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The Significance of Membrane Transport

The Significance of Membrane Transport

The transport of solutes across the cell membrane is essential for metabolic processes, like maintaining cell size and volume, generating the action potential, exchanging nutrients and gases, etc. Membrane transport can be either passive or active. It can be simple diffusion, facilitated, or mediated transport aided by transport proteins such as transporters and channels.
Transporters facilitate either an active or passive movement of solutes. They can allow a single-molecule transport down its...

Membrane Transporters

Membrane Transporters

Transporters are essential membrane transport proteins with functions related to cell nutrition, homeostasis, communication, etc. Approximately 7% of all genes in the human genome code for transporters or transporter-related proteins.
Transporters are mainly composed of alpha-helices, built from bundles of ten or more helices traversing the plasma membrane. The solute-binding sites are located midway, where some of the helices are broken or distorted, making space for the binding site through...

Membrane Asymmetry Regulating Transporters

Membrane Asymmetry Regulating Transporters

Enzymes like flippase, floppase, and scramblase transfer phospholipids from one layer to another in the membrane, thereby affecting membrane asymmetry.
Flippase
Eukaryotic flippases are type-IV P-type ATPases or P4-ATPases belonging to P-type ATPase family proteins that are membrane-bound pumps involved in the ATP-mediated transport of ions and molecules across the membrane. Flippases flip specific phospholipids from the outer to the inner leaflet of a membrane. All P4-ATPases have one...

Physiological Pharmacokinetic Models: Incorporating Hepatic Transporter-Mediated Clearance

Physiological Pharmacokinetic Models: Incorporating Hepatic Transporter-Mediated Clearance

Drug transporters are critical in drug absorption, distribution, and excretion processes. They should be included in physiological-based pharmacokinetic (PBPK) models, which help predict human drug disposition. However, predicting this is challenging during drug development, especially when liver transport is involved. However, with a realistic representation of body transport processes, an accurate model may be possible.
A recent model describes pravastatin's hepatobiliary excretion,...

Facilitated Diffusion

Facilitated Diffusion

The plasma membrane, a critical structure in cellular biology, houses an array of transporters, or carrier proteins, interspersed within its lipid bilayer. These proteins play a crucial role in solute transport through facilitated diffusion, a form of passive diffusion that uses transporters to move the molecules across the membrane.
In this process, substrates such as organic compounds and ions interact with a transporter on one side, triggering conformational changes in proteins that enable...

ABC Transporters: Exporter

ABC Transporters: Exporter

ATP-binding cassette or ABC transporter is the largest superfamily of integral membrane proteins. The transporters have transmembrane-binding domains (TMDs) and nucleotide-binding domains (NBDs). The TMDs are specific to their substrates, whereas the NBDs are similar to engines that complete ATP hydrolysis to complete the substrate transport. They can be full transporters consisting of two TMDs and NBDs, half transporters with one TMD and NBD, while some encoded with a single TMD or NBD are...

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Related Experiment Video

Updated: Aug 5, 2025

Application of I TASSER, trRosetta, UCSF Chimera, HADDOCK server, and HEX loria for De Novo and In Silico Design of Proteins

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Homology Modeling of Transporter Proteins.

Ingebrigt Sylte¹, Mari Gabrielsen², Kurt Kristiansen²

¹Molecular Pharmacology and Toxicology, Department of Medical Biology, Faculty of Health Sciences, UiT The Arctic University of Norway, Tromsø, Norway. Ingebrigt.Sylte@uit.no.

Methods in Molecular Biology (Clifton, N.J.)

|March 24, 2023

Summary

Homology modeling generates 3D structures for membrane transporter proteins, crucial for drug discovery. Advances in computational power and available template structures enhance the accuracy and applicability of these models.

Keywords:

Carriers Channels and pores Homology modeling Model building and refinements Model validation Structure-based virtual screening Transporter proteins

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Published on: September 29, 2023

Area of Science:

Biochemistry and structural biology
Computational biology and bioinformatics

Background:

Membrane transporter proteins, including channels/pores and carriers, are vital drug targets.
Current lack of human transporter 3D structures impedes drug discovery and experimental research.

Approach:

This chapter reviews homology modeling for creating 3D structural models of membrane transporter proteins.
Utilizes advancements in template structures, algorithms for sequence alignment and prediction, and increased computational power.

Key Points:

Homology modeling is increasingly applicable for generating transporter protein structures.
Discusses template selection, alignment, model generation, optimization, and validation.
Highlights the use of models for structure-based virtual ligand screening.

Conclusions:

Homology modeling offers a viable approach to overcome structural data limitations for membrane transporters.
Facilitates structure-based drug design and discovery targeting these essential proteins.