Explanipedia

Development of long-acting formulations for hydrophobic Kifunensine analogues as potent inhibitors of type I mannosidase enzymes Open

Moustafa M. Abdelaziz, Chad E. Groer, Jack Weiner, Suresh E. Kurhade, Megan Craven , et al. · 2025

Sialidases derived from Gardnerella vaginalis and Prevotella timonensis remodel the sperm glycocalyx and impair sperm function Open

Sarah Dohadwala, Pooja Shah, Mark P. Farrell, Joseph A. Politch, Jai Marathe , et al. · 2025

Bacterial vaginosis (BV), a dysbiosis of the vaginal microbiome, affects approximately 30 percent of women worldwide (up to 50% in some regions) and is associated with several adverse health outcomes including preterm birth and increased i…

In This Issue, Volume 15, Issue 11 Open

Mark P. Farrell · 2024

Announcing the Early Career Board of ACS Medicinal Chemistry Letters Open

Aleksandra Baranczak, Simone V. Bigi-Botterill, Chiara Borsari, Amanda W. Dombrowski, Michelle A. Estrada , et al. · 2024

CD22L Conjugation to Insulin Attenuates Insulin-Specific B Cell Activation Open

Kyle D. Apley, Amber S. Griffith, Grant M. Downes, Patrick Ross, Mark P. Farrell , et al. · 2023

Pancreatic islet-reactive B lymphocytes promote Type 1 diabetes (T1D) by presenting an antigen to islet-destructive T cells. Teplizumab, an anti-CD3 monoclonal, delays T1D onset in patients at risk, but additional therapies are needed to p…

CD22L Conjugation to Insulin Attenuates Insulin-Specific B cell Activation Open

Kyle D. Apley, Amber S. Griffith, Grant M. Downes, Patrick Ross, Mark P. Farrell , et al. · 2023

Pancreatic islet-reactive B lymphocytes promote Type 1 diabetes (T1D) by presenting antigen to islet-destructive T cells. Teplizumab, an anti-CD3 monoclonal, delays T1D onset in patients at risk, but additional therapies are needed to prev…

Selective targeting of auto reactive B cells using bispecific molecules Open

Amber S. Griffith, Kyle D. Apley, Grant M. Downes, Patrick Ross, Brandon J. DeKosky , et al. · 2023

Type 1 diabetes occurs when autoreactive T cells attack insulin-producing cells in pancreatic islets. B cells promote disease by acting as essential antigen presenting cells. Targeted immune therapy for treatment and prevention of autoimmu…

Disrupting N-Glycosylation Using Type I Mannosidase Inhibitors Alters B-Cell Receptor Signaling Open

Aric Huang, Suresh E. Kurhade, Patrick Ross, Kyle D. Apley, J. Daniel Griffin , et al. · 2022

Kifunensine is a known inhibitor of type I α-mannosidase enzymes and has been shown to have therapeutic potential for a variety of diseases and application in the expression of high-mannose N-glycan bearing glycoproteins; however, the comp…

Lectin Drug Conjugates Targeting High Mannose N‐Glycans Open

Suresh E. Kurhade, Patrick Ross, Fei Gao, Mark P. Farrell · 2022

Cancer‐associated alterations to glycosylation have been shown to aid cancer development and progression. An increased abundance of high mannose N‐glycans has been observed in several cancers. Here, we describe the preparation of lectin dr…

Directing CAR NK Cells via the Metabolic Incorporation of CAR Ligands into Malignant Cell Glycans Open

Kathia Antillon, Patrick Ross, Mark P. Farrell · 2022

The abundance of sialic acid-containing glycans in the glycocalyx of malignant cells enables immune evasion. Here, we leverage the biosynthetic pathways that permit pervasive sialylation to incorporate a chimeric antigen receptor (CAR) lig…

The Road to Structurally Defined β‐Glucans Open

Patrick Ross, Mark P. Farrell · 2021

β‐glucans are polymers of glucose that have been isolated from a variety of organisms. Isolated β‐glucans have been used for medical purposes for centuries; however, efforts to define the biological activities of β‐glucans experimentally w…

Functionalized High Mannose‐Specific Lectins for the Discovery of Type I Mannosidase Inhibitors Open

Suresh E. Kurhade, Jack Weiner, Fei Gao, Mark P. Farrell · 2021

An engineered cyanovirin‐N homologue that exhibits specificity for high mannose N‐glycans has been constructed to aid type I α 1,2‐mannosidase inhibitor discovery and development. Engineering the lectins C‐terminus permitted facile functio…

Long-Acting BMS-378806 Analogues Stabilize the State-1 Conformation of the Human Immunodeficiency Virus Type 1 Envelope Glycoproteins Open

Shitao Zou, Shijian Zhang, Althea Gaffney, Haitao Ding, Maolin Lu , et al. · 2020

The envelope glycoprotein (Env) spike on the surface of human immunodeficiency virus type 1 (HIV-1) mediates the entry of the virus into host cells and is also the target for antibodies. During virus entry, Env needs to change shape. Env f…

Strain-Dependent Activation and Inhibition of Human Immunodeficiency Virus Entry by a Specific PF-68742 Stereoisomer Open

Connie Zhao, Amy M. Princiotto, Hanh T. Nguyen, Shitao Zou, Meiqing Zhao , et al. · 2019

Envelope glycoprotein (Env) spikes on the surface of human immunodeficiency virus (HIV-1) bind target cell receptors, triggering changes in the shape of Env. We studied a small molecule, MF275, that also induced shape changes in Env. The c…

The Glycogen Synthase Kinase-3β Inhibitor LSN 2105786 Promotes Zebrafish Fin Regeneration Open

Swapnalee Sarmah, Courtney Curtis, Jennifer Mahin, Mark P. Farrell, Thomas A. Engler , et al. · 2019

The Wnt pathway has been shown to regulate bone homeostasis and to influence some bone disease states. We utilized a zebrafish model system to study the effects of a synthetic, orally bioavailable glycogen synthase kinase-3β (GSK3β) inhibi…

540. Investigating the Mechanism of a Unique Human Immunodeficiency Virus-1 (HIV-1) Entry Inhibitor, MF275 Open

Connie Zhao, Amy M. Princiotto, Mark P. Farrell, Amos B. Smith, Navid Madani , et al. · 2018

BACKGROUND: HIV-1 entry into cells is mediated by sequential binding of target cell CD4 and CCR5 or CXCR4 to the metastable envelope (Env) trimer of gp120-gp41 heterodimers (Figure 1). We determined that MF275, a single diastereomer of the…

Publisher Correction: The β20–β21 of gp120 is a regulatory switch for HIV-1 Env conformational transitions Open

Alon Herschhorn, Christopher Gu, Francesca Moraca, Xiaochu Ma, Mark P. Farrell , et al. · 2018

The β20–β21 of gp120 is a regulatory switch for HIV-1 Env conformational transitions Open

Alon Herschhorn, Christopher Gu, Francesca Moraca, Xiaochu Ma, Mark P. Farrell , et al. · 2017

The entry of HIV-1 into target cells is mediated by the viral envelope glycoproteins (Env). Binding to the CD4 receptor triggers a cascade of conformational changes in distant domains that move Env from a functionally “closed” State 1 to m…

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