Search Results - "Kamboj, Rajender"
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Discovery and pre-clinical characterization of a selective PI3Kδ inhibitor, LL-00071210 in rheumatoid arthritis
Published in European journal of pharmacology (15-07-2022)“…PI3Kδ plays a critical role in adaptive immune cell activation and function. Suppression of PI3Kδ has been shown to counter excessive triggering of immune…”
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LL-00066471, a novel positive allosteric modulator of α7 nicotinic acetylcholine receptor ameliorates cognitive and sensorimotor gating deficits in animal models: Discovery and preclinical characterization
Published in European journal of pharmacology (15-01-2021)“…α7 nicotinic acetylcholine receptor (α7 nAChR) is an extensively validated target for several neurological and psychiatric conditions namely, dementia and…”
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Discovery of benzylisothioureas as potent divalent metal transporter 1 (DMT1) inhibitors
Published in Bioorganic & medicinal chemistry letters (01-08-2012)“…Inhibition of intestinal brush border DMT1 offers a novel therapeutic approach to the prevention and treatment of disorders of iron overload. Several series of…”
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A hippocampal GluR5 kainate receptor regulating inhibitory synaptic transmission
Published in Nature (London) (09-10-1997)“…The principal excitatory neurotransmitter in the vertebrate central nervous system, L-glutamate, acts on three classes of ionotripic glutamate receptors, named…”
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Characterization of antiallodynic actions of ALE-0540, a novel nerve growth factor receptor antagonist, in the rat
Published in The Journal of pharmacology and experimental therapeutics (01-06-1999)“…There is growing evidence that nerve growth factor (NGF) may function as a mediator of persistent pain states. We have identified a novel nonpeptidic molecule,…”
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Activity of 2,3-benzodiazepines at native rat and recombinant human glutamate receptors in vitro : Stereospecificity and selectivity profiles
Published in Neuropharmacology (01-01-1996)“…The activity and selectivity of the glutamate receptor antagonists belonging to the 2,3-benzodiazepine class of compounds have been examined at recombinant…”
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Design and Synthesis of a Novel Series of 1,2-Disubstituted Cyclopentanes as Small, Potent Potentiators of 2-Amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propanoic Acid (AMPA) Receptors
Published in Journal of medicinal chemistry (09-05-2002)“…2-Amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propanoic acid (AMPA) potentiators are ligands that act as positive allosteric modulators at the AMPA receptors. We…”
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Prototypic G Protein-Coupled Receptor for the Intestinotrophic Factor Glucagon-Like Peptide 2
Published in Proceedings of the National Academy of Sciences - PNAS (16-02-1999)“…Glucagon-like peptide 2 (GLP-2) is a 33-aa proglucagon-derived peptide produced by intestinal enteroendocrine cells. GLP-2 stimulates intestinal growth and…”
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4-Alkyl- and 4-Cinnamylglutamic Acid Analogues Are Potent GluR5 Kainate Receptor Agonists
Published in Journal of medicinal chemistry (18-05-2000)“…Enantiomerically pure (2S,4R)-4-substituted glutamic acids were prepared and tested for homomeric GluR5 and GluR6 kainate subtype receptor affinity. Some of…”
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Discovery of LNP1892: A Precision Calcimimetic for the Treatment of Secondary Hyperparathyroidism
Published in Journal of medicinal chemistry (27-07-2023)“…The calcium sensing receptor (CaSR) plays an important role in maintaining calcium homeostasis. The use of calcimimetic cinacalcet has been established to…”
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4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists
Published in Bioorganic & medicinal chemistry letters (21-08-2000)“…Twenty-four 4-alkylidene glutamic acids were synthesised and tested as potential subtype selective GluR5 and 6 ligands. It was found that a critical size of…”
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A Deep Dive into the Conformational Dynamics of CYP3A4 : Understanding the Binding of Homotropic and Non‐homotropic Ligands for Mitigating Drug‐Drug interaction (DDI)
Published in ChemistrySelect (Weinheim) (06-05-2022)“…Cytochrome P450 (CYP) enzymes are well known for metabolism of drugs. The present study attempts to understand the homotropic cooperativity of CYP3A4 inhibitor…”
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Dual PI3Kδγ inhibition demonstrates potent anticancer effects in diffuse large B-cell lymphoma models: Discovery and preclinical characterization of LL-00084282
Published in Biochemical and biophysical research communications (31-12-2022)“…Phosphoinositide 3-kinase (PI3K) pathway mediates key signaling events downstream to B-cell receptor (BCR) for survival of mature B-cells, and overexpression…”
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Discovery and Characterization of Potent Pan-Genotypic HCV NS5A Inhibitors Containing Novel Tricyclic Central Core Leading to Clinical Candidate
Published in Journal of medicinal chemistry (12-12-2019)“…The identification of a novel class of potent pan-genotypic NS5A inhibitors with good pharmacokinetic profile suitable for potential use in treating HCV…”
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Discovery of Novel, Potent, Brain-Permeable, and Orally Efficacious Positive Allosteric Modulator of α7 Nicotinic Acetylcholine Receptor [4-(5-(4-Chlorophenyl)-4-methyl-2-propionylthiophen-3-yl)benzenesulfonamide]: Structure–Activity Relationship and Preclinical Characterization
Published in Journal of medicinal chemistry (13-02-2020)“…The discovery of a series of thiophenephenylsulfonamides as positive allosteric modulators (PAM) of α7 nicotinic acetylcholine receptor (α7 nAChR) is…”
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Discovery of a Potent and Selective PI3Kδ Inhibitor ( S )-2,4-Diamino-6-((1-(7-fluoro-1-(4-fluorophenyl)-4-oxo-3-phenyl-4 H -quinolizin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile with Improved Pharmacokinetic Profile and Superior Efficacy in Hematological Cancer Models
Published in Journal of medicinal chemistry (10-12-2020)“…PI3Kδ inhibitors have been approved for B-cell malignancies like CLL, small lymphocytic lymphoma, and so forth. However, currently available PI3Kδ inhibitors…”
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Differential RNA editing efficiency of AMPA receptor subunit GluR-2 in human brain
Published in Neuroreport (15-08-1994)“…RNA editing in rat brain has been found to control a determinant of cation flow in alpha-amino-3-hydroxy-5-methyl-4-isoxasolepropionic acid (AMPA)-gated…”
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Discovery of a Potent and Selective PI3Kδ Inhibitor (S)‑2,4-Diamino-6-((1-(7-fluoro-1-(4-fluorophenyl)-4-oxo-3-phenyl‑4H‑quinolizin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile with Improved Pharmacokinetic Profile and Superior Efficacy in Hematological Cancer Models
Published in Journal of medicinal chemistry (10-12-2020)“…PI3Kδ inhibitors have been approved for B-cell malignancies like CLL, small lymphocytic lymphoma, and so forth. However, currently available PI3Kδ inhibitors…”
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Discovery of a Novel Potent and Selective Calcium Release-Activated Calcium Channel Inhibitor: 2,6-Difluoro‑N‑(2′-methyl-3′-(4-methyl-5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)-[1,1′-biphenyl]-4-yl)benzamide. Structure–Activity Relationship and Preclinical Characterization
Published in Journal of medicinal chemistry (09-12-2021)“…The role of calcium release-activated calcium (CRAC) channels is well characterized and is of particular importance in T-cell function. CRAC channels are…”
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