Results 231 to 240 of about 107,657 (326)

Discovery of VU0467319: an M₁ Positive Allosteric Modulator Candidate That Advanced into Clinical Trials. [PDF]

ACS Chem Neurosci
Poslunsey MS, Wood MR, Han C, Stauffer SR, Panarese JD, Melancon BJ, Engers JL, Dickerson JW, Peng W, Noetzel MJ, Cho HP, Rodriguez AL, Hopkins CR, Morrison R, Crouch RD, Bridges TM, Blobaum AL, Boutaud O, Daniels JS, Kates MJ, Castelhano A, Rook JM, Niswender CM, Jones CK, Conn PJ, Lindsley CW.   +25 more
europepmc   +1 more source

Inhibition of kynurenine 3‐monooxygenase (KMO) reduces fentanyl and sucrose intake and relapse‐like behaviour in rats

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Opioid use disorder, particularly involving fentanyl, poses major challenges due to high relapse rates and limited effectiveness of pharmacotherapies. The kynurenine pathway has emerged as a target for addiction treatment through its modulation of glutamatergic and dopaminergic neurotransmission.
Carlos Núñez‐de la Calle, Lluna Careaga, Stefanie Malan‐Müller, Álvaro del Río‐García, Yaiza Trueba, Leticia Gil de Biedma‐Elduayen, Nuria Morales‐Puerto, Rebeca Vidal, Åsa Wiman, Sophie Erhardt, María Dolores Gutiérrez‐López, Esther O'Shea, María Isabel Colado   +12 more
wiley   +1 more source

ENX-101, a GABA_A receptor α2,3,5-selective positive allosteric modulator, displays antiseizure effects in rodent seizure and epilepsy models. [PDF]

Epilepsia
Serrats J, Vadodaria KC, Brubaker W, Barker-Haliski M, White HS, Evrard A, Roucard C, Taylor E, Vanover KE, Cunningham S, Sudarsan V, Rogawski MA.   +11 more
europepmc   +1 more source

Extracellular matrix and proteolysis: mechanisms driving irreversible changes and shaping cell behavior

The FEBS Journal, EarlyView.
Irreversible ECM proteolysis by remodeling enzymes shapes development, homeostasis, and disease. ECM‐degrading proteases display cell specificity and are governed by shared mechanisms, exhibiting functional redundancy in generating matrikines, growth factors, and cytokines.
Inna Solomonov, Orit Kollet, Irit Sagi
wiley   +1 more source

Preclinical pharmacology of alogabat: a novel GABA_A-α5 positive allosteric modulator targeting neurodevelopmental disorders with impaired GABA_A signaling. [PDF]

Front Pharmacol
Cecere G, Ballard TM, Knoflach F, Honer M, Hipp JF, Garces P, Mueggler T, Künnecke B, Bruns A, Prinssen EP, Schoenenberger P, Janz P, Redondo R, Biemans B, Knust H, Olivares-Morales A, Brigo A, Schulz JM, Bertrand D, Saxe M, O'Connor EC, Hernandez MC.   +21 more
europepmc   +1 more source

Curcumin Acts as a Positive Allosteric Modulator of α7-Nicotinic Acetylcholine Receptors and Reverses Nociception in Mouse Models of Inflammatory Pain

Journal of Pharmacology and Experimental Therapeutics, 2018
Eslam El Nebrisi, D. Bagdas, Wisam B. Toma, Halima Al Samri, Anna Brodzik, Yasmin Alkhlaif, K. Yang, F. Howarth, I. Damaj, M. Oz   +9 more
semanticscholar   +1 more source

Investigating transthyretin variants H88R and I107V in amyloid priming: From destabilization to complete dissociation

The FEBS Journal, EarlyView.
Investigated mutations in transthyretin (TTR) disrupt the F87‐centered hydrophobic core that stabilizes its tetrameric structure. The mild I107V mutation weakens inter‐chain packing, while H88R fully abolishes tetramer formation, yielding a monomeric, aggregation‐prone form. Structural, biophysical, and computational analyses reveal that both mutations
István L. Bódy, Zsolt Fazekas, Nóra Wágner, Anna J. Kiss‐Szemán, Veronika Harmat, Zoltán Pozsonyi, Dóra K. Menyhárd, András Perczel   +7 more
wiley   +1 more source

Proteolysis at the extracellular matrix interface: Molecular architects and regulators in health and disease

The FEBS Journal, EarlyView.
The extracellular matrix (ECM) is a dynamic scaffold that orchestrates tissue architecture and cellular communication. A critical but underexplored interplay between proteases and cluster of differentiation molecules (CD) governs ECM turnover and directs cell fate.
David Jurnečka, Matija Hrovatin, Bor Bokalj, Boris Turk   +3 more
wiley   +1 more source

PEG400 regulates Falcipain 2 activity through an allosteric mechanism

The FEBS Journal, EarlyView.
Falcipain‐2 can potentially be leveraged as a drug target due to its critical role as a haemoglobinase during the intra‐erythrocytic stage of Plasmodium falciparum. Here, we investigate the regulation of the proteolytic and haemoglobinase activity of falcipain‐2 in the presence of polyethylene glycol.
Bikram Nath, Subhoja Chakraborty, Sampa Biswas   +2 more
wiley   +1 more source