Results 11 to 20 of about 8,212 (230)

PROTAC-Splitter: a machine learning framework for automated identification of PROTAC substructures

Journal of Cheminformatics
Proteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules composed of an E3 ligase ligand, a linker, and a warhead targeting a protein of interest. Despite their modular structure, accurately identifying and annotating these components in
Stefano Ribes, Ranxuan Zhang, Télio Cropsal, Anders Källberg, Christian Tyrchan, Eva Nittinger, Rocío Mercado   +6 more
doaj   +6 more sources

Frontiers in PROTACs [PDF]

Drug Discovery Today, 2021
Targeting protein-protein interactions (PPI) is a key focus in the development of new and emerging small-molecule therapeutics. Shallow interacting surfaces can render PPI targeting notoriously difficult. This leaves many therapeutically captivating targets 'undruggable'.
Gregory R. Hughes, Ashley P. Dudey, Andrew M. Hemmings, Andrew Chantry   +3 more
openaire   +3 more sources

PROTAC-DB: an online database of PROTACs [PDF]

Nucleic Acids Research, 2020
Abstract Proteolysis-targeting chimeras (PROTACs), which selectively degrade targeted proteins by the ubiquitin-proteasome system, have emerged as a novel therapeutic technology with potential advantages over traditional inhibition strategies.
Gaoqi Weng, Chao Shen 0008, Dong-Sheng Cao 0001, Junbo Gao, Xiaowu Dong, Qiaojun He, Bo Yang 0023, Dan Li 0013, Jian Wu 0001, Tingjun Hou   +9 more
openaire   +3 more sources

Estrogen Receptor-α Targeting: PROTACs, SNIPERs, Peptide-PROTACs, Antibody Conjugated PROTACs and SNIPERs

Pharmaceutics, 2022
Targeting selective estrogen subtype receptors through typical medicinal chemistry approaches is based on occupancy-driven pharmacology. In occupancy-driven pharmacology, molecules are developed in order to inhibit the protein of interest (POI), and their popularity is based on their virtue of faster kinetics.
Arvind Negi, Kavindra Kumar Kesari, Anne Sophie Voisin-Chiret   +2 more
  +8 more sources

Recent Advances of Degradation Technologies Based on PROTAC Mechanism

Biomolecules, 2022
PROTAC (proteolysis-targeting chimeras), which selectively degrades target proteins, has become the most popular technology for drug development in recent years.
Mingchao Xiao, Jiaojiao Zhao, Qiang Wang, Jia Liu, Leina Ma   +4 more
doaj   +1 more source

PROTAC-DB 2.0: an updated database of PROTACs

Nucleic Acids Research, 2022
AbstractProteolysis targeting chimeras (PROTACs), which harness the ubiquitin-proteasome system to selectively induce targeted protein degradation, represent an emerging therapeutic technology with the potential to modulate traditional undruggable targets.
Gaoqi Weng, Xuanyan Cai, Dong-Sheng Cao 0001, Hongyan Du, Chao Shen 0008, Yafeng Deng, Qiaojun He, Bo Yang 0023, Dan Li 0013, Tingjun Hou   +9 more
openaire   +2 more sources

Innovative developments and emerging technologies in RNA therapeutics

RNA Biology, 2022
RNA-based therapeutics are emerging as a powerful platform for the treatment of multiple diseases. Currently, the two main categories of nucleic acid therapeutics, antisense oligonucleotides and small interfering RNAs (siRNAs), achieve their therapeutic ...
François Halloy, Annabelle Biscans, Katherine E. Bujold, Alexandre Debacker, Alyssa C. Hill, Aurélie Lacroix, Olivia Luige, Roger Strömberg, Linda Sundstrom, Jörg Vogel, Alice Ghidini   +10 more
doaj   +1 more source

PROTACs in gastrointestinal cancers

Molecular Therapy - Oncolytics, 2022
Proteolysis targeting chimera (PROTAC) presents a powerful strategy for targeted protein degradation (TPD). The heterobifunctional PROTAC molecule consists of an E3 ligase ligand covalently linked to a protein of interest (POI) via a linker. PROTAC can induce ubiquitinated proteasomal degradation of proteins by hijacking the ubiquitin-proteasome ...
Yu Chen, Qingfan Yang, Jinrun Xu, Liyao Tang, Yan Zhang, Fukuan Du, Yueshui Zhao, Xu Wu, Mingxing Li, Jing Shen, Ruilin Ding, Hongying Cao, Wanping Li, Xiaobing Li, Meijuan Chen, Zhigui Wu, Chi Hin Cho, Yu Du, Qinglian Wen, Zhangang Xiao   +19 more
openaire   +3 more sources

Degradation of proteins by PROTACs and other strategies

Acta Pharmaceutica Sinica B, 2020
Blocking the biological functions of scaffold proteins and aggregated proteins is a challenging goal. PROTAC proteolysis-targeting chimaera (PROTAC) technology may be the solution, considering its ability to selectively degrade target proteins.
Yang Wang, Xueyang Jiang, Feng Feng, Wenyuan Liu, Haopeng Sun   +4 more
doaj   +1 more source

H4K12 Lactylation Regulates NDUFS7 to Drive Microglia Reverse Electron Transport in Spinal Cord Injury. [PDF]

Adv Sci (Weinh)
Lactate accumulation after SCI promotes H4K12la lactylation, which upregulates NDUFS7, triggering mitochondrial RET and ROS, enforcing pro‐inflammatory microglial polarization. MM@mPTC, a biomimetic nanotherapeutic, degrades LDHA in activated microglia, reducing H4K12la lactylation and blocking RET, thus curbing ROS, fostering a reparative phenotype ...
Hong C, Jiang Z, Wu Z, Wu C, Liu J, Guo K, Liang Y, Xu S, Jin Y, Xiao Y, Guo L, Xu H, Sheng S, Wang C.   +13 more
europepmc   +2 more sources