Martin Augustin
Overview
Explore the profile of Martin Augustin including associated specialties, affiliations and a list of published articles.
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Articles
32
Citations
659
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0
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Recent Articles
1.
Baldwin E, van Eeuwen T, Hoyos D, Zalevsky A, Tchesnokov E, Sanchez R, et al.
Nature
. 2023 Dec;
626(7997):194-206.
PMID: 38096902
The LINE-1 (L1) retrotransposon is an ancient genetic parasite that has written around one-third of the human genome through a 'copy and paste' mechanism catalysed by its multifunctional enzyme, open...
2.
Gradler U, Schwarz D, Wegener A, Eichhorn T, Bandeiras T, Freitas M, et al.
J Biol Chem
. 2023 Oct;
299(11):105328.
PMID: 37806493
The receptor tyrosine kinase MET is activated by hepatocyte growth factor binding, followed by phosphorylation of the intracellular kinase domain (KD) mainly within the activation loop (A-loop) on Y1234 and...
3.
Guilinger J, Archna A, Augustin M, Bergmann A, Centrella P, Clark M, et al.
Bioorg Med Chem
. 2021 Jun;
42:116223.
PMID: 34091303
Libraries of DNA-Encoded small molecules created using combinatorial chemistry and synthetic oligonucleotides are being applied to drug discovery projects across the pharmaceutical industry. The majority of reported projects describe the...
4.
Methot J, Achab A, Christopher M, Zhou H, McGowan M, Trotter B, et al.
ACS Med Chem Lett
. 2020 Dec;
11(12):2461-2469.
PMID: 33335668
The 3,3-disubstituted oxindole moiety is a versatile and rigid three-dimensionally shaped scaffold. When engineered with a purine hinge-binding core, exceptionally selective PI3Kδ kinase inhibitors were discovered by exploiting small differences...
5.
Colarusso S, De Simone D, Frattarelli T, Andreini M, Cerretani M, Missineo A, et al.
Bioorg Med Chem
. 2020 Oct;
28(21):115738.
PMID: 33065433
Inhibition of KEAP1-NRF2 protein-protein interaction is considered a promising strategy to selectively and effectively activate NRF2, a transcription factor which is involved in several pathologies such as Huntington's disease (HD)....
6.
Ontoria J, Biancofiore I, Fezzardi P, Ferrigno F, Torrente E, Colarusso S, et al.
ACS Med Chem Lett
. 2020 May;
11(5):740-746.
PMID: 32435379
The NRF2-ARE pathway is an intrinsic mechanism of defense against oxidative stress. Inhibition of the interaction between NRF2 and its main negative regulator KEAP1 is an attractive strategy toward neuroprotective...
7.
White C, McGowan M, Zhou H, Sciammetta N, Fradera X, Lim J, et al.
ACS Med Chem Lett
. 2020 Apr;
11(4):550-557.
PMID: 32292563
Indoleamine-2,3-dioxygenase-1 (IDO1) has emerged as a target of significant interest to the field of cancer immunotherapy, as the upregulation of IDO1 in certain cancers has been linked to host immune...
8.
Kalliokoski T, Rummakko P, Rantanen M, Blaesse M, Augustin M, Ummenthala G, et al.
Bioorg Med Chem Lett
. 2020 Mar;
30(8):127060.
PMID: 32113843
Human kynurenine aminotransferase 2 (KAT2) inhibitors could be potentially used to treat the cognitive deficits associated with bipolar disease and schizophrenia. Although, there has been active drug research activity by...
9.
Ladi E, Everett C, Stivala C, Daniels B, Durk M, Harris S, et al.
J Med Chem
. 2019 Jul;
62(15):7032-7041.
PMID: 31283222
The pan-proteasome inhibitor bortezomib demonstrated clinical efficacy in off-label trials of Systemic Lupus Erythematosus. One potential mechanism of this clinical benefit is from the depletion of pathogenic immune cells (plasmablasts...
10.
Reuberson J, Horsley H, Franklin R, Ford D, Neuss J, Brookings D, et al.
J Med Chem
. 2018 Jun;
61(15):6705-6723.
PMID: 29952567
The primary target of a novel series of immunosuppressive 7-piperazin-1-ylthiazolo[5,4- d]pyrimidin-5-amines was identified as the lipid kinase, PI4KIIIβ. Evaluation of the series highlighted their poor solubility and unwanted off-target activities....