Results 141 to 150 of about 103,093 (251)

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

Deep learning applications in protein crystallography. [PDF]

Acta Crystallogr A Found Adv
Matinyan S, Filipcik P, Abrahams JP.
europepmc   +1 more source

Novel drugs approved by the EMA, the FDA and the MHRA in 2025: A year in review

British Journal of Pharmacology, EarlyView.
Abstract In the 2025 novel drug mini‐review, one can take a full measure of the ingenuity that underlies current drug design and development, despite the year's smaller harvest (46 novel drugs) compared to 2024 (53) and 2023 (70). 54% of the novel drugs are first‐in‐class (FIC).
Andreas Papapetropoulos, Stavros Topouzis, Steve P. H. Alexander, Miriam M. Cortese‐Krott, Zsuzsanna Helyes, Kirill Martemyanov, Claudio Mauro, Nithyanandan Nagercoil, Reynold A. Panettieri Jr, Hemal H. Patel, Rainer Schulz, Barbara Stefanska, Gary J. Stephens, Nathalie Vergnolle, Xin Wang, Stephen Ward, Péter Ferdinandy   +16 more
wiley   +1 more source

Scalable fabrication of an array-type fixed-target device for automated room temperature X-ray protein crystallography. [PDF]

Sci Rep
Saha S, Chen Y, Russi S, Marchany-Rivera D, Cohen A, Perry SL.   +5 more
europepmc   +1 more source

Teleost‐specific ictacalcins exhibit similar structural organization, cation‐dependent activation, and transcriptional regulation as human S100 proteins

The FEBS Journal, EarlyView.
Calcium‐binding S100 proteins are important mediators of inflammation in humans. Distant members of this family have been recently discovered in teleost fish but their resemblance to human proteins has not been explored yet. This study demonstrates that zebrafish‐specific S100i1 and S100i2 (ictacalcins) possess identical structural organization and ...
Liz Hernández, Théo Paris, Maria Demou, Catherine Birck, Christina Begon‐Pescia, Juan Francisco Rodríguez Vidal, Sylwia D. Tyrkalska, Charlotte Bureau, Catherine Gonzalez, Juliette Gracia, Etienne Lelièvre, Victoriano Mulero, Mai Nguyen‐Chi, Laure Yatime   +13 more
wiley   +1 more source

The current status and future prospects of the Synchrotron Radiation Protein Crystallography Core Facility at NSRRC: a focus on the TPS 05A, TPS 07A and TLS 15A1 beamlines. [PDF]

J Synchrotron Radiat
Chou CK, Tseng CC, Chiang CH, Chen YH, Liu YC, Huang CY, Chao CH, Huang CH.   +7 more
europepmc   +1 more source

Anemia‐associated mutations disrupt the CDIN1‐Codanin1 complex in inherited congenital dyserythropoietic anemia I (CDA‐I) disease

The FEBS Journal, EarlyView.
Congenital dyserythropoietic anemia type I (CDA‐I) arises from mutations in Codanin1 and CDIN1. Using quantitative biophysical approaches, we show that disease‐associated mutations disrupt the CDIN1‐Codanin1 complex. Our findings provide critical insights into the molecular mechanism that links protein dysfunction to disturbing chromatin arrangement ...
Martin Stojaspal, Tomas Brom, Ivona Nečasová, Tomáš Janovič, Pavel Veverka, Naina Verma, Lukáš Uhrík, Lenka Hernychova, Ctirad Hofr   +8 more
wiley   +1 more source

The XFEL Protein Crystallography: Developments and Perspectives. [PDF]

Int J Mol Sci, 2019
Liu H, Lee W.
europepmc   +1 more source

Kinetic and structural characterisation of domain‐specific angiotensin I‐converting enzyme inhibition by captopril, rentiapril and zofenoprilat

The FEBS Journal, EarlyView.
Angiotensin I‐converting enzyme (ACE) contains two catalytic domains (nACE and cACE) and is a key therapeutic target for hypertension and cardiovascular disease. Current ACE inhibitors (ACEi) nonselectively inhibit both domains, causing adverse effects. Selective inhibition requires an understanding of domain‐specific binding.
Kyle S. Gregory, Vinasha Ramasamy, Edward D. Sturrock, K. Ravi Acharya   +3 more
wiley   +1 more source

A brief history of protein crystallography in Brazil. [PDF]

Biophys Rev, 2019
Garratt RC.
europepmc   +1 more source