Search Results - "Alhamadsheh, Mamoun M."

Enhancing the Safety and Efficacy of PSMA-Based Small-Molecule Drug Conjugates by Linker Stabilization and Conjugation to Transthyretin Binding Ligand by Amin, Toufiq Ul, Emara, Rasha, Pal, Arindom, Aldawod, Hala, Jiang, Guanming, Liang, Dengpan, Haque Tuhin, Md Tariqul, Balgoname, Abdulmalek, Patel, Arjun D., Alhamadsheh, Mamoun M.

“…This work describes the enhancement of a novel antitumor therapeutic platform that combines advantages from small-molecule drug conjugates (SMDCs) and antibody…”
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A biomimetic approach for enhancing the in vivo half-life of peptides by Penchala, Sravan C, Miller, Mark R, Pal, Arindom, Dong, Jin, Madadi, Nikhil R, Xie, Jinghang, Joo, Hyun, Tsai, Jerry, Batoon, Patrick, Samoshin, Vyacheslav, Franz, Andreas, Cox, Trever, Miles, Jesse, Chan, William K, Park, Miki S, Alhamadsheh, Mamoun M

“…Linking a peptide with a small-molecule ligand for the serum protein transthyretin ensures half-life extension without diminishing potency through protection…”
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AG10 inhibits amyloidogenesis and cellular toxicity of the familial amyloid cardiomyopathy-associated V122I transthyretin by Penchala, Sravan C., Connelly, Stephen, Wang, Yu, Park, Miki S., Zhao, Lei, Baranczak, Aleksandra, Rappley, Irit, Vogel, Hannes, Liedtke, Michaela, Witteles, Ronald M., Powers, Evan T., Reixach, Natàlia, Chan, William K., Wilson, Ian A., Kelly, Jeffery W., Graef, Isabella A., Alhamadsheh, Mamoun M.

“…The misassembly of soluble proteins into toxic aggregates, including amyloid fibrils, underlies a large number of human degenerative diseases. Cardiac…”
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Peripherally restricted transthyretin-based delivery system for probes and therapeutics avoiding opioid-related side effects by Tuhin, Md Tariqul Haque, Liang, Dengpan, Liu, Fang, Aldawod, Hala, Amin, Toufiq Ul, Ho, Joshua S., Emara, Rasha, Patel, Arjun D., Felmlee, Melanie A., Park, Miki S., Uchizono, James A., Alhamadsheh, Mamoun M.

“…Several investigations into the sites of action of opioid analgesics have utilized peripherally acting mu-opioid receptor antagonists (PAMORAs), which have…”
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Biosynthesis of the salinosporamide A polyketide synthase substrate chloroethylmalonyl-coenzyme A from S-adenosyl-L-methionine by Eustáquio, Alessandra S, McGlinchey, Ryan P, Liu, Yuan, Hazzard, Christopher, Beer, Laura L, Florova, Galina, Alhamadsheh, Mamoun M, Lechner, Anna, Kale, Andrew J, Kobayashi, Yoshihisa, Reynolds, Kevin A, Moore, Bradley S

“…Polyketides are among the major classes of bioactive natural products used to treat microbial infections, cancer, and other diseases. Here we describe a…”
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Modular Polyketide Synthases and cis Double Bond Formation:  Establishment of Activated cis-3-Cyclohexylpropenoic Acid as the Diketide Intermediate in Phoslactomycin Biosynthesis by Alhamadsheh, Mamoun M, Palaniappan, Nadaraj, DasChouduri, Suparna, Reynolds, Kevin A

“…The majority of modular polyketide synthase (PKS) systems which generate unsaturated products do so with trans double bonds. Phoslactomycin B (PLM B) presents…”
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Enhancing the Pharmacokinetic Profile of Interleukin 2 through Site-Specific Conjugation to a Selective Small-Molecule Transthyretin Ligand by Liu, Fang, Ul Amin, Toufiq, Liang, Dengpan, Park, Miki S, Alhamadsheh, Mamoun M

“…Protein drugs hold great promise as therapeutics for a wide range of diseases. Unfortunately, one of the greatest challenges to be addressed during clinical…”
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Total Synthesis and Selective Activity of a New Class of Conformationally Restrained Epothilones by Alhamadsheh, Mamoun M., Gupta, Shuchi, Hudson, Richard A., Perera, Lalith, Tillekeratne, L. M. Viranga

“…Stereoselective total syntheses of two novel conformationally restrained epothilone analogues are described. Evans asymmetric alkylation, Brown allylation, and…”
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Hydrophilic Small Molecules That Harness Transthyretin To Enhance the Safety and Efficacy of Targeted Chemotherapeutic Agents by Pal, Arindom, Albusairi, Wabel, Liu, Fang, Tuhin, Md Tariqul Haque, Miller, Mark, Liang, Dengpan, Joo, Hyun, Amin, Toufiq Ul, Wilson, Elizabeth A, Faridi, Jesika S, Park, Miki, Alhamadsheh, Mamoun M

