Efficacy of the MCHR1 antagonist N-[3-(1-{[4-(3, 4-difluorophenoxy) phenyl] methyl}(4-piperidyl))-4-methylphenyl]-2-methylpropanamide (SNAP 94847) in mouse …

…, DA Craig, H Zhong, CJ Swanson, LG Hegde… - … of Pharmacology and …, 2007 - ASPET
Melanin-concentrating hormone (MCH) is a hypothalamic neuropeptide that plays a role in
the modulation of food intake and mood. In rodents, the actions of MCH are mediated via the …

Concomitant angiotensin AT1 receptor antagonism and neprilysin inhibition produces omapatrilat-like antihypertensive effects without promoting tracheal plasma …

LG Hegde, C Yu, T Renner, H Thibodeaux… - Journal of …, 2011 - journals.lww.com
Dual inhibition of angiotensin-converting enzyme (ACE) and neprilysin (NEP) by drugs such
as omapatrilat produces superior antihypertensive efficacy but cause high incidence of …

Structure-guided discovery of aminoquinazolines as brain-penetrant and selective LRRK2 inhibitors

…, S Neelamkavil, P Liu, J Su, LG Hegde… - Journal of medicinal …, 2021 - ACS Publications
The leucine-rich repeat kinase 2 (LRRK2) protein has been genetically and functionally
linked to Parkinson’s disease (PD), a disabling and progressive neurodegenerative disorder …

[PDF][PDF] Inhibition of RORγT skews TCRα gene rearrangement and limits T cell repertoire diversity

…, GA Baltus, K Barr, H Zhang, H Mehmet, LG Hegde… - Cell reports, 2016 - cell.com
Recent studies have elucidated the molecular mechanism of RORγT transcriptional regulation
of Th17 differentiation and function. RORγT was initially identified as a transcription factor …

Discovery of MK-1468: A Potent, Kinome-Selective, Brain-Penetrant Amidoisoquinoline LRRK2 Inhibitor for the Potential Treatment of Parkinson's Disease

…, D Xiao, J Piesvaux, S Lee, LG Hegde… - Journal of Medicinal …, 2023 - ACS Publications
Genetic mutation of the leucine-rich repeat kinase 2 (LRRK2) protein has been associated
with Parkinson’s disease (PD), a disabling and progressive neurodegenerative disorder that …

[HTML][HTML] Ileocolonic-targeted JAK inhibitor: a safer and more effective treatment for inflammatory bowel disease

…, L Dou, AW Basit, LY Moy, R Saklatvala, LG Hegde… - Pharmaceutics, 2022 - mdpi.com
Janus kinase (JAK) inhibitors, such as tofacitinib (Xeljanz) and filgotinib (Jyseleca), have
been approved for treatment of ulcerative colitis with several other JAK inhibitors in late-stage …

Discovery and Optimization of Potent, Selective, and Brain-Penetrant 1-Heteroaryl-1H-Indazole LRRK2 Kinase Inhibitors for the Treatment of Parkinson's Disease

…, CA Lesburg, P Liu, J Su, LG Hegde… - Journal of Medicinal …, 2022 - ACS Publications
Inhibition of leucine-rich repeat kinase 2 (LRRK2) kinase activity represents a genetically
supported, chemically tractable, and potentially disease-modifying mechanism to treat …

The novel neuropeptide Y Y5 receptor antagonist Lu AA33810 [N-[[trans-4-[(4, 5-dihydro [1] benzothiepino [5, 4-d] thiazol-2-yl) amino] cyclohexyl] methyl] …

…, H Zhong, X Huang, S Miller, LG Hegde… - … of Pharmacology and …, 2009 - ASPET
Neuropeptide Y (NPY) regulates physiological processes via receptor subtypes (Y 1 , Y 2 ,
Y 4 , Y 5 , and y 6 ). The Y 5 receptor is well known for its role in appetite. Based on …

Endothelin-receptor antagonists: current and future perspectives

A Ray, LG Hegde, A Chugh, JB Gupta - Drug discovery today, 2000 - Elsevier
Despite much effort over recent years to design and develop endothelin-receptor antagonists,
these compounds are far from becoming new drug entities. This article will review …

The effects of stressful stimuli and hypothalamic–pituitary–adrenal axis activation are reversed by the melanin-concentrating hormone 1 receptor antagonist SNAP …

DG Smith, LG Hegde, TD Wolinsky, S Miller… - Behavioural brain …, 2009 - Elsevier
Melanin-concentrating hormone (MCH) is an orexigenic and dipsogenic neuropeptide that
has been reported to mediate acute behavioral and neuroendocrine stress-related responses …