Robert T Gampe
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Explore the profile of Robert T Gampe including associated specialties, affiliations and a list of published articles.
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7
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Recent Articles
1.
Schulte C, Deaton D, Diaz E, Do Y, Gampe R, Guss J, et al.
Bioorg Med Chem Lett
. 2021 May;
47:128113.
PMID: 33991628
Through an internal virtual screen at GlaxoSmithKline a distinct class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors were discovered. Careful evaluation of crystal structures and SAR led to a novel, potent, and orally...
2.
Pearce K, Overton L, Gampe R, Barrett G, Taylor J, McKee D, et al.
Acta Crystallogr F Struct Biol Commun
. 2019 Apr;
75(Pt 4):239-245.
PMID: 30950824
Furin, also called proprotein convertase subtilisin/kexin 3 (PCSK3), is a calcium-dependent serine endoprotease that processes a wide variety of proproteins involved in cell function and homeostasis. Dysregulation of furin has...
3.
Axten J, Romeril S, Shu A, Ralph J, Medina J, Feng Y, et al.
ACS Med Chem Lett
. 2014 Jun;
4(10):964-8.
PMID: 24900593
We recently reported the discovery of GSK2606414 (1), a selective first in class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK), which inhibited PERK activation in cells and...
4.
Axten J, Medina J, Feng Y, Shu A, Romeril S, Grant S, et al.
J Med Chem
. 2012 Jul;
55(16):7193-207.
PMID: 22827572
Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states. Evidence that PERK is implicated in...
5.
Zuercher W, Buckholz R, Campobasso N, Collins J, Galardi C, Gampe R, et al.
J Med Chem
. 2010 Mar;
53(8):3412-6.
PMID: 20345102
Tertiary sulfonamides were identified in a HTS as dual liver X receptor (LXR, NR1H2, and NR1H3) ligands, and the binding affinity of the series was increased through iterative analogue synthesis....
6.
Hassell A, An G, Bledsoe R, Bynum J, Carter 3rd H, Deng S, et al.
Acta Crystallogr D Biol Crystallogr
. 2006 Dec;
63(Pt 1):72-9.
PMID: 17164529
Obtaining diffraction-quality crystals has long been a bottleneck in solving the three-dimensional structures of proteins. Often proteins may be stabilized when they are complexed with a substrate, nucleic acid, cofactor...
7.
Adkison K, Barrett D, Deaton D, Gampe R, Hassell A, Long S, et al.
Bioorg Med Chem Lett
. 2005 Nov;
16(4):978-83.
PMID: 16290936
Starting from potent aldehyde inhibitors with poor drug properties, derivatization to semicarbazones led to the identification of a series of semicarbazone-based cathepsin K inhibitors with greater solubility and better pharmacokinetic...