Publications by Somi Reddy Majjigapu

Anticancer Activities of Novel Nicotinamide Phosphoribosyltransferase Inhibitors in Hematological Malignancies

Pierre Vogel, Somi Reddy Majjigapu, Jianfei Bai

Targeting cancer cells that are highly dependent on the nicotinamide adenine dinucleotide (NAD+) metabolite is a promising therapeutic strategy. Nicotinamide phosphoribosyltransferase (NAMPT) is the rate-limiting enzyme catalyzing NAD(+) production. Despit ...

MDPI2023

Ein neuer NAMPT-Inhibitor JJ-08 vermindert Wachstum und Koloniebildung von Pankreaskarzinomzellen in Kombination mit NAPRT-Hemmung

Pierre Vogel, Somi Reddy Majjigapu

KARGER2022

Identification of new FK866 analogues with potent anticancer activity against pancreatic cancer

Pierre Vogel, Somi Reddy Majjigapu, Jianfei Bai

Pancreatic ductal adenocarcinoma (PDAC) is one of the most lethal diseases for which chemotherapy has not been very successful yet. FK866 ((E)-N-(4-(1-benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide) is a well-known NAMPT (nicotinamide phosphoribos ...

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER2022

Structure-based optimization of type III indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors

Pierre Vogel, Florence Pojer, Somi Reddy Majjigapu

The haem enzyme indoleamine 2,3-dioxygenase 1 (IDO1) catalyses the rate-limiting step in the kynurenine pathway of tryptophan metabolism and plays an essential role in immunity, neuronal function, and ageing. Expression of IDO1 in cancer cells results in t ...

TAYLOR & FRANCIS LTD2022

Azole-Based Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors

Pierre Vogel, Olivier Michielin, Florence Pojer, Somi Reddy Majjigapu, George Coukos

The heme enzyme indoleamine 2,3-dioxygenase 1 (IDO1) plays an essential role in immunity, neuronal function, and aging through catalysis of the rate-limiting step in the kynurenine pathway of tryptophan metabolism. Many IDO1 inhibitors with different chemo ...

AMER CHEMICAL SOC2021

Inhibition Mechanisms of Indoleamine 2,3-Dioxygenase 1 (IDO1)

Pierre Vogel, Florence Pojer, Somi Reddy Majjigapu

Indoleamine 2,3-dioxygenase 1 (IDO1) catalyzes the rate-limiting step in the kynurenine pathway of tryptophan metabolism, which is involved in immunity, neuronal function, and aging. Its implication in pathologies such as cancer and neurodegenerative disea ...

AMER CHEMICAL SOC2019

1,2,3-Triazoles as inhibitors of indoleamine 2,3-dioxygenase 2 (IDO2)

Pierre Vogel, Olivier Michielin, Somi Reddy Majjigapu, George Coukos

Indoleamine 2,3-dioxygenase 2 (IDO2) is a potential therapeutic target for the treatment of diseases that involve immune escape such as cancer. In contrast to IDO1, only a very limited number of inhibitors have been described for IDO2 due to inherent diffi ...

Pergamon-Elsevier Science Ltd2016

Challenges in the Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors

Pierre Vogel, Somi Reddy Majjigapu

Since the discovery of indoleamine 2,3-dioxygenase 1 (IDO1) as an attractive target for anticancer therapy in 2003, the search for inhibitors has been intensely pursued both in academia and in pharmaceutical companies. Many novel IDO1 inhibitor scaffolds h ...

Amer Chemical Soc2015

A critical role of autophagy in antileukemia/lymphoma effects of APO866, an inhibitor of NAD biosynthesis

Pierre Vogel, Bernard Sordat, Somi Reddy Majjigapu

APO866, an inhibitor of NAD biosynthesis, exhibits potent antitumor properties in various malignancies. Recently, it has been shown that APO866 induces apoptosis and autophagy in human hematological cancer cells, but the role of autophagy in APO866-induced ...

Landes Bioscience2014

The anti-lymphoma activity of APO866, an inhibitor of nicotinamide adenine dinucleotide biosynthesis, is potentialized when used in combination with anti-CD20 antibody

Pierre Vogel, Bernard Sordat, Somi Reddy Majjigapu

APO866 is an inhibitor of nicotinamide adenine dinucleotide (NAD) biosynthesis that exhibits potent anti-lymphoma activity. Rituximab (RTX), an anti-CD20 antibody, kills lymphoma cells by direct apoptosis and antibody- and complement-dependent cell-mediate ...

Informa Healthcare2014

Detailed analysis and follow-up studies of a high-throughput screening for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors

Gerardo Turcatti, Marc Chambon, Pierre Vogel, Olivier Michielin, Somi Reddy Majjigapu

Indoleamine 2,3-dioxygenase 1 (IDO1) is a key regulator of immune responses and therefore an important therapeutic target for the treatment of diseases that involve pathological immune escape, such as cancer. Here, we describe a robust and sensitive high-t ...

Elsevier France-Editions Scientifiques Medicales Elsevier2014

Synthesis of a C-Iminoribofuranoside Analog of the Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitor FK866

Pierre Vogel, Annabelle Gillig, Bernard Sordat, Somi Reddy Majjigapu

FK866 (also named APO866 or WK175) is a potent NAMPT inhibitor being evaluated (Phase II) as a potential anticancer drug. The preparation of the C-iminoribofuranoside analog (2E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-{3-[(2S,3S,4R,5R)-3,4-dihydroxy-5-(hyd ...

Wiley-VHCA AG2012

Rational Design of 4-Aryl-1,2,3-Triazoles for Indoleamine 2,3-Dioxygenase 1 Inhibition

Pierre Vogel, Olivier Michielin, Somi Reddy Majjigapu

Indoleamine 2,3-dioxygenase 1 (IDO1) is an important therapeutic target treatment of diseases such as cancer that involve pathological immune escape. Starting from the scaffold of our previously discovered IDO1 inhibitor 4-phenyl-1,2,3-triazole, we used co ...

2012