B
Bharat Lagu
Researcher at Astellas Pharma
Publications - 6
Citations - 117
Bharat Lagu is an academic researcher from Astellas Pharma. The author has contributed to research in topics: Gene & Ubiquitin ligase. The author has an hindex of 4, co-authored 6 publications receiving 81 citations. Previous affiliations of Bharat Lagu include Salk Institute for Biological Studies.
Papers
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Journal ArticleDOI
Novel highly selective inhibitors of ubiquitin specific protease 30 (USP30) accelerate mitophagy.
Arthur F. Kluge,Bharat Lagu,Pranab Maiti,Mahaboobi Jaleel,Michael Webb,Jyoti Malhotra,Ashley Mallat,P. Akhila Srinivas,James E. Thompson +8 more
TL;DR: The structure-activity relationships (SAR) within a novel series of highly selective USP30 inhibitors are disclosed and it is shown that MF-094 increases protein ubiquitination and accelerates mitophagy.
Journal ArticleDOI
Novel highly selective peroxisome proliferator-activated receptor δ (PPARδ) modulators with pharmacokinetic properties suitable for once-daily oral dosing.
Bharat Lagu,Arthur F. Kluge,Ross Fredenburg,Effie Tozzo,Ramesh S. Senaiar,Mahaboobi Jaleel,Sunil Kumar Panigrahi,Nirbhay Kumar Tiwari,Narasimha Rao Krishnamurthy,Taisuke Takahashi,Michael A. Patane +10 more
TL;DR: Optimization of benzamide PPARδ modulator 1 led to (E)-6-(2-((4-(furan-2-yl)-N-methylbenzamido)methyl)phenoxy)-4-methylhex-4-enoic acid, a potent selective PPAR Δ modulator with significantly improved exposure in multiple species following oral administration.
Journal ArticleDOI
Selective PPARδ Modulators Improve Mitochondrial Function: Potential Treatment for Duchenne Muscular Dystrophy (DMD)
Bharat Lagu,Arthur F. Kluge,Effie Tozzo,Ross Fredenburg,Eric L. Bell,Matthew M. Goddeeris,Peter Dwyer,Andrew Basinski,Ramesh S. Senaiar,Mahaboobi Jaleel,Nirbhay Kumar Tiwari,Sunil Kumar Panigrahi,Narasimha Rao Krishnamurthy,Taisuke Takahashi,Michael A. Patane +14 more
TL;DR: The X-ray structure of the previously reported PPARδ modulator 1 bound to the ligand binding domain (LBD) revealed that the amide moiety in 1 exists in the thermodynamically disfavored cis-amide orientation, which supports the therapeutic hypothesis for the study of MA-0204 in DMD patients.
Journal ArticleDOI
Highly selective peroxisome proliferator-activated receptor δ (PPARδ) modulator demonstrates improved safety profile compared to GW501516.
Bharat Lagu,Arthur F. Kluge,Matthew M. Goddeeris,Effie Tozzo,Ross Fredenburg,Shekar Chellur,Ramesh S. Senaiar,Mahaboobi Jaleel,D. Ravi Krishna Babu,Nirbhay Kumar Tiwari,Taisuke Takahashi,Michael A. Patane +11 more
TL;DR: Compound 1 regulates significantly fewer genes than the PPARδ modulator, GW501516, which suggests that 1 may be pharmacoequivalent to GW 501516 with fewer PPAR-related safety concerns.
Patent
PPAR agonists, compounds, pharmaceutical compositions, and methods of use thereof
Michael Downes,Ronald M. Evans,Arthur F. Kluge,Bharat Lagu,Masanori Miura,Sunil Kumar Panigrahi,Michael A. Patane,Susanta Samajdar,Ramesh Senaiar,Taisuke Takahashi +9 more
TL;DR: In this article, compounds of formula (I) useful for the treatment of PPAR-delta related diseases (e.g. mitochondrial diseases, muscular diseases, vascular diseases, demyelinating diseases and metabolic diseases) are presented.