Increased Plasma Concentrations of 6-oxo-Methylphenidate in CES1 G134E Carriers Following a Single Oral Dose of Methylphenidate [0.03%]
单次口服哌甲酯后CES1 G134E携带者的血浆6-氧代-甲基苯环利定浓度升高
Qingchen Zhang,Philip W Melchert,Ahmed Awad et al.
Qingchen Zhang et al.
Attention-deficit/hyperactivity disorder (ADHD) is a neurodevelopmental disorder, with methylphenidate used as a first-line treatment. Methylphenidate is primarily hydrolyzed by carboxylesterase 1 (CES1) to inactive ritalinic acid, with min...
IND-Enabling Preclinical Studies of [11C]COU, a Trapped Metabolite PET Radiotracer for Monoamine Oxidase-B [0.03%]
一种单胺氧化酶B的PET放射示踪剂[11C]COU被俘获代谢物的药代动力学预临床研究
Madison Frazier,Tanpreet Kaur,Jenelle Stauff et al.
Madison Frazier et al.
[11C]COU is a trapped metabolite radiotracer for in vivo analysis of Monoamine Oxidase B activity using positron emission tomography (PET) imaging. [11C]COU has the potential to quantify astrocytosis in the early stages of Alzheimer's disea...
Peptide halogenation biochemistry: interfacing pharmaceutical deliverables with chemical innovation [0.03%]
肽卤化生物化学：药物传输与化工创新之间的接口问题研究
Vinayak Agarwal
Vinayak Agarwal
The biosynthetic schemes for the production of halogenated peptidic natural products offer avenues for the discovery of peptide halogenases, and opportunities for development of biocatalysts for derivatization of peptides and proteins. Here...
Discovery of CRBN-recruiting PROTAC degraders of the METTL3-METTL14 complex [0.03%]
发现CRBN募集型PROTAC降解METTL3-METTL14复合物的分子
Alexis R Smith,Rukiye Nar,Yafang Li et al.
Alexis R Smith et al.
METTL3 and METTL14, key components of the m6A writer complex, are frequently overexpressed in various malignancies, including acute myeloid leukemia (AML), where aberrant methylation has been linked to the upregulation of oncogenic transcri...
Anaeic and tumoic acids, new functionalized fatty acids from marine cyanobacteria, inhibit quorum sensing in Pseudomonas aeruginosa [0.03%]
来源于海洋蓝绿藻的两种新型功能化脂肪酸анаeic和tumoic酸可抑制铜绿假单胞菌的群体感应
Emma K Ellis,Sarath P Gunasekera,Sofia Kokkaliari et al.
Emma K Ellis et al.
Quorum sensing (QS) is the mechanism in which bacteria assess the threshold concentration of small signaling molecules to induce cell survival by overwhelming the host's defenses. It is one of the fundamental mechanisms controlling bacteria...
Halogenated quinoline kill agent rapidly induces iron starvation of Staphylococcal biofilms [0.03%]
卤代喹啉杀菌剂可快速导致金黄色葡萄球菌生物被膜铁缺乏
Robert W Huigens rd,Ke Liu,Nana Shao et al.
Robert W Huigens rd et al.
Bacterial biofilms are surface-attached communities comprised of slow- or non-replicating bacteria. Transcriptomic responses of bacterial biofilms to anti-biofilm small molecules have been largely unexplored, with existing studies typically...
CO prodrugs: A new scaffold of adamantane-fused norbornen-7-ones with tunable water solubility [0.03%]
含金刚烷并诺硼烯酮衍生物的CO前药类化合物及其制备和应用
Ce Yang,Xingyue Ji,G S Sainaga Jyothi Vaskuri et al.
Ce Yang et al.
We have had a long-standing interest in developing organic prodrugs for controlled delivery of CO for various therapeutic applications. Based on an earlier approach of taking advantage of a cheletropic extrusion reaction of norbornadienone ...
Targeting cAMP signaling and phosphodiesterase 4 for liver disease treatment [0.03%]
瞄准cAMP信号传导和磷酸二酯酶4以治疗肝病
Jingyi Ma,Dalton W Staler,Ram I Mahato
Jingyi Ma
Liver disease is a significant health burden globally and accounts for 4% of total deaths annually. Alcoholic liver disease (ALD) and metabolism-associated fatty liver disease (MAFLD) are the leading causes of cirrhosis. Extensive studies h...
Iron Porphyrin-mediated Production of Carbon Monoxide from Phenylpyruvic Acid: From Potential Therapeutic and Diagnostic Use to Physiological Implications [0.03%]
铁泊酚介导的苯丙酮酸生成一氧化碳：从潜在的治疗和诊断应用到生理意义
Wen Lu,Rujuta Ghorpade,Xiaoxiao Yang et al.
Wen Lu et al.
Because of CO's known endogenous signaling roles and its demonstrated pharmacological activity at low and safe concentrations, there is considerable interest in chemical strategies that allows for generation of carbon monoxide from organic ...
Quinazolinone-based Subchemotypes for Targeting HIV-1 Capsid Protein: Design and Synthesis [0.03%]
基于喹唑啉酮的HIV-1衣壳蛋白靶向亚化学型的设计与合成
Thamina Akther,William M McFadden,Huanchun Zhang et al.
Thamina Akther et al.
The recent FDA-approval of lenacapavir (LEN, GS-6207) and the subsequent discovery of GSK878 strongly validate HIV-1 capsid protein (CA) as a target for antiviral development. However, multiple single mutations drastically reduced the susce...