Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase

Compound 12 Human/mouse NNMT enzymatic inhibition (IC50): 0.58/4.5 µM. Inhibition of MNA in U2OS/3T3L1 cell based assay: 0.3/2.1 µM. Human/mouse metabolic stability (% remaining after 30 m): 85/69. In vivo target engagement (MNA reduction, 2 h): ∼80%.

Gespeichert in:

Autor*in:	Ruf, Sven [verfasserIn] Hallur, Mahanandeesha Siddappa Anchan, Nisha K. Swamy, Indu N. Murugesan, Karthikai Raj Sarkar, Sayantani Narasimhulu, Lokesh Kananti Putta, V.P. Rama Kishore Shaik, Shama Chandrasekar, Devaraj Venkatapura Mane, Vishal Subhash Kadnur, Sanjay Venkatachalapathi Suresh, Juluri Bhamidipati, Ravi Kanth Singh, Manvi Burri, Raghunadha Reddy Kristam, Rajendra Schreuder, Herman Czech, Joerg Rudolph, Christine Marker, Alexander Langer, Thomas Mullangi, Ramesh Yura, Takeshi Gosu, Ramachandraiah Kannt, Aimo Dhakshinamoorthy, Saravanakumar Rajagopal, Sridharan

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2018

Schlagwörter:	Obesity Nicotinamide N-methyltransferase (NNMT) Methyl-nicotinamide (MNA) Ncotinamide Diabetes

Umfang:	4

Übergeordnetes Werk:	Enthalten in: Feeding European sea bass ( - Torrecillas, S. ELSEVIER, 2018, a Tetrahedron publication for rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines, Amsterdam [u.a.]
Übergeordnetes Werk:	volume:28 ; year:2018 ; number:5 ; day:1 ; month:03 ; pages:922-925 ; extent:4

