Search Results - "Samant, Manoj"
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Novel exenatide analogs with peptidic albumin binding domains: potent anti-diabetic agents with extended duration of action
Published in PloS one (04-02-2014)“…The design, synthesis and pharmacology of novel long-acting exenatide analogs for the treatment of metabolic diseases are described. These molecules display…”
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2
Novel Analogues of Degarelix Incorporating Hydroxy-, Methoxy-, and Pegylated-Urea Moieties at Positions 3, 5, 6 and the N-Terminus. Part III
Published in Journal of medicinal chemistry (15-06-2006)“…Novel degarelix (Fe200486) analogues were screened for antagonism of GnRH-induced response (IC50) in a reporter gene assay. Inhibition of luteinizing hormone…”
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3
Norcystine, a New Tool for the Study of the Structure−Activity Relationship of Peptides
Published in Organic letters (25-05-2006)“…Norcysteine (Ncy) is an unnatural amino acid possessing an electronegative sulfur atom directly attached to the α-carbon atom. We describe the synthesis of…”
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Structure−Activity Relationship Studies of Gonadotropin-Releasing Hormone Antagonists Containing S-Aryl/Alkyl Norcysteines and Their Oxidized Derivatives
Published in Journal of medicinal chemistry (03-05-2007)“…A series of acyline analogues incorporating l- and d-isomers of S-arylated/alkylated norcysteines [Ncy(R), where R is 2-naphthyl, methyl, and isopropyl] at…”
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Synthesis of protected norcysteines for SPPS compatible with Fmoc strategy
Published in Tetrahedron letters (16-07-2007)“…We report the synthesis of racemic Alloc-Ncy(Tmob)–OH, the resolution of its methyl ester and demonstrate its application to form a norcystine bridge in…”
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Iterative Approach to the Discovery of Novel Degarelix Analogues: Substitutions at Positions 3, 7, and 8. Part II
Published in Journal of medicinal chemistry (28-07-2005)“…Degarelix (FE200486, Ac-d-2Nal-d-4Cpa-d-3Pal-Ser-4Aph(l-Hor)-d-4Aph(Cbm)-Leu-ILys-Pro-d-Ala-NH2) is a potent and very long acting antagonist of…”
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Novel gonadotropin-releasing hormone antagonists with substitutions at position 5
Published in Biopolymers (2005)“…Gonadotropin‐releasing hormone (GnRH) antagonists with high potency and improved duration of action are needed for potential clinical applications. We…”
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Synthesis, in vivo and in vitro biological activity of novel azaline B analogs
Published in Bioorganic & medicinal chemistry letters (02-06-2005)“…[Display omitted] Several azaline B analogs ( 2– 10) were synthesized and evaluated for their ability to antagonize GnRH in vitro and for duration of action in…”
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Self-Assembling, Cystine-Derived, Fused Nanotubes Based on Spirane Architecture: Design, Synthesis, and Crystal Structure of Cystinospiranes
Published in Journal of the American Chemical Society (20-06-2001)“…A novel family of cystine-based spirobicyclic peptides (cystinospiranes) has been synthesized by a single-step procedure involving condensation of…”
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Efficacy and safety of mavrilimumab in giant cell arteritis: a phase 2, randomised, double-blind, placebo-controlled trial
Published in Annals of the rheumatic diseases (01-05-2022)“…Granulocyte-macrophage colony-stimulating factor (GM-CSF) is implicated in pathogenesis of giant cell arteritis. We evaluated the efficacy of the GM-CSF…”
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Design, synthesis and membrane ion transport properties of cystine- and serine-based cyclo -4-oxa-heptane-1,7-bisamides
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Abstract 12057: Absence of Pericarditis Recurrence in Rilonacept-Treated Patients With COVID-19 and mRNA Vaccinations: Experience From Phase 3 Rhapsody Long-Term Extension
Published in Circulation (New York, N.Y.) (08-11-2022)“…IntroductionRare cardiac complications of COVID-19 and COVID-19 mRNA vaccination include pericarditis and myocarditis. Patients with recurrent pericarditis may…”
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Abstract 11653: Prolonged Rilonacept Treatment in Rhapsody Long-Term Extension Provided Persistent Reduction of Pericarditis Recurrence Risk
Published in Circulation (New York, N.Y.) (08-11-2022)“…IntroductionRilonacept reduced pericarditis recurrence in the phase 3 trial RHAPSODY. The long-term extension (LTE) enabled further insights into efficacy,…”
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14
NOAA National Water Level Observation Network Recapitalization
Published in OCEANS 2022, Hampton Roads (17-10-2022)“…This paper describes the recently developed plan to systematically recapitalize the entire National Oceanic and Atmospheric Administration (NOAA) National…”
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Conference Proceeding -
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Pseudoprogression (PsP) in Patients with Peripheral T-Cell Lymphoma (PTCL) Treated with the Novel Stapled Peptide ALRN-6924, a Dual Inhibitor of MDMX and MDM2
Published in Blood (29-11-2018)“…Background: ALRN-6924, an α-helical stapled p53 peptide, is the first-in-class and only dual inhibitor of MDMX and MDM2 currently in clinical trials for both,…”
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Characterization of Multisubstituted Corticotropin Releasing Factor (CRF) Peptide Antagonists (Astressins)
Published in Journal of medicinal chemistry (11-02-2016)“…CRF mediates numerous stress-related endocrine, autonomic, metabolic, and behavioral responses. We present the synthesis and chemical and biological properties…”
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Abstract CT109: First-in-class first-in-human phase 1 trial and translational study of the mono(ADP-ribose) polymerase-7 (PARP7) inhibitor RBN-2397 in patients with selected advanced solid tumors
Published in Cancer research (Chicago, Ill.) (14-04-2023)“…Abstract Background: PARP7 is a stress-induced monoART that suppresses the cellular type I interferon (IFN) response following cytosolic nucleic acid sensing…”
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Ring Size of Somatostatin Analogues (ODT-8) Modulates Receptor Selectivity and Binding Affinity
Published in Journal of medicinal chemistry (08-05-2008)“…The synthesis, biological testing, and NMR studies of several analogues of H-c[Cys3-Phe6-Phe7-DTrp8-Lys9-Thr10-Phe11-Cys14]-OH (ODT-8, a pan-somatostatin…”
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Ring Size in Octreotide Amide Modulates Differently Agonist versus Antagonist Binding Affinity and Selectivity
Published in Journal of medicinal chemistry (08-05-2008)“…H-DPhe2-c[Cys3-Phe7-DTrp8-Lys9-Thr10-Cys14]-Thr15-NH2 (1) (a somatostatin agonist, SRIF numbering) and H-Cpa2-c[DCys3-Tyr7-DTrp8-Lys9-Thr10-Cys14]-Nal15-NH2…”
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Novel Exenatide Analogs with Peptidic Albumin Binding Domains: Potent Anti-Diabetic Agents with Extended Duration of Action: e87704
Published in PloS one (01-02-2014)“…The design, synthesis and pharmacology of novel long-acting exenatide analogs for the treatment of metabolic diseases are described. These molecules display…”
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Journal Article