Results 41 to 50 of about 689,457 (314)

Thermostable neutral metalloprotease from Geobacillus sp. EA1 does not share thermolysin's preference for substrates with leucine at the P1′ position

FEBS Letters, EarlyView.
Knowing how proteases recognise preferred substrates facilitates matching proteases to applications. The S1′ pocket of protease EA1 directs cleavage to the N‐terminal side of hydrophobic residues, particularly leucine. The S1′ pocket of thermolysin differs from EA's at only one position (leucine in place of phenylalanine), which decreases cleavage ...
Grant R. Broomfield, Torsten Kleffmann, David J. Saul, Sigurd M. Wilbanks   +3 more
wiley   +1 more source

Vanillin enones as selective inhibitors of the cancer associated carbonic anhydrase isoforms IX and XII. The out of the active site pocket for the design of selective inhibitors?

Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
New C-glycosides and α,β-unsaturated ketones incorporating the 4-hydroxy-3-methoxyphenyl (vanillin) moiety as inhibitors of carbonic anhydrase (CA, EC 4.2.1.1) isoforms have been investigated.
Leonardo E. Riafrecha, Macarena S. Le Pors, Martín J. Lavecchia, Silvia Bua, Claudiu T. Supuran, Pedro A. Colinas   +5 more
doaj   +1 more source

Exploring lipid diversity and minimalism to define membrane requirements for synthetic cells

FEBS Letters, EarlyView.
Designing the lipid membrane of synthetic cells is a complex task, in which its various roles (among them solute transport, membrane protein support, and self‐replication) should all be integrated. In this review, we report the latest top‐down and bottom‐up advances and discuss compatibility and complexity issues of current engineering approaches ...
Sergiy Gan, Victoria Scarpelli, Marten Exterkate   +2 more
wiley   +1 more source

C‐mannosylation promotes ADAMTS1 activation and secretion in human testicular germ cell tumor NEC8 cells

FEBS Letters, EarlyView.
C‐mannosylation is a unique form of protein glycosylation. In this study, we demonstrated that ADAMTS1 is C‐mannosylated at Trp562 and Trp565 in human testicular germ cell tumor NEC8 cells. We found that C‐mannosylation of ADAMTS1 is essential for its secretion, processing, enzymatic activity, and ability to promote vasculogenic mimicry. These findings
Takato Kobayashi, Takehiro Suzuki, Ryota Kawahara, Natsumi Harai, Naoshi Dohmae, Siro Simizu   +5 more
wiley   +1 more source

The nicotinamide hypothesis revisited—plant defense signaling integrating PARP, nicotinamide, nicotinic acid, epigenetics, and glutathione

FEBS Letters, EarlyView.
Nicotinamide (NIC) and nicotinic acid (NIA) are proposed as stress signaling compounds in plants. Oxidative stress may lead to single strand breaks (SSB) in DNA, which activate poly(ADP‐ribose) polymerase (PARP). NIC and NIA are then formed from NAD. NIC and NIA can promote epigenetic changes leading to the expression of defense genes specific for the ...
Torkel Berglund, Anna B. Ohlsson
wiley   +1 more source

Angiotensin-converting enzyme inhibitors

Revista Cubana de Cardiología y Cirugía Cardiovascular, 2014
In an updated review concerning the angiotensin-converting enzyme inhibitors, an account of the historical development of this group of drugs proved as highly effective in the treatment of hypertension and of congestive heart failure is made.
David García Barreto, Alberto Toruncha Chuckram   +1 more
doaj  

Leishmania mexicana Trypanothione Reductase Inhibitors: Computational and Biological Studies

Molecules, 2019
Leishmanicidal drugs have many side effects, and drug resistance to all of them has been documented. Therefore, the development of new drugs and the identification of novel therapeutic targets are urgently needed.
Félix Matadamas-Martínez, Alicia Hernández-Campos, Alfredo Téllez-Valencia, Alejandra Vázquez-Raygoza, Sandra Comparán-Alarcón, Lilián Yépez-Mulia, Rafael Castillo   +6 more
doaj   +1 more source

Mechanistic basis for inhibition of the extended‐spectrum β‐lactamase GES‐1 by enmetazobactam and tazobactam

FEBS Letters, EarlyView.
Antimicrobial resistance (AMR) is of huge importance, resulting in over 1 million deaths each year. Here, we describe how a new drug, enmetazobactam, designed to help fight resistant bacterial diseases, inhibits a key enzyme (GES‐1) responsible for AMR. Our data show it is a more potent inhibitor than the related tazobactam, with high‐level computation
Michael Beer, Philip Hinchliffe, Marko Hanževački, Christopher R. Bethel, Catherine L. Tooke, Marc W. Van der Kamp, Krisztina M. Papp‐Wallace, Robert A. Bonomo, Stuart Shapiro, Adrian J. Mulholland, James Spencer   +10 more
wiley   +1 more source

From lactation to malignancy: A comparison between healthy and cancerous breast gland at single‐cell resolution reveals new issues for tumorigenesis

FEBS Letters, EarlyView.
Single‐cell RNA sequencing reveals an opposite role of SLPI in basal tumors based on metastatic spread, along with shared activation of specific regulons in cancer cells and mature luminal lactocytes, as well as downregulation of MALAT1 and NEAT1 in the latter.
Pietro Ancona, Carlo M. Bergamini, Carlo Ferrari, Stefano Volinia, Nicoletta Bianchi   +4 more
wiley   +1 more source

Cancer cell death induced by the NAD antimetabolite Vacor discloses the antitumor potential of SARM1

FEBS Letters, EarlyView.
Vacor, a compound converted into the toxic metabolite Vacor adenine dinucleotide (VAD) by the nicotinamide salvage pathway enzymes NAMPT and NMNAT2, exhibits antitumor activity by inducing rapid and complete NAD depletion. We report that Vacor toxicity is limited to cell lines expressing high levels of SARM1, a NAD glycohydrolase.
Giuseppe Ranieri, Andrea Lapucci, Giuseppe Orsomando, Nadia Raffaelli, Alberto Chiarugi, Daniela Buonvicino   +5 more
wiley   +1 more source