Links:	Volltext

DOI / URN:	10.1016/j.bmcl.2018.01.058

Katalog-ID:	ELV042102197

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spelling	10.1016/j.bmcl.2018.01.058 doi GBV00000000000148A.pica (DE-627)ELV042102197 (ELSEVIER)S0960-894X(18)30069-6 DE-627 ger DE-627 rakwb eng 540 610 540 DE-600 610 DE-600 630 VZ 22 ssgn 46.00 bkl Ruf, Sven verfasserin aut Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase 2018 4 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Compound 12 Human/mouse NNMT enzymatic inhibition (IC50): 0.58/4.5 µM. Inhibition of MNA in U2OS/3T3L1 cell based assay: 0.3/2.1 µM. Human/mouse metabolic stability (% remaining after 30 m): 85/69. In vivo target engagement (MNA reduction, 2 h): ∼80%. Obesity Elsevier Nicotinamide N-methyltransferase (NNMT) Elsevier Methyl-nicotinamide (MNA) Elsevier Ncotinamide Elsevier Diabetes Elsevier Hallur, Mahanandeesha Siddappa oth Anchan, Nisha K. oth Swamy, Indu N. oth Murugesan, Karthikai Raj oth Sarkar, Sayantani oth Narasimhulu, Lokesh Kananti oth Putta, V.P. Rama Kishore oth Shaik, Shama oth Chandrasekar, Devaraj Venkatapura oth Mane, Vishal Subhash oth Kadnur, Sanjay Venkatachalapathi oth Suresh, Juluri oth Bhamidipati, Ravi Kanth oth Singh, Manvi oth Burri, Raghunadha Reddy oth Kristam, Rajendra oth Schreuder, Herman oth Czech, Joerg oth Rudolph, Christine oth Marker, Alexander oth Langer, Thomas oth Mullangi, Ramesh oth Yura, Takeshi oth Gosu, Ramachandraiah oth Kannt, Aimo oth Dhakshinamoorthy, Saravanakumar oth Rajagopal, Sridharan oth Enthalten in Elsevier Science Torrecillas, S. ELSEVIER Feeding European sea bass ( 2018 a Tetrahedron publication for rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines Amsterdam [u.a.] (DE-627)ELV000272361 volume:28 year:2018 number:5 day:1 month:03 pages:922-925 extent:4 https://doi.org/10.1016/j.bmcl.2018.01.058 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 46.00 Tiermedizin: Allgemeines VZ AR 28 2018 5 1 0301 922-925 4 045F 540
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language	English
source	Enthalten in Feeding European sea bass ( Amsterdam [u.a.] volume:28 year:2018 number:5 day:1 month:03 pages:922-925 extent:4
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bklname	Tiermedizin: Allgemeines
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topic_facet	Obesity Nicotinamide N-methyltransferase (NNMT) Methyl-nicotinamide (MNA) Ncotinamide Diabetes
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author	Ruf, Sven
spellingShingle	Ruf, Sven ddc 540 ddc 610 ddc 630 ssgn 22 bkl 46.00 Elsevier Obesity Elsevier Nicotinamide N-methyltransferase (NNMT) Elsevier Methyl-nicotinamide (MNA) Elsevier Ncotinamide Elsevier Diabetes Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase
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topic_title	540 610 540 DE-600 610 DE-600 630 VZ 22 ssgn 46.00 bkl Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase Obesity Elsevier Nicotinamide N-methyltransferase (NNMT) Elsevier Methyl-nicotinamide (MNA) Elsevier Ncotinamide Elsevier Diabetes Elsevier
topic	ddc 540 ddc 610 ddc 630 ssgn 22 bkl 46.00 Elsevier Obesity Elsevier Nicotinamide N-methyltransferase (NNMT) Elsevier Methyl-nicotinamide (MNA) Elsevier Ncotinamide Elsevier Diabetes
topic_unstemmed	ddc 540 ddc 610 ddc 630 ssgn 22 bkl 46.00 Elsevier Obesity Elsevier Nicotinamide N-methyltransferase (NNMT) Elsevier Methyl-nicotinamide (MNA) Elsevier Ncotinamide Elsevier Diabetes
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title	Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase
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title_full	Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase
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title_sort	novel nicotinamide analog as inhibitor of nicotinamide n-methyltransferase
title_auth	Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase
abstract	Compound 12 Human/mouse NNMT enzymatic inhibition (IC50): 0.58/4.5 µM. Inhibition of MNA in U2OS/3T3L1 cell based assay: 0.3/2.1 µM. Human/mouse metabolic stability (% remaining after 30 m): 85/69. In vivo target engagement (MNA reduction, 2 h): ∼80%.
abstractGer	Compound 12 Human/mouse NNMT enzymatic inhibition (IC50): 0.58/4.5 µM. Inhibition of MNA in U2OS/3T3L1 cell based assay: 0.3/2.1 µM. Human/mouse metabolic stability (% remaining after 30 m): 85/69. In vivo target engagement (MNA reduction, 2 h): ∼80%.
abstract_unstemmed	Compound 12 Human/mouse NNMT enzymatic inhibition (IC50): 0.58/4.5 µM. Inhibition of MNA in U2OS/3T3L1 cell based assay: 0.3/2.1 µM. Human/mouse metabolic stability (% remaining after 30 m): 85/69. In vivo target engagement (MNA reduction, 2 h): ∼80%.
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title_short	Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase
url	https://doi.org/10.1016/j.bmcl.2018.01.058
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author2	Hallur, Mahanandeesha Siddappa Anchan, Nisha K. Swamy, Indu N. Murugesan, Karthikai Raj Sarkar, Sayantani Narasimhulu, Lokesh Kananti Putta, V.P. Rama Kishore Shaik, Shama Chandrasekar, Devaraj Venkatapura Mane, Vishal Subhash Kadnur, Sanjay Venkatachalapathi Suresh, Juluri Bhamidipati, Ravi Kanth Singh, Manvi Burri, Raghunadha Reddy Kristam, Rajendra Schreuder, Herman Czech, Joerg Rudolph, Christine Marker, Alexander Langer, Thomas Mullangi, Ramesh Yura, Takeshi Gosu, Ramachandraiah Kannt, Aimo Dhakshinamoorthy, Saravanakumar Rajagopal, Sridharan
author2Str	Hallur, Mahanandeesha Siddappa Anchan, Nisha K. Swamy, Indu N. Murugesan, Karthikai Raj Sarkar, Sayantani Narasimhulu, Lokesh Kananti Putta, V.P. Rama Kishore Shaik, Shama Chandrasekar, Devaraj Venkatapura Mane, Vishal Subhash Kadnur, Sanjay Venkatachalapathi Suresh, Juluri Bhamidipati, Ravi Kanth Singh, Manvi Burri, Raghunadha Reddy Kristam, Rajendra Schreuder, Herman Czech, Joerg Rudolph, Christine Marker, Alexander Langer, Thomas Mullangi, Ramesh Yura, Takeshi Gosu, Ramachandraiah Kannt, Aimo Dhakshinamoorthy, Saravanakumar Rajagopal, Sridharan
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doi_str	10.1016/j.bmcl.2018.01.058
up_date	2024-07-06T21:54:39.083Z
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