Results 71 to 80 of about 522,643 (238)

dUTPase is essential in zebrafish development and possesses several single‐nucleotide variants with pronounced structural and functional consequences

FEBS Open Bio, EarlyView.
dUTPases are involved in balancing the appropriate nucleotide pools. We showed that dUTPase is essential for normal development in zebrafish. The different zebrafish genomes contain several single‐nucleotide variations (SNPs) of the dut gene. One of the dUTPase variants displayed drastically lower protein stability and catalytic efficiency as compared ...
Viktória Perey‐Simon, Angéla Békesi, Latifa Kazzazy, Jázmin Mihály, Máté Varga, Beáta G. Vértessy, Kinga Nyíri   +6 more
wiley   +1 more source

Target‐Mediated Drug Disposition (TMDD) Revisited: High Versus Low‐Affinity Approximations of the TMDD Model

CPT: Pharmacometrics & Systems Pharmacology
Target‐mediated drug disposition (TMDD) is often associated with high‐affinity binding to a target resulting in nonlinear pharmacokinetics. For large molecules, such as monoclonal antibodies, this can lead to increased clearance at sub‐saturating ...
Ronny Straube
doaj   +1 more source

Temperature-sensitive protein–DNA dimerizers [PDF]

, 2005
Programmable DNA-binding polyamides coupled to short peptides have led to the creation of synthetic artificial transcription factors. A hairpin polyamide-YPWM tetrapeptide conjugate facilitates the binding of a natural transcription factor Exd to an ...
Ansari, Aseem Z., Arndt, Hans-Dieter, Dervan, Peter B., Hauschild, Karl E., Metzler, Renee E., Moretti, Rocco, Raffaelle, Marni   +6 more
core   +1 more source

The cooperative regulation of miR‐221 by APE1 and AUF1 impacts p27Kip1 defining a miR signature relevant for cervical cancer

FEBS Open Bio, EarlyView.
A regulatory axis involving APE1, AUF1, and miR‐221 is proposed. Pri‐miR‐221 is processed by DROSHA and DICER to generate mature miR‐221, which targets p27Kip1 mRNA. APE1 and AUF1 compete for pre‐miR‐221 binding. Reduced APE1/AUF1 levels impair miR‐221 biogenesis, decrease p27Kip1 mRNA degradation, and promote cell cycle progression, chemoresistance ...
Matilde Clarissa Malfatti, Nicolò Gualandi, Gianluca Tell, Giulia Antoniali   +3 more
wiley   +1 more source

DTBind: A Mechanism-Driven Deep Learning Framework for Accurate Prediction of Drug–Target Molecular Recognition

Research
Accurate prediction of drug–target molecular recognition is essential for early-stage drug discovery, spanning binding occurrence, binding site localization, and binding affinity estimation.
Qiuyu Li, Zeyu Xu, Yanhao Zhu, Wanyun Zhou, Mingming Guan, Shiqing Zhao, Mengyuan Liu, Bin Liu, Juntao Liu   +8 more
doaj   +1 more source

Identification of functional murine mitochondrial formyl peptides and their effects on myeloid‐derived suppressor cell generation

FEBS Open Bio, EarlyView.
We first identified functional murine mitochondrial N‐formyl peptides (MT‐FPs) and investigated their effects on the in vitro myeloid‐derived suppressor cell (MDSC) generation from bone marrow cells. We demonstrated that MT‐FPs acted directly on bone marrow cells to promote MDSC generation and modulated the polymorphonuclear (PMN)‐MDSC/monocyte (M ...
Miyako Ozawa, Saori Kagoshima, Akira Yamada   +2 more
wiley   +1 more source

Fluoxetine: a case history of its discovery and preclinical development [PDF]

, 2014
Introduction: Depression is a multifactorial mood disorder with a high prevalence worldwide. Until now, treatments for depression have focused on the inhibition of monoaminergic reuptake sites, which augment the bioavailability of monoamines in the CNS ...
Bel N, Bergstrom RF, Bravo L, Bremner JD, Burrows GD, Chouinard G, Datla KP, Esther Berrocoso, Juan Antonio Mico, Kreiss DS, Laura Perez-Caballero, Lemberger L, Li Q, Lidia Bravo, Maj J, Nibuya M, Owens MJ, Rutter JJ, Sonia Torres-Sanchez, Stevens JC, Wong DT   +20 more
core   +2 more sources

Development of human monoclonal antibodies against TARM1 by yeast display

FEBS Open Bio, EarlyView.
Human monoclonal antibodies against TARM1 are generated by yeast display‐guided selection. These antibodies bind to soluble and cell‐surface forms of TARM1. Also, these antibodies exhibit agonistic activity in the NFAT‐GFP reporter assay, indicating that TARM1 signaling can be functionally modulated by antibodies and suggesting TARM1 as a potential ...
Rikio Yabe, Mayumi Saeki, Masaaki Hashiguchi, Sayaka Ono, Kazuhisa Aoki, Hidetaka Tanno   +5 more
wiley   +1 more source

In vitro and in vivo evaluation of cephalosporins for the treatment of Lyme disease. [PDF]

, 2018
BackgroundLyme disease accounts for >90% of all vector-borne disease cases in the United States and affect ~300,000 persons annually in North America.
Ambati, Aditya, Babar, Mustafeez Mujtaba, Inayathullah, Mohammed, Kim, Kwang-Min, Maguire, Peter, Parekh, Mansi B, Pothineni, Venkata Raveendra, Potula, Hari-Hara Sk, Rajadas, Jayakumar, Tayebi, Lobat   +9 more
core  

Structure based de novo design of IspD inhibitors as anti-tubercular agents [PDF]

, 2012
Tuberculosis is one of the leading contagious diseases, caused by Mycobacterium tuberculosis. Despite improvements in anti-tubercular agents, it remains one of the most prevalent infectious diseases worldwide, responsible for a total of 1.6 million ...
Abhay T. Sangamwar, Gaurao V. Dhoke, Rahul P. Gangwal, Rohith Anand Varikoti, Venkata Krishnan Ramaswamy   +4 more
core   +2 more sources