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Jayvardhan Pandit

Explore the profile of Jayvardhan Pandit including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 40
Citations 777
Followers 0
Related Specialties
Chemistry
Biochemistry
Molecular Biology
Top 10 Co-Authors
Dennis E Danley
Patrick R Verhoest
Christopher J Schmidt
Eric S Marr
Thomas A Chappie
John M Humphrey
Christopher J Helal
Christopher J ODonnell
Frank S Menniti
Kimberly F Fennell
Published In
J Med Chem
Bioorg Med Chem Lett
ACS Med Chem Lett
Proc Natl Acad Sci U S A
Structure
Affiliations
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Recent Articles
11.
A Novel Binding Mode Reveals Two Distinct Classes of NMDA Receptor GluN2B-selective Antagonists
Stroebel D, Buhl D, Knafels J, Chanda P, Green M, Sciabola S, et al.
Mol Pharmacol . 2016 Feb; 89(5):541-51. PMID: 26912815
N-methyl-d-aspartate receptors (NMDARs) are glutamate-gated ion channels that play key roles in brain physiology and pathology. Because numerous pathologic conditions involve NMDAR overactivation, subunit-selective antagonists hold strong therapeutic potential, although...
12.
The discovery and characterization of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor potentiator N-{(3S,4S)-4-[4-(5-cyano-2-thienyl)phenoxy]tetrahydrofuran-3-yl}propane-2-sulfonamide (PF-04958242)
Shaffer C, Patel N, Schwarz J, Scialis R, Wei Y, Hou X, et al.
J Med Chem . 2015 Apr; 58(10):4291-308. PMID: 25905800
A unique tetrahydrofuran ether class of highly potent α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor potentiators has been identified using rational and structure-based drug design. An acyclic lead compound, containing an ether-linked isopropylsulfonamide and...
13.
Utilizing structures of CYP2D6 and BACE1 complexes to reduce risk of drug-drug interactions with a novel series of centrally efficacious BACE1 inhibitors
Brodney M, Beck E, Butler C, Barreiro G, Johnson E, Riddell D, et al.
J Med Chem . 2015 Mar; 58(7):3223-52. PMID: 25781223
In recent years, the first generation of β-secretase (BACE1) inhibitors advanced into clinical development for the treatment of Alzheimer's disease (AD). However, the alignment of drug-like properties and selectivity remains...
14.
Engineered stabilization and structural analysis of the autoinhibited conformation of PDE4
Cedervall P, Aulabaugh A, Geoghegan K, McLellan T, Pandit J
Proc Natl Acad Sci U S A . 2015 Mar; 112(12):E1414-22. PMID: 25775568
Phosphodiesterase 4 (PDE4) is an essential contributor to intracellular signaling and an important drug target. The four members of this enzyme family (PDE4A to -D) are functional dimers in which...
15.
Discovery of cytotoxic dolastatin 10 analogues with N-terminal modifications
Maderna A, Doroski M, Subramanyam C, Porte A, Leverett C, Vetelino B, et al.
J Med Chem . 2014 Nov; 57(24):10527-43. PMID: 25431858
Auristatins, synthetic analogues of the antineoplastic natural product Dolastatin 10, are ultrapotent cytotoxic microtubule inhibitors that are clinically used as payloads in antibody-drug conjugates (ADCs). The design and synthesis of...
16.
Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions
Tuttle J, Anderson M, Bechle B, Campbell B, Chang C, Dounay A, et al.
ACS Med Chem Lett . 2014 Jun; 4(1):37-40. PMID: 24900560
A series of aryl hydroxamates recently have been disclosed as irreversible inhibitors of kynurenine amino transferase II (KAT II), an enzyme that may play a role in schizophrenia and other...
17.
Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia
Dounay A, Anderson M, Bechle B, Campbell B, Claffey M, Evdokimov A, et al.
ACS Med Chem Lett . 2014 Jun; 3(3):187-92. PMID: 24900455
Kynurenine aminotransferase (KAT) II has been identified as a potential new target for the treatment of cognitive impairment associated with schizophrenia and other psychiatric disorders. Following a high-throughput screen, cyclic...
18.
Discovery and characterization of a novel dihydroisoxazole class of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor potentiators
Patel N, Schwarz J, Hou X, Hoover D, Xie L, Fliri A, et al.
J Med Chem . 2013 Nov; 56(22):9180-91. PMID: 24215237
Positive allosteric modulators ("potentiators") of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors (AMPAR) enhance excitatory neurotransmission and may improve the cognitive deficits associated with various neurological disorders. The dihydroisoxazole (DHI) series of AMPAR...
19.
Discovery of potent selective bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model. Part II: optimization studies and demonstration of in vivo efficacy
Plummer M, Cornicelli J, Roark H, Skalitzky D, Stankovic C, Bove S, et al.
Bioorg Med Chem Lett . 2013 Apr; 23(11):3443-7. PMID: 23597790
Selective phosphodiesterase 2 (PDE2) inhibitors are shown to have efficacy in a rat model of osteoarthritis (OA) pain. We identified potent, selective PDE2 inhibitors by optimizing residual PDE2 activity in...
20.
Discovery of potent, selective, bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model, part I: transformation of selective pyrazolodiazepinone phosphodiesterase 4 (PDE4) inhibitors into selective PDE2 inhibitors
Plummer M, Cornicelli J, Roark H, Skalitzky D, Stankovic C, Bove S, et al.
Bioorg Med Chem Lett . 2013 Apr; 23(11):3438-42. PMID: 23582272
We identified potent, selective PDE2 inhibitors by optimizing residual PDE2 activity in a series of PDE4 inhibitors, while simultaneously minimizing PDE4 activity. These newly designed PDE2 inhibitors bind to the...