Results 191 to 200 of about 37,458 (256)

Correction for Mittal et al., Mechanisms underlying allosteric modulation of antiseizure medication binding to synaptic vesicle protein 2A (SV2A). [PDF]

Proc Natl Acad Sci U S A
europepmc   +1 more source

Conformational diversity in class C GPCR positive allosteric modulation. [PDF]

Nat Commun
Cannone G, Berto L, Malhaire F, Ferguson G, Fouillen A, Balor S, Font-Ingles J, Llebaria A, Goudet C, Kotecha A, K R V, Lebon G.   +11 more
europepmc   +1 more source

An intracellular recombinant single‐chain variable antibody fragment as a new class of phosphodiesterase type 5 inhibitors

British Journal of Pharmacology, EarlyView.
Background and Purpose Cyclic guanosine monophosphate (cGMP) is a ubiquitous second messenger involved in human (patho‐)physiology. Phosphodiesterase 5 (PDE5) is a major cGMP hydrolyzing enzyme in many cell types including vascular smooth muscle cells (VSMCs). Several highly selective PDE5 inhibitors are in clinical use. However, there are currently no
Kürsat Kirkgöz, Sophie Sprenger, Olga Schweigert, Sanika Mohagaonkar, Matti Walsdorff, Tanja Zeller, Filip Berisha, Viacheslav O. Nikolaev, Sergei D. Rybalkin   +8 more
wiley   +1 more source

Positive allosteric modulation of a GPCR ternary complex. [PDF]

Sci Adv
Burger WAC, Draper-Joyce CJ, Valant C, Christopoulos A, Thal DM.   +4 more
europepmc   +1 more source

Novel approaches for drug development against chronic primary pain: A systematic review

British Journal of Pharmacology, EarlyView.
Abstract Chronic primary pain (CPP) persisting for more than 3 months, associated with significant emotional distress without any known underlying cause, is an unmet medical need. Traditional or adjuvant analgesics do not provide satisfactory pain relief for a great proportion of these patients.
Valéria Tékus, Éva Borbély, Andreas Goebel, Ralf Baron, Zsófia Hajna, Zsuzsanna Helyes   +5 more
wiley   +1 more source

Allosteric modulation of proton binding confers Cl- activation and glutamate selectivity to vesicular glutamate transporters. [PDF]

PLoS Comput Biol
Borghans B, Kortzak D, Longo P, Kolen B, Machtens JP, Fahlke C.   +5 more
europepmc   +1 more source

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source

Presynaptic hyperexcitability reversed by positive allosteric modulation of a GABABR epilepsy variant. [PDF]

Brain
Minere M, Mortensen M, Dorovykh V, Warnes G, Nizetic D, Smart TG, Hannan SB.   +6 more
europepmc   +1 more source

Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries

British Journal of Pharmacology, EarlyView.
Abstract Protein–protein interactions (PPIs) are central to diverse cellular functions, and represent a rapidly expanding class of therapeutic targets. Advancements in covalent drug design have enabled small‐molecule drugs to overcome challenges associated with engaging these targets, such as limited durations of action and difficult‐to‐drug (expansive,
Ruchira Basu, Steven Fletcher
wiley   +1 more source

ROS-induced allosteric modulation of NikR promotes <i>Helicobacter pylori</i> biofilm formation by attenuating FlgR-dependent inhibition of the molybdate transport system. [PDF]

Virulence
Zheng Y, Li S, Xue J, Zhang L, Wang L, Zhao Y, Zhang W, Ma W, Liu J, Sun Y, Sun Y.   +10 more
europepmc   +1 more source