Search Results - "Mookhtiar, Kasim"
-
1
Recombinant irisin induces weight loss in high fat DIO mice through increase in energy consumption and thermogenesis
Published in Biochemical and biophysical research communications (05-11-2019)“…Irisin is known to be an important metabolic regulator of glucose and lipid metabolism. The aims of the present study are to assess the role of mouse Irisin in…”
Get full text
Journal Article -
2
Regulation of RIPK1 activation by TAK1-mediated phosphorylation dictates apoptosis and necroptosis
Published in Nature communications (25-08-2017)“…Stimulation of TNFR1 by TNFα can promote three distinct alternative mechanisms of cell death: necroptosis, RIPK1-independent and -dependent apoptosis. How…”
Get full text
Journal Article -
3
RIPK1 mediates axonal degeneration by promoting inflammation and necroptosis in ALS
Published in Science (American Association for the Advancement of Science) (05-08-2016)“…Mutations in the optineurin (OPTN) gene have been implicated in both familial and sporadic amyotrophic lateral sclerosis (ALS). However, the role of this…”
Get full text
Journal Article -
4
Design and synthesis of novel xanthine derivatives as potent and selective A2B adenosine receptor antagonists for the treatment of chronic inflammatory airway diseases
Published in European journal of medicinal chemistry (07-07-2017)“…Adenosine induces bronchial hyperresponsiveness and inflammation in asthmatics through activation of A2B adenosine receptor (A2BAdoR). Selective antagonists…”
Get full text
Journal Article -
5
Discovery and evaluation of novel FAAH inhibitors in neuropathic pain model
Published in Bioorganic & medicinal chemistry letters (15-01-2019)“…[Display omitted] •Novel scaffold as FAAH inhibitor with reversible mechanism of action.•Proof of MoA by recovery of active enzyme upon preincubation with…”
Get full text
Journal Article -
6
Discovery and pharmacological evaluation of indole derivatives as potent and selective RORγt inverse agonist for multiple autoimmune conditions
Published in Bioorganic & medicinal chemistry letters (15-08-2019)“…[Display omitted] •Identification of indole analogues as potent RORγt inverse agonists, SAR of around 44 compounds is presented.•Potent compounds were…”
Get full text
Journal Article -
7
Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A2A Receptor Antagonists and Their Biological Evaluation
Published in Journal of medicinal chemistry (26-01-2017)“…Our initial structure–activity relationship studies on 7-methoxy-4-morpholino-benzothiazole derivatives featured by aryloxy-2-methylpropanamide moieties at the…”
Get full text
Journal Article -
8
Modifications of flexible nonyl chain and nucleobase head group of (+)-erythro-9-(2′s-hydroxy-3′s-nonyl)adenine [(+)-EHNA] as adenosine deaminase inhibitors
Published in Bioorganic & medicinal chemistry (15-10-2017)“…[Display omitted] A series of terminal nonyl chain and nucleobase modified analogues of (+)-EHNA (III) were synthesized and evaluated for their ability to…”
Get full text
Journal Article -
9
Discovery of a potent and selective small molecule hGPR91 antagonist
Published in Bioorganic & medicinal chemistry letters (15-06-2011)“…GPR91, a 7TM G-Protein-Coupled Receptor, has been recently deorphanized with succinic acid as its endogenous ligand. Current literature indicates that GPR91…”
Get full text
Journal Article -
10
257 Combination of adenosine antagonists A2AR (TT-10) and A2BR (TT-4) with checkpoint inhibitors demonstrate anti-tumor activity in CT-26 murine colon tumor allograft model
Published in Journal for immunotherapy of cancer (01-11-2021)“…BackgroundTT-10 and TT-4 are potent and selective antagonists of adenosine A2A receptor (A2AR) and A2B receptor (A2BR) respectively. Both agents are being…”
Get full text
Journal Article -
11
Evaluation of separate role of intestine and liver in first pass metabolism of budesonide in rat
Published in Xenobiotica (02-12-2018)“…1. Budesonide, a potent topical corticosteroid, reported to have low oral bioavailability in mice, rat, dog and human due to rapid first pass metabolism…”
Get full text
Journal Article -
12
Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia
Published in European journal of medicinal chemistry (16-06-2017)“…Glucokinase activators (GKAs) are among the emerging drug candidates for the treatment of type 2 diabetes (T2D). Despite effective blood glucose lowering in…”
Get full text
Journal Article -
13
Discovery and evaluation of 1H-pyrrolo[2,3-b]pyridine based selective and reversible small molecule BTK inhibitors for the treatment of rheumatoid arthritis
Published in Bioorganic & medicinal chemistry letters (15-04-2017)“…Anti-arthritic effect of 11 and 13 in mouse CIA model. [Display omitted] In a pursuit to identify reversible and selective BTK inhibitors, two series based on…”
Get full text
Journal Article -
14
759 ADPORT-601 (TT-10–101): first-in-human study of adenosine 2A (A2A) and adenosine 2B (A2B) receptor antagonists in participants with selected advanced solid tumors
Published in Journal for immunotherapy of cancer (01-11-2023)“…BackgroundDespite significant advances in immunotherapy, novel approaches to promoting immune response and overcoming immunosuppressive pathways are needed…”
Get full text
Journal Article -
15
Pharmacological and X-Ray Structural Characterization of a Novel Selective Androgen Receptor Modulator: Potent Hyperanabolic Stimulation of Skeletal Muscle with Hypostimulation of Prostate in Rats
Published in Endocrinology (Philadelphia) (01-01-2007)“…A novel, highly potent, orally active, nonsteroidal tissue selective androgen receptor (AR) modulator (BMS-564929) has been identified, and this compound has…”
Get full text
Journal Article -
16
Design and synthesis of novel xanthine derivatives as potent and selective A 2B adenosine receptor antagonists for the treatment of chronic inflammatory airway diseases
Published in European journal of medicinal chemistry (07-07-2017)“…Adenosine induces bronchial hyperresponsiveness and inflammation in asthmatics through activation of A adenosine receptor (A AdoR). Selective antagonists have…”
Get full text
Journal Article -
17
Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A 1 receptor antagonists and their biological evaluation
Published in Bioorganic & medicinal chemistry (15-03-2017)“…Multipronged approach was used to synthesize a library of diverse C-8 cyclopentyl hypoxanthine analogs from a common intermediate III. Several potent and…”
Get full text
Journal Article -
18
Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A1 receptor antagonists and their biological evaluation
Published in Bioorganic & medicinal chemistry (15-03-2017)“…[Display omitted] Multipronged approach was used to synthesize a library of diverse C-8 cyclopentyl hypoxanthine analogs from a common intermediate III…”
Get full text
Journal Article -
19
Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A 2A Receptor Antagonists and Their Biological Evaluation
Published in Journal of medicinal chemistry (26-01-2017)“…Our initial structure-activity relationship studies on 7-methoxy-4-morpholino-benzothiazole derivatives featured by aryloxy-2-methylpropanamide moieties at the…”
Get full text
Journal Article -
20
A2B adenosine receptor antagonists: Design, synthesis and biological evaluation of novel xanthine derivatives
Published in European journal of medicinal chemistry (15-02-2017)“…A2BAdoR is a low affinity adenosine receptor that functions by Gs mediated elevation of cAMP and subsequent downstream signaling. The receptor has been…”
Get full text
Journal Article