Results 231 to 240 of about 79,537 (266)

Cancer‐Associated BCL‐2 Mutants Reveal Mechanisms Towards Venetoclax Resistance

Advanced Science, EarlyView.
Venetoclax (VEN) resistance in chronic lymphocytic leukemia arises from diverse BCL2 mutations. We map mechanisms contributing to VEN resistance across common BCL‐2 variants. G101V and D103Y reduce drug binding and increase sequestration of pro‐apoptotic proteins. V156D blocks VEN allosterically.
Jonas Aufdermauer, Ian de Ridder, Mahjoobeh Ehsani, Marasim Khan, Justin Kale, Lukas P. Frenzel, David Andrews, Spyridoula Karamanou, Ana J. Garcia‐Saez, Geert Bultynck   +9 more
wiley   +1 more source

Data-Driven Predictions of Diastereoselectivity in Crystallization-Induced Diastereomer Transformations. [PDF]

Org Lett
McCormack SL, Sherman ER, Johnson JS, Sigman MS.   +3 more
europepmc   +1 more source

Pyrazole‐Derived Antibacterial Compounds Effectively Treat Methicillin‐Resistant Staphylococcus Aureus Infections by Inhibiting Aspartate Transcarbamoylase

Advanced Science, EarlyView.
This study unveils a novel antibacterial mechanism against MRSA, in which the compound Py‐27 selectively targets and inhibits aspartate transcarbamoylase (ATCase), a key enzyme in pyrimidine synthesis. This inhibition disrupts DNA replication, induces oxidative damage, leading to potent bactericidal activity.
Xiaorong Yang, Xinyuan Cao, Lixia Dai, Feng Yang, Jing Wang, Yudong Ma, Tong Bu, Zile Gong, Xueyan Liu, Changcai Bai, Xiaolou Miao, Xiaofei Shang   +11 more
wiley   +1 more source

Computational prediction of substrate scope of a homogeneous catalyst: the case of metal-free C-H borylation by a frustrated Lewis pair catalyst. [PDF]

Chem Sci
Nielsen JM, Rasmussen MH, Jensen JH.
europepmc   +1 more source

O‐GlcNAcylation Regulation of SNAP29‐Dependent Autophagy Activation Dictates Chemoresistance in Gastric Cancer

Advanced Science, EarlyView.
Model illustrating the proposed mechanism by which chemotherapy‐induced downregulation of OGT disrupts SNAP29 O‐GlcNAcylation, promoting STX17‐SNAP29‐VAMP8 SNARE complex assembly and protective autophagy, leading to chemoresistance, which in turn establishes a feedforward loop to perpetuate drug tolerance.
Liang Tang, Shaoji Zhao, Ziling Shao, Tao Luo, Baifu Peng, Yifan Liu, Jinning Ye, Jianjun Peng, Kaiyu Sun, Jianbo Xu   +9 more
wiley   +1 more source

Unactivated Photoredox C-H Amination with Diazirines: Access to Acyldiaziridines. [PDF]

Org Lett
Galaktionova DV, Maharaj V, Lopchuk JM.
europepmc   +1 more source

Trafficking Deficiency of TMEM175 Variants in Parkinson's Disease Pathogenesis and the Prospects of Precision Medicine

Advanced Science, EarlyView.
This study identifies that the PD‐associated TMEM175‐L156P variant disrupts lysosomal ion channel trafficking by causing aberrant endoplasmic reticulum retention. A “chaperone–agonist” bifunctional small molecule restores TMEM175‐L156P lysosomal localization and channel function, thereby alleviating PD‐relevant cellular phenotypes and highlighting a ...
Ting Luo, Yu He, Shuyao Li, Haoyu Guan, Ruili Cui, Yu Shi, Zhongwen Jiang, Siyu Wang, Xuan Li, Jiyuan Li, Mei Hu, Yupeng Zhou, Beisha Tang, Yanyan Zhang, Zhaobing Gao, Yu Zhou, Zhenhua Liu, Ping Li   +17 more
wiley   +1 more source

Creating a non-native bio-amidation activity in asparagine synthetase <i>via</i> biosensor-guided directed evolution for the synthesis of (<i>S</i>)-2-aminobutyramide. [PDF]

Chem Sci
Lai Q, Meng Y, Liu Z, Han L, Guo J, Peplowski L, Cheng Z, Zhou Z.   +7 more
europepmc   +1 more source

CLRe: A Synergistic Dual‐Engine Framework for One‐Step Retrosynthesis Prediction

Advanced Science, EarlyView.
CLRe uses a contrastive difficulty score to order pretrained seq2seq fine‐tuning for retrosynthesis. Reaction embeddings define the ranking score, and a cumulative easy‐to‐hard schedule expands from the easiest subset to the full training set while earlier examples remain active.
Tianhao Su, Xitao Wang, Musen Li, Guanhua Qin, Shunbo Hu, Tong‐Yi Zhang   +5 more
wiley   +1 more source