Jean-Christophe Harmange
Overview
Explore the profile of Jean-Christophe Harmange including associated specialties, affiliations and a list of published articles.
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Articles
41
Citations
940
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Recent Articles
1.
Westerling-Bui A, Fast E, Soare T, Venkatachalan S, DeRan M, Fanelli A, et al.
Sci Adv
. 2022 Jul;
8(27):eabj5633.
PMID: 35857479
Pharmacodynamic (PD) studies are an essential component of preclinical drug discovery. Current approaches for PD studies, including the analysis of novel kidney disease targeting therapeutic agents, are limited to animal...
2.
Daniels M, Malojcic G, Clugston S, Williams B, Coeffet-Le Gal M, Pan-Zhou X, et al.
J Med Chem
. 2022 Feb;
65(4):3575-3596.
PMID: 35143203
Autosomal dominant polycystic kidney disease (ADPKD) is the most prevalent monogenic human disease, but to date, only one therapy (tolvaptan) is approved to treat kidney cysts in ADPKD patients. Cyclin-dependent...
3.
Pedchenko V, Boudko S, Barber M, Mikhailova T, Saus J, Harmange J, et al.
J Biol Chem
. 2021 Mar;
296:100592.
PMID: 33775696
We identified a genetic variant, an 8-residue appendage, of the α345 hexamer of collagen IV present in patients with glomerular basement membrane diseases, Goodpasture's disease and Alport syndrome, and determined...
4.
Gehling V, McGrath J, Duplessis M, Khanna A, Brucelle F, Vaswani R, et al.
ACS Med Chem Lett
. 2020 Jun;
11(6):1213-1220.
PMID: 32551003
Leveraging the catalytic machinery of LSD1 (KDM1A), a series of covalent styrenylcyclopropane LSD1 inhibitors were identified. These inhibitors represent a new class of mechanism-based inhibitors that target and covalently label...
5.
Yu M, Ledeboer M, Daniels M, Malojcic G, Tibbitts T, Coeffet-Le Gal M, et al.
ACS Med Chem Lett
. 2019 Nov;
10(11):1579-1585.
PMID: 31749913
The nonselective Ca-permeable transient receptor potential (TRP) channels play important roles in diverse cellular processes, including actin remodeling and cell migration. TRP channel subfamily C, member 5 (TRPC5) helps regulate...
6.
Liang J, Labadie S, Zhang B, Ortwine D, Patel S, Vinogradova M, et al.
Bioorg Med Chem Lett
. 2017 May;
27(13):2974-2981.
PMID: 28512031
A high-throughput screening (HTS) of the Genentech/Roche library identified a novel, uncharged scaffold as a KDM5A inhibitor. Lacking insight into the binding mode, initial attempts to improve inhibitor potency failed...
7.
Vaswani R, Gehling V, Dakin L, Cook A, Nasveschuk C, Duplessis M, et al.
J Med Chem
. 2016 Oct;
59(21):9928-9941.
PMID: 27739677
Polycomb repressive complex 2 (PRC2) has been shown to play a major role in transcriptional silencing in part by installing methylation marks on lysine 27 of histone 3. Dysregulation of...
8.
Labadie S, Dragovich P, Cummings R, Deshmukh G, Gustafson A, Han N, et al.
Bioorg Med Chem Lett
. 2016 Aug;
26(18):4492-4496.
PMID: 27499454
Features from a high throughput screening (HTS) hit and a previously reported scaffold were combined to generate 1,7-naphthyridones as novel KDM5 enzyme inhibitors with nanomolar potencies. These molecules exhibited high...
9.
Gehling V, Bellon S, Harmange J, LeBlanc Y, Poy F, Odate S, et al.
Bioorg Med Chem Lett
. 2016 Aug;
26(17):4350-4.
PMID: 27476424
This communication describes the identification and optimization of a series of pan-KDM5 inhibitors derived from compound 1, a hit initially identified against KDM4C. Compound 1 was optimized to afford compound...
10.
Liang J, Zhang B, Labadie S, Ortwine D, Vinogradova M, Kiefer J, et al.
Bioorg Med Chem Lett
. 2016 Jul;
26(16):4036-41.
PMID: 27406798
Starting with a lead [1,5-a]pyrimidin-7(4H)-one-containing molecule (1), we generated potent, selective and orally bioavailable KDM5 inhibitors. Using structure- and property-based approaches, we designed 48 with improved cell potency (PC9 H3K4Me3...