“…The hydrophobicity of many chemotherapeutic agents usually results in their nonselective passive distribution into healthy cells and organs causing collateral…”
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cis-Delta(2,3)-double bond of phoslactomycins is generated by a post-PKS tailoring enzyme by Palaniappan, Nadaraj, Alhamadsheh, Mamoun M, Reynolds, Kevin A

“…The antifungal phoslactomycins (PLM A-F), produced by Streptomyces sp. HK803, are structurally unusual in that three of their four double bonds are in the cis…”
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Potent kinetic stabilizers that prevent transthyretin-mediated cardiomyocyte proteotoxicity by Alhamadsheh, Mamoun M, Connelly, Stephen, Cho, Ahryon, Reixach, Natàlia, Powers, Evan T, Pan, Dorothy W, Wilson, Ian A, Kelly, Jeffery W, Graef, Isabella A

“…A valine-to-isoleucine mutation at position 122 of the serum protein transthyretin (TTR), found in 3 to 4% of African Americans, alters its stability, leading…”
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Synthesis and biological evaluation of novel sulfonyl-naphthalene-1,4-diols as FabH inhibitors by Alhamadsheh, Mamoun M., Waters, Norman C., Sachdeva, Sarbjot, Lee, Patricia, Reynolds, Kevin A.

“…A series of analogs of 2-tosylnaphthalene-1,4-diol were prepared and were found to be potent 10–20 nM reversible inhibitors of the Escherichia coli FabH…”
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Synthesis and biological evaluation of thiazolidine-2-one 1,1-dioxide as inhibitors of Escherichia coli β-ketoacyl-ACP-synthase III (FabH) by Alhamadsheh, Mamoun M., Waters, Norman C., Huddler, Donald P., Kreishman-Deitrick, Mara, Florova, Galina, Reynolds, Kevin A.

“…A series of cyclic sulfones has been synthesized and their activity against β-ketoacyl-ACP-synthase III (FabH) has been investigated. The compounds are…”
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cis-Δ2,3-Double Bond of Phoslactomycins Is Generated by a Post-PKS Tailoring Enzyme by Palaniappan, Nadaraj, Alhamadsheh, Mamoun M, Reynolds, Kevin A

“…The antifungal phoslactomycins (PLM A-F), produced by Streptomyes sp. HK803, are structurally unusual in that three of their four double bonds are in the cis…”
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Application of a Newly Identified and Characterized 18-O-Acyltransferase in Chemoenzymatic Synthesis of Selected Natural and Nonnatural Bioactive Derivatives of Phoslactomycins by Ghatge, Mohini S, Palaniappan, Nadaraj, Alhamadsheh, Ma'moun M, DiBari, Jessica, Reynolds, Kevin A

“…Phoslactomycins (PLMs) and related leustroducsins (LSNs) have been isolated from a variety of bacteria based on antifungal, anticancer, and other biological…”
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Elucidation of the Streptomyces coelicolor Pathway to 2-Undecylpyrrole, a Key Intermediate in Undecylprodiginine and Streptorubin B Biosynthesis by Mo, SangJoon, Sydor, Paulina K., Corre, Christophe, Alhamadsheh, Mamoun M., Stanley, Anna E., Haynes, Stuart W., Song, Lijiang, Reynolds, Kevin A., Challis, Gregory L.

“…The red gene cluster of Streptomyces coelicolor directs production of undecylprodiginine. Here we report that this gene cluster also directs production of…”
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Breaking protein-protein interactions: A combined chemical and computational approach to develop a new class of protein aggregation inhibitors by Graef, Isabella, Alhamadsheh, Mamoun M, Esteras-Chopo, Alexandra, Branson, Kim, Bose, Mohua, Pande, Vijay

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Design, Total Synthesis, and Evaluation of Novel Open-Chain Epothilone Analogues by Alhamadsheh, Mamoun M, Hudson, Richard A, Viranga Tillekeratne, L. M

“…The design, total synthesis, and biological evaluation of two open-chain analogues of epothilone incorporating the critical C1−C8 fragment and the aromatic…”
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Unsymmetric aryl–alkyl disulfide growth inhibitors of methicillin-resistant Staphylococcus aureus and Bacillus anthracis by Turos, Edward, Revell, Kevin D., Ramaraju, Praveen, Gergeres, Danielle A., Greenhalgh, Kerriann, Young, Ashley, Sathyanarayan, Nalini, Dickey, Sonja, Lim, Daniel, Alhamadsheh, Mamoun M., Reynolds, Kevin

“…A series of aryl–alkyl disulfides have been identified to have strong antibacterial activity against Staphylococcus aureus (including MRSA) and Bacillus…”
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Probing reactivity and substrate specificity of both subunits of the dimeric Mycobacterium tuberculosis FabH using alkyl-CoA disulfide inhibitors and acyl-CoA substrates by Sachdeva, Sarbjot, Musayev, Faik, Alhamadsheh, Mamoun M., Neel Scarsdale, J., Tonie Wright, H., Reynolds, Kevin A.

“…The dimeric Mycobacterium tuberculosis FabH (mtFabH) catalyses a Claisen-type condensation between an acyl-CoA and malonyl-acyl carrier protein (ACP) to…”
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