Thanigaimalai Pillaiyar

New insights into SREB orphan receptor roles in the ovary, using comparative transcriptomics across 3 fishes

Charles Heyder, Casey A. Murray, Philip K. E. Granith, Mukhriddin Makhkamov et autres

Superconserved receptors expressed in brain (SREB) are a family of orphan G protein-coupled receptors with 3 members in most vertebrates (GPR27 or SREB1, GPR85 or SREB2, and GPR173 or SREB3). They are associated with diverse physiological processes, ranging from glucose homeostasis to …

bg, fi, uz, us, de, be, ru (code pays fourni par la source)

Inhibitors Targeting SARS‐CoV‐2 Papain‐Like Protease: Screening, Design, Synthesis, and Biological Evaluation

Elena‐Oriana Iuga, Nilu Gone, Mariana Ortiz de Godoy, Gabriel Corrêa Veríssimo et autres

Despite the availability of vaccines and antiviral drugs, SARS‐CoV‐2 still presents a global health threat, emphasizing the need for new therapeutic targets beyond the main protease and RNA‐dependent RNA polymerase. The papain‐like protease (PL pro ) is a highly conserved and essential …

de, br, us, fi (code pays fourni par la source)

Discovery and characterization of quinoxaline and quinoline carboxamides as allosteric cannabinoid receptor modulators

Chunyang Bi, Andhika B. Mahardhika, Thanigaimalai Pillaiyar, Christa E. Müller

Cannabinoid (CB) receptors type 1 (CB 1 ) and type 2 (CB 2 ) are G i protein-coupled receptors that play important roles in brain function and immune regulation. While orthosteric CB 1 and CB 2 receptor agonists and antagonists have been …

de (code pays fourni par la source)

Adrenergic Ligands-Induced Transinhibition of EGFR by GPR27 and GPR173 Reveals a Novel GPCR Signaling Mechanism

Sorin Tunaru, Sorina Andreea Anghel, Rodica A. Badea, Cosmin Trif et autres

ro, de, be (code pays fourni par la source)

Azapeptide-Based SARS-CoV-2 Main Protease Inhibitors: Design, Synthesis, Enzyme Inhibition, Structural Determination, and Antiviral Activity

Philipp Flury, Jyoti Vishwakarma, Katharina Sylvester, Nobuyo Higashi‐Kuwata et autres

Abstract Mpro of SARS-CoV-2 plays a vital role in the replication and pathogenesis of virus. Additionally, its high conservation within the Coronaviridae family makes it an attractive therapeutic target for developing broad-spectrum agents. This study describes the design, synthesis, and structure−activity relationships …

de, us, jp, sk, br, fr, cn (code pays fourni par la source)

Azapeptide-based SARS-CoV-2 Main Protease Inhibitors: Design, Synthesis, Enzyme Inhibition, Structural Determination, and Antiviral Activity

Philipp Flury, Jyoti Vishwakarma, Katharina Sylvester, Nobuyo Higashi‐Kuwata et autres

The main protease (Mpro) of SARS-CoV-2 plays a crucial role in the replication and pathogenesis of the virus. The relatively high conservation within the Coronaviridae family makes it an attractive therapeutic target for developing broad-spectrum agents to prevent and control SARS-CoV-2 and …

de, us, jp, br, cn (code pays fourni par la source)

Allosteric modulation of the succinate receptor: A potential approach to attenuate renal ischemia/reperfusion injury

Rokaya Zahar, Parthiban Marimuthu, Philip Granith, Thanigaimalai Pillaiyar et autres

peer reviewed

be (code pays fourni par la source)

An overview of progress in human metapneumovirus (hMPV) research: Structure, function, and therapeutic opportunities

Nadine Krüger, Stefan Laufer, Thanigaimalai Pillaiyar

• Human metapneumovirus (hMPV) is a respiratory virus that causes severe infections in infants, children, and the elderly. • We examine the virus’s structure and replication and highlight prophylaxis and treatment for hMPV infections. • hMPV entry/fusion/release inhibitors, hMPV RNA polymerase inhibitors, …

de (code pays fourni par la source)

A patent review of CXCR7 modulators (2019-present)

Thanigaimalai Pillaiyar, Stefan Laufer

INTRODUCTION: Atypical chemokine receptor 3 (ACKR3) (formerly CXCR7) regulates various biological processes through its ligands and is closely associated with numerous diseases, including inflammation, cancer, cardiovascular diseases (CVDs), pain, and neurological disorders. Therefore, ACKR3 has emerged as a potential target for disease …

de (code pays fourni par la source)

Succinate receptor 1 signaling mutually depends on subcellular localization and cellular metabolism

Aenne‐Dorothea Liebing, Philipp Rabe, Petra Krumbholz, Christian Zieschang et autres

Succinate is a pivotal tricarboxylic acid cycle metabolite but also specifically activates the G i ‐ and G q ‐coupled succinate receptor 1 (SUCNR1). Contradictory roles of succinate and succinate‐SUCNR1 signaling include reports about its anti‐ or pro‐inflammatory effects. The link between …

de, us (code pays fourni par la source)

Design, Synthesis, and Unprecedented Interactions of Covalent Dipeptide-Based Inhibitors of SARS-CoV-2 Main Protease and Its Variants Displaying Potent Antiviral Activity

Philipp Flury, Nadine Krüger, Katharina Sylvester, Julian Breidenbach et autres

The main protease (M pro ) of SARS-CoV-2 is a key drug target for the development of antiviral therapeutics. Here, we designed and synthesized a series of small-molecule peptidomimetics with various cysteine-reactive electrophiles. Several compounds were identified as potent SARS-CoV-2 M pro …

de, cn, br, us, fr, gb, fi (code pays fourni par la source)

Pyrazinyl-Substituted Aminoazoles as Covalent Inhibitors of Thrombin: Synthesis, Structure, and Anticoagulant Properties

Lukas Imberg, Alena I. Siutkina, Catharina Erbacher, Judith Schmidt et autres

This study presents a novel series of N -acylated 1,2,4-triazol-5-amines and 1 H -pyrazol-5-amines, featuring a pyrazin-2-yl moiety, developed as covalent inhibitors of thrombin. These compounds demonstrated potent inhibitory activity, with derivatives 13a and 13b achieving IC 50 values as low as …

de, ru, br, us, fi (code pays fourni par la source)