Results 231 to 240 of about 692,160 (279)

Rapid evolution and genetic basis of spinetoram resistance in Phthorimaea absoluta: evidence from six years of monitoring and laboratory selection

Pest Management Science, EarlyView.
Resistance to spinetoram in Phthorimaea absoluta is rapidly selected and functionally recessive at field‐relevant concentrations. Metabolic detoxification contributes partially, while cross‐resistance to spinosad and increased susceptibility to diamides and isoxazolines highlight practical options for resistance monitoring and insecticide rotation ...
Teófilo P. Langa, Vitor Quintela, Marcos de Oliveira, Herbert A. A. Siqueira   +3 more
wiley   +1 more source

The continuing significance of chiral agrochemicals

Pest Management Science, Volume 81, Issue 4, Page 1697-1716, April 2025.
In the time frame 2018–2023, around 43% of the 35 chiral agrochemicals introduced to the market (herbicides, fungicides, insecticides, acaricides, and nematicides) contain one or more stereogenic centers in the molecule, and almost 69% of them have been marketed as racemic mixtures of enantiomers or stereoisomers.
Peter Jeschke
wiley   +1 more source

Molecular glues: Recent advances in cereblon substrate identification and mechanistic insights

Smart Molecules, EarlyView.
Molecular glues exert diverse core biological functions by inducing or stabilizing protein–protein interactions, extending far beyond the traditional scope of targeted protein degradation. Key breakthroughs include expanded cereblon substrate recognition, sustained G protein‐coupled receptor megacomplex signaling, and the first orthosteric molecular ...
Qingyun Guan, Xiaoyu Shi, Qian Yang, Xiangyi Jiang, Xinyong Liu, Peng Zhan   +5 more
wiley   +1 more source

Evolutionary Mechanisms of Coagulation Factors in Cetaceans During Aquatic Adaptation

Integrative Zoology, EarlyView.
Compared with Bos taurus, T. truncatus showed shorter prothrombin time and thrombin time but prolonged activated partial thromboplastin time, indicating pathway‐specific remodeling of coagulation. Evolutionary analyses identified 18 positively selected genes and accelerated F11 evolution, while functional assays revealed increased coagulation factor ...
Wenjun Lv, Wanfei Deng, Fei Deng, Shixia Xu, Wenhua Ren   +4 more
wiley   +1 more source

Exploring Binding Pockets in the Conformational States of the SARS-CoV-2 Spike Trimers for the Screening of Allosteric Inhibitors Using Molecular Simulations and Ensemble-Based Ligand Docking. [PDF]

Int J Mol Sci
Gupta G, Verkhivker G.
europepmc   +1 more source

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Allosteric inhibitors of the STAT3 signaling pathway

European Journal of Medicinal Chemistry, 2020
Over-expression and/or hyperactivation of signal transducer and activator of transcription 3 (STAT3) signaling are found in various human diseases, including cancer, autoimmune disorders, and inflammatory diseases. Therefore, STAT3 represents a highly promising therapeutic target for the treatment of these diseases. However, the traditional orthosteric
Xiao-Fei Shen, Da Jia
exaly   +3 more sources

Quinoline and thiazolopyridine allosteric inhibitors of MALT1

Bioorganic and Medicinal Chemistry Letters, 2019
Quinolines and thiazolopyridines were developed as allosteric inhibitors of MALT1, with good cellular potency and exquisite selectivity. Mouse pharmacokinetic (PK) profiling showed these to have low in vivo clearance, and moderate oral exposure. The thiazolopyridines were less lipophilic than the quinolines, and one thiazolopyridine example was active ...
Nathanael Gray, Hao Wu, Lorena Fontán
exaly   +3 more sources

New Promise and Opportunities for Allosteric Kinase Inhibitors

Angewandte Chemie - International Edition, 2020
AbstractDrugs that function through allosteric inhibition of kinase signaling represent a promising approach for the targeted discovery of therapeutics. The majority of developed allosteric kinase inhibitors are characterized as type III and IV inhibitors that show good kinome selectivity but generally lack the subtype selectivity of same kinase family.
Xiaoyun Lu, Ke Ding, Ke Ding
exaly   +3 more sources

Allosteric inhibitors of chemoattractant receptors: opportunities and pitfalls

Trends in Pharmacological Sciences, 2008
Given the central role of chemokines in infection, inflammation and immunity, chemokine receptors are a prime target for pharmacological intervention, and more so after the recent approval of chemokine receptor inhibitors for HIV. Allosteric inhibitors offer a largely unexploited opportunity to interfere with and modulate chemokine receptor activation ...
M. Allegretti, R. Bertini, C. Bizzarri, A. Beccari, A. Mantovani, M. Locati   +5 more
openaire   +3 more sources

Designing Allosteric Inhibitors of Thrombin [PDF]

, 2011
VCU Theses and ...
Sidhu, Preetpal
openaire   +2 more sources