pathological proteins precisely.
Xinyang Wang, Ming Zhang, Heng Mei
doaj   +1 more source

CENP-C unwraps the human CENP-A nucleosome through the H2A C-terminal tail

, 2019
Centromeres are defined epigenetically by nucleosomes containing the histone H3 variant CENP-A, upon which the constitutive centromere-associated network of proteins (CCAN) is built. CENP-C is considered to be a central organizer of the CCAN.
Ali-Ahmad, A., Bilokapic, S., Halic, M., Schäfer, I., Sekulic, N.   +4 more
core   +1 more source

Shining a Light on Proteolysis Targeting Chimeras [PDF]

ACS Central Science, 2019
Ellen Teichmann, Stefan Hecht
openaire   +2 more sources

Multi‐Targeting Ligands as Prospective Therapeutics for Alzheimer's Disease, a Prevalent Neurodegenerative Disorder: Mechanistic Insights, Emerging Targets and Drug Discovery Campaigns

Medicinal Research Reviews, EarlyView.
ABSTRACT Alzheimer's disease (AD) is a debilitating neurodegenerative condition characterized by progressive cognitive impairment, memory deterioration, and neuronal dysfunction. Its complex pathophysiology involves multiple interlinked processes, including amyloid‐β (Aβ) aggregation, tau hyperphosphorylation, oxidative stress, neuroinflammation ...
Amandeep Thakur, Mandeep Rana, Sakshi Vanjani, Kei‐Chi Liou, Rajeev Taliyan, Kunal Nepali, Chih‐Hao Yang   +6 more
wiley   +1 more source

In Silico Structure‐Guided Design of Peptide Candidates Targeting γ‐Secretase Subunit Assembly

Proteins: Structure, Function, and Bioinformatics, EarlyView.
ABSTRACT The γ‐secretase complex is a membrane‐embedded protease essential for intramembrane cleavage of substrates such as Notch receptors and the amyloid precursor protein (APP), processes central to cancer progression and Alzheimer's disease (AD) pathology.
Selcen Arı Yuka, Kübra Telli, Alper Yılmaz   +2 more
wiley   +1 more source

New generation estrogen receptor-targeted agents in breast cancer: present situation and future prospectives

Acta Materia Medica
Endocrine therapy that blocks estrogen receptor signaling has been effective for decades as a primary treatment choice for breast cancer patients expressing the estrogen receptor.
Jian Min, Xin Liu, Rouming Peng, Chun-Chi Chen, Wei Wang, Rey-Ting Guo   +5 more
doaj   +1 more source

Update on Non‐Biological and RNA‐Based Therapeutics in Chronic Inflammatory Diseases: Precision Medicine Through Small Molecules: An EAACI Position Paper

Allergy, EarlyView.
ABSTRACT In the last decades, critical advancements in research technology and knowledge on disease mechanisms steered therapeutic approaches for chronic inflammatory diseases towards unprecedented target specificity. For allergic and chronic lung diseases, biologic drugs pioneered this goal, acquiring on the way—through the clinical use of monoclonal ...
F. Roth‐Walter, I. M. Adcock, C. Benito‐Villalvilla, R. Bianchini, L. Bjermer, G. Caramori, L. Cari, K. F. Chung, Z. Diamant, I. Eguiluz‐Gracia, E. F. Knol, M. Jesenak, F. Levi‐Schaffer, G. Nocentini, L. O'Mahony, O. Palomares, F. Redegeld, M. Sokolowska, B. Van Esch, M. Zurlo, C. Stellato   +20 more
wiley   +1 